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SML1759 CD1530 ≥98% (HPLC) CD1530 is a potent and selective agonist of retinoic acid receptor RARγ with Kd values of 150, 1,500, and 2,750 nM for RARγ, RARβ, and RARα receptors, respectively. In various studies, CD1530 has been shown to preserve human tendon stem cell characteristics, promote repair of injured skeletal muscle, and in combination with bexarotene to inhibit oral carcinogenesis.
C7249 CI-1033 ≥98% (HPLC) CI-1033 is a potent, irreversible ATP binding site–directed pan-ErbB tyrosine kinase inhibitor with IC50 in the low nanomolar range for EGFR, HER2, and ErbB-4.
human ... EGFR(1956), ERBB2(2064), ERBB4(2066)
C3743 CI 976 >98% (HPLC), solid CI-976, a new trimethoxy fatty acid anilide, is a potent and specific inhibitor of liver and intestinal acyl coenzyme A; cholesterol acyltransferase (ACAT) in vitro. CI-976 decreased non-high density lipoprotein (HDL)-cholesterol and increased HDL-cholesterol in rats with pre-established dyslipidemia. High performance gel chromatographic separation of plasma lipoproteins also revealed that CI-976, but not CL 277,082, lowered low density lipoprotein (LDL)-cholesterol and elevated HDL-cholesterol.
C0621 CI−994 ≥98% (HPLC), powder CI-994 is the acetylated derivative form of the original compound Dinaline (PD 104 208). It is an oral cytostatic drug with impressive differential activity against leukemic cells & normal stem-cells. It is used for combination therapy for selected tumors including non-small cell lung, pancreatic, breast, and colorectal cancers. It acts as a histone deacetylase inhibitor. CI-994 blocks cells in the G1-S phase of the cell cycle. The 16 kDa phosphoprotein is confined to the nuclear compartment. Loss of the 16-kDa nuclear phosphoprotein appears to be a direct effect of CI-994 treatment and that the inhibition of this phosphoprotein may play a critical role in the mechanism of action of CI-994.
human ... HDAC1(3065), HDAC10(83933), HDAC11(79885), HDAC2(3066), HDAC3(8841), HDAC4(9759), HDAC5(10014), HDAC6(10013), HDAC7(51564), HDAC8(55869), HDAC9(9734)
C1618 Cibenzoline succinate ≥98% (HPLC), solid Cibenzoline is a class IA antiarrhythmic drug. Cibenzoline (μM concentrations) blocks ATP-sensitive K channels in heart and pancreatic cells. Cibenzoline interacts with the channel pore-forming subunit of the K(ATP) channel (Kir6.2) from the cytoplasmic side. Cibenzoline also inhibits the delayed rectifier K current [I(Kr)] in sino-atrial node cells.
SML1955 Ciclesonide ≥98% (HPLC) Ciclesonide is a glucocorticoid antiasthmatic prodrug; it is de-esterified in the lung to the active metabolite.
SML2011 Ciclopirox ≥98% (HPLC) Ciclopirox is a chemical compound belonging to the class of hydroxypyridones. It is found active against dermatophytes, yeasts, molds, some bacterias and also azole-resistant Candida species. Unlike other antifungal agents that act for ergosterol inhibition, ciclopirox has a different action. It targets metal-dependent enzymes, which degrades fungal cell peroxides. This unique action of ciclopirox provides less chance for resistance in pathogenic fungi. This compound is used in topical formulations specifically for nails and skin.
Ciclopirox is an antifungal and cell-permeable iron-chelating agent. It has been found to inhibit multiple enzymes and signaling pathways including prolyl hydroxylase 2 (PHD2), eukaryotic translation initiation factor 5A (eIF5A), Wnt/β-catenin, hypoxia-inducible factor-1α (HIF-1 α)/vascular endothelial growth factor (VEGF), vascular endothelial growth factor receptor 3 (VEGFR-3), mammalian target of rapamycin (mTOR), and cyclin dependent kinases (CDKs). Ciclopirox has been shown to have anti-viral and anticancer activity in addition to its antifungal activity. Ciclopirox has also been shown to counteract glucotoxicity in diabetic mice in a p21-dependent manner.
SML0545   CID 1067700 ≥98% (HPLC) CID 1067700 antagonizes ras-related protein Rab-7 and reduces class switch DNA recombination (CSR) in B cells and survival of plasma cells.
CID 1067700 is a potent and competitive inhibitor of Ras-related GTPases that potently binds to Rab7 nucleotide binding site.
SML0698   CID 11210285 hydrochloride ≥98% (HPLC) CID 11210285 is a cell-permeable, potent and selective activator of Wnt signaling without inhibiting GSK-3β. CID 11210285is a Wnt agonist.
SML2043 CID 1375606 ≥98% (HPLC) CID 1375606 (N-[4-(Anilinocarbonyl)phenyl]-2,4-dichlorobenzamide) is a specific and potent surrogate agonist of GPR27 (SREB1) that induces coupling of the receptor to β-arrestin 2 but not to G proteins.
SML0805   CID16020046 ≥98% (HPLC) CID16020046 is a potent and a selective GPR55 antagonist that inhibits GPR55-mediated ERK1/2 phosphorylation. CID16020046 inhibits LPI-induced Ca2+ signaling in HEK-GPR55 cells.
SML0369 CID-2011756 ≥98% (HPLC) CID-2011756 is a cell-active ATP competitive and specific PKD1 inhibitor that inhibits phorbol ester-induced endogenous PKD1 activation in LNCaP prostate cancer cells.
SML0487   CID 2818500 ≥98% (HPLC) CID 2818500 (trans-α-Nitrostilbene; 1,1′-[(1Z)-1-Nitro-1,2-ethenediyl]bis-benzene) is a selective inhibitor of Protein Arginine Methyltransferases PRMT1 and PRMT8. PRMT1 is responsible for the majority of arginine methylation in the cell involved in transcription, chromatin modification, and signal transduction. CID 2818500 has an IC50 values of 11 μM for PRMT1, and does not inhibit PRMTs 3, 4, and 6, although it does inhibit PRMT8. The mechanism is believed to involve a specific S-adenosylmethionine (SAM)-binding cysteine present only in the Type I PRMTs PRMT1 and PRMT8 and absent in other SAM-dependent methyltransferases.
SML0634 CID2858522 ≥98% (HPLC) CID2858522 specifically inhibits NF-kB activation downstream of protein kinsase C (PKC). CID2858522 dose dependently inhibits NF-kB reporter activity in PMA-ionomycin stimulated HEK293 cells, but does not affect NF-kB activity in cells challenged with TNFa, retinoic acid, or stimulation of the toll-like receptor signaling pathway.
SML0918 CID44216842 ≥98% (HPLC) CID44216842 is a potent and selective non-competitive allosteric inhibitor of Cdc42 GTPase that does not inhabit Rho and Rac. CID44216842 inhibits Cdc42 dependent filopodia formation and cell migration.
SML0375 CID 5951923 ≥98% (HPLC) CID 5951923 is an inhibitor of Kruppel-like factor 5 (KLF5) expression that significantly reduced endogenous KLF5 protein levels and decreased viability of several colorectal cancer cell lines. CID 5951923 is selective for colon cancer cells over nontransformed cells.
SML0003 CID755673 ≥98% (HPLC), powder CID755673 is a cell-permeable, potent and selective inhibitor of all three protein kinase D (PKD) isoforms PKD1 (PKCμ), PKD2, and PKD3 (PKCν). CID755673 is not competitive with ATP.
CID755673 was not suitable to inhibit PKD in Swiss 3T3 cells as it utilizes PKD-dependent pathway to enhance the mitogenic signaling triggered by EGF, phorbol esters and bombesin. It should, therefore, be used with caution.
C5874 Cidofovir hydrate ≥98% (HPLC) Selective inhibitor of viral DNA synthesis through the selective inhibition of viral DNA polymerase.
C3974 Ciglitizone ≥98% (HPLC) Selective peroxisome proliferator-activated receptor-γ (PPARγ) agonist (EC50 = 3 μM) and antihyperglycemic agent displaying activity in genetically obese C57 B1/6 ob/ob mice.
human ... PPARG(5468)
mouse ... Pparg(19016)
C5492 CIL-102 ≥95% (HPLC), solid CIL-102 is a tubulin polymerization inhibitor: apoptosis inducer.
SML1594   Cilengitide trifluoroacetic acid salt ≥98% (HPLC) Cilengitide is a vascular targeting agent (VTA) that acts as an integrin antagonist. Cilengitide is a cyclized Arg-Gly-Glu(RGD)-containing pentapeptide that selectively blocks activation of the αvβ3 and αvβ5 integrins.
It exhibits antitumor activity in glioblastoma multiforme tumors. Integrins are heterodimers of α and β chain. They are transmembrane receptors which are responsible for cell-to-cell and cell-extracellular matrix interactions. They control tumor angiogenesis, invasion and migration.
C1493 Cilnidipine ≥98% (HPLC), powder Cilnidipine is a slow-acting Ca2+ channel blocker; antihypertensive; vasodilator; dual blocker of L-type voltage-gated Ca2+ channels in vascular smooth muscle and N-type Ca2+ channels in sympathetic nerve terminals that supply blood vessels. Cilnidipine may offer an advantage over nifedipine as the long term intake of the latter has been linked to increased risk of myocardial infarction and mortality in patients with coronary artery disease. Cilnidipine lowers blood pressure, but has less effect on sympathetic activity. Unlike nifedipine, cilnidipine does not inhibit PKC.
SML0733   Cilomilast ≥95% (HPLC) Cilomilast (SB-207499) is a potent, selective and orally available PDE4 inhibitor that exhibits anti-inflamatory and anti-asthmatic activity.
C0737 Cilostazol ≥98% (HPLC), powder Phosphodiesterase III (PDE3) inhibitor
human ... PDE3A(5139), PDE3B(5140)
C4522 Cimetidine H2 histamine receptor antagonist; I1 imidazoline receptor agonist; anti-ulcer agent. Blocks cancer metastasis by inhibiting the expression of E-selectin on the surface of endothelial cells, thus blocking tumor cell adhesion.
human ... ABCB1(5243), CYP1A2(1544), CYP3A4(1576), HRH2(3274), SLC9A2(6549), SLC9A5(6553)
mouse ... Abcb1a(18671), Abcb1b(18669)
rat ... Slc9a1(24782), Slc9a3(24784), Slc9a5(192215)
SML2012   Cinacalcet hydrochloride ≥98% (HPLC) Cinacalcet is a positive allosteric modulator of the Calcium Sensing Receptor (CaSR) that acts as a calcimimetic. It increases the sensitivity of the calcium-sensing receptor to extracellular calcium resulting in a decrease in serum calcium levels.
SML1532 Cinaciguat hydrochloride ≥98% (HPLC) Cinaciguat activates sGC (soluble guanylate cyclase) independently of NO. Cinaciguat binds to sGC′s NO-sensory H-NOX domain when it is heme-depleted. Also, the compound Cinaciguat protects sGC from oxidation-induced ubiquitin-triggered degradation.
Cinaciguat, also known as BAY 58-2667, is a novel activator of guanylate cyclase. It is used in the treatment of acute decompensated heart failure (ADHF). It has been reported that cinaciguat possesses cardiovascular effects.
C6239 Cinalukast ~98% (HPLC) Specific CysLT1 leukotriene receptor antagonist.
human ... CYSLTR1(10800)
SML1498 Cinepazide maleate ≥98% (HPLC) Cinepazide maleate is a vasodilator used clinically in China used in China for the treatment of cardiovascular and cerebrovascular diseases, and peripheral vascular diseases. Cinepazide maleate is thought to act as a potentiator of adenosine A2 receptors and has also been characterized as a calcium channel blocker. It was withdrawn for agranulocytosis in several countries.
SML1352 CINK4 ≥95% (HPLC) CINK4 is a specific inhbitor of CDK4/cyclin D1 complexes (IC50 = 1.5 mM). CINK4 has greater than 50 fold selectivity over CDK1 or CDK2. CINK4 dose-dependently inhibits phosphorylation of retinoblastoma (Rb) and induces G0-G1 cell cycle arrest and apoptosis in cancer cell lines.
SML0096 Cinnabarinic Acid ≥98% (HPLC) Caspase Inducer; mGlu4R agonist
Cinnabarinic acid (CA) connects between initiation of the kynurenine pathway and immune tolerance that is used to prevent neuroinflammation.
Cinnabarinic acid is a kynurenine pathway metabolite of tryptophan, produced by the oxidation of 3-Hydroxyanthranilic acid. Cinnabarinic acid leads to loss of mitochondrial respiration and apoptosis, and has also been shown to be an mGlu4R-specific agonist.
C5241   Cinnamycin from Streptomyces cinnamoneus, ≥95% (HPLC) Cinnamycin based analogs may be useful in treating cystic fibrosis or Clostridium infections.
Cinnamycin is a tetracyclic polypeptide antibiotic containing 19 amino acids. The polypeptide has the unusual amino acids threo-3-methyl-lanthionine, meso-lanthionine, lysinoalanine and 3-hydroxyaspartic acid. It is produced by Streptomyces cinnamoneus and belongs to the duramycin-type l antibiotics. Lantibiotics are synthesized in the ribosome and undergo extensive post-translational modifications to attain their active antimicrobial form. The unique receptor for Cinnamycin, phosphatidylethanolamine (PE), is located on the inner leaflet of the plasma membrane. Cinnamycin induces transbilayer lipid movement leading to the exposure of PE to the outer leaflet of the plasma membrane. The interaction of Cinnamycin with PE provides a tool for PE monitoring. Cinnamycin is active against Gram-positive rods such as Bacilli, Clostyridium and Mycobacterium, causing cell wall biosynthesis stress.
Cinnamycin, like other lantibiotics, was also reported to inhibit phospholipase A2 (PLA2). It was suggested as an alternative treatment for atherosclerosis through its ability to inhibit PLA2 by binding to its substrate PE. Moreover, Cinnamycin was found to inhibit Herpes simplex virus (HSV-1) activity.
SML0105 Cinnamyl-3,4-dihydroxy-α-cyanocinnamate ≥98% (HPLC) Cinnamyl-3,4-dihydroxy-α-cyanocinnamate (CDC) is a potent and direct inhibitor of 5-LO (5-Lipoxygenase) that reduces 5-LO activity in cell-free assays. CDC also inhibits 12-LO and 15-LO
C5270 Cinnarizine powder Ca2+ channel blocker; central and peripheral vasodilator.
Cinnarizine is a piperazine and a specific anti-vertigo agent. It is used to treat and prevent vertigo and motion sickness. In addition, cinnarizine is also used as an anti-histamine agent. Chronic use of this drug leads to side effects such as extrapyramidal reactions (Parkinson, tremor and akathisia) and depression.
human ... CACNA1A(773), CACNA1C(775), CACNA1D(776), CACNA1F(778), CACNA1S(779), DRD2(1813), HRH1(3269)
C1147 Cinobufotalin    
SML2468 CINPA1 ≥98% CINPA1 is a ligand-binding domain (LBD)-targeting constitutive androstane receptor (CAR) inhibitor that prevents CAR recruitment to promoter regions of regulated genes (by >85%; 1 μM CINPA1 against 0.1 μM CITCO-induced CAR recruitment to CYP2B6 or CYP3A4 promoters; human hepatocytes) by altering CAR-coregulator interactions. CINPA1 inhibits CAR-mediated transcription in a potent (IC50 = 70 nM; HepG2-hCAR1 CYP2B6-luc reporter cells) and selective manner with only weak PXR antagonist potency (68% inhibition by 18 μM CINPA1 against 5 μM rifampicin; HepG2-PXR reporter cells) and no cytotoxicity or agonist/antagonist activity toward FXR, GR, LXRα/β, PPARγ, RXRα/β, VDR.
SML0366 Cipamfylline ≥98% (HPLC) Cipamfylline is a PDE4 inhibitor that has been shown to cause a cellular redistribution of PDE4A4 into accretion foci, through an association with the ubiquitin scaffolding protein p62.
C0330 Ciprofibrate Peroxisome proliferator-activated receptor α (PPARα) agonist
human ... PPARA(5465)
C6492 Ciproxifan hydrochloride ≥98% (HPLC), solid Ciproxifan belongs to a novel chemical series of histamine H3-receptor antagonists. In vitro, it behaved as a competitive antagonist at the H3 autoreceptor controlling 3H histamine release from synaptosomes and displayed similar Ki values (0.5-1.9 nM) at the H3 receptor controlling the electrically-induced contraction of guinea pig ileum or at the brain H3 receptor labeled with 125I-iodoproxyfan. Ciproxifan appears to be an orally bioavailable, extremely potent and selective H3-receptor antagonist whose vigilance- and attention-promoting effects are promising for therapeutic applications in aging disorders.
C6848 Ciproxifan maleate ≥98% (HPLC), powder Potent, selective H3 histamine receptor antagonist.
SML0229   CIQ ≥98% (HPLC) CIQ is positive allosteric modulator of NR2C/NR2D subunit containing NMDA receptors. CIQ increases channel opening frequency of recombinant NR2Cor NR2D containing receptors by two-fold (EC50 = 2.7 and 2.8 μM, respectively), with no effect on NR2A or NR2B subtypes. The compound does not alter the EC50 values for glutamate or glycine on channel opening.
C223 Cirazoline hydrochloride solid Selective α1-adrenoceptor agonist; non-selective imidazoline binding site ligand
human ... ADRA1A(148), ADRA1B(147), ADRA1D(146)
SML0953   Cirsiliol ≥95% (HPLC) Cirsiliol is a flavonoid that displays anti-inflammatory, anti-oxidant, anti-proliferative, and anti-bacterial activities. Cirsiliol sensitizes non-small cell lung cancer cell lines (NSCLC) to radiation therapy. Cirsiliol inhibits epithelial-mesenchymal transition likely by induction of tumor-suppressive miR-34a, which suppresses Notch-1 expression NSCLC.
C4740 Cisapride monohydrate ≥98% (HPLC), solid 5-HT4 serotonin receptor agonist.
SML0727   cisTPD ≥98% (HPLC) cisTPD is a constitutive androstane receptor (CAR) agonist that inhibits FOXO1 and HNF4 driven expression of the gluconeogeneis PEPCK and glucose-6-phosphatase. cisTPD reduces blood glucose levels, insulin sensitivity and weight gain in rats fed a high fat diet.
C7861 Citalopram hydrobromide ≥98% (HPLC) Potent and selective serotonin uptake inhibitor (Ki = 5.4 nM); antidepressant
human ... HTR1A(3350), HTR1B(3351), HTR1D(3352), HTR1E(3354), HTR1F(3355), HTR2A(3356), HTR2B(3357), HTR2C(3358), HTR3A(3359), HTR3B(9177), HTR3C(170572), HTR3D(200909), HTR3E(285242), HTR4(3360), HTR5A(3361), HTR5B(645694), HTR6(3362), HTR7(3363), SLC6A4(6532)
C6240 CITCO ≥98% (HPLC), solid CITCO is a constitutive androstane receptor (CAR) agonist; nuclear receptor NR113 agonist.
C1017 Citrinin from Penicillium citrinum, ≥98% (HPLC)    
SML0187 CJ-13610 ≥98% (HPLC) CJ-13,610 is a potent inhbititor of 5-lipoxygenase (5-LO) activity (IC50 = 70 nM).
CJ-13610 inhibits the biosynthesis of leukotriene B4 and regulates the IL-6 mRNA expression in macrophages. It reduces fibrosis and necroinflammation of liver in carbon tetrachloride-treated mice.
SML0080 CJB 090 dihydrochloride hydrate ≥98% (HPLC) CJB 090 is a Dopamine D3 receptor partial agonist. CJB 090 was found to attenuate the discriminative stimulus (DS) effects of cocaine while showing no cocaine-like effects when tested alone, and has also been shown to reduce methamphetamine self-administration.
C7499 CK-548 ≥98% (HPLC) CK-548 inhibits the activity of actin-related protein (Arp)2/3 complex by inserting into the hydrophobic core of Arp3 and altering its conformation: inhibits
C7374 CK-636 ≥98% (HPLC) CK-636 binds between Arp2 and Arp3, where it appears to block movement of Arp2 and Arp3 into their active conformation. CK-636 inserts into the hydrophobic core of Arp3 and alters its conformation. Both classes of compounds inhibit formation of actin filament comet tails by Listeria and podosomes by monocytes.
SML0006 CK-666 ≥98% (HPLC), powder CK-666 binds to Arp2/3 complex, stabilizes the inactive state of the complex and prevents its movement into active conformation.
CK-666 is a cell-permeable inhibitor of actin assembly mediated by actin-related protein Arp2/3 complex.
C9124   CK-869 ≥98% (HPLC) CK-869 is a cell-permeable inhibitor of actin assembly mediated by the actin-related protein Arp2/3 complex of human and bovine, but not yeast. The actin-related protein Arp2/3 complex plays a major role in the regulation of the actin cytoskeleton. Apparently the compound binds to the hydrophobic core of Arp3 and alters its conformation.
C0742 CKI-7 dihydrochloride ≥98% (HPLC), solid CKI-7 is a CK1 inhibitor; also inhibits SGK, S6K1 and MSK1. CKI-7 inhibits SGK as potently as CK1. IC50 = 6 μM.
SML2235 CL075 ≥98% (HPLC) CL075 is a selective agonist of Toll-like receptor-8 (TLR-8) with immunostimulant activity. It showed an EC50 value of 400nM for IRF-NFΚB stimulation in TLR8 compared to 4 μM for TLR7.
SML2566 CL097 ≥98% (HPLC) CL097 is an imidazoquinoline (IMDQ) derivative (IQD) with dual toll-like receptor 7 & 8 (TLR7 & TLR8; TLR7/8) agonist activity. CL097 is commonly employed in the concentration range from 0.5 μg/mL to 45 μg/mL for stimulating cell surface TLR7/8 in cultures and is reported to be a stronger TLR7 ligand than CL075.
C5976 CL 316,243 hydrate ≥98% (HPLC), powder CL 316,243 is a β3 adrenoceptor agonist; anti-obesity agent.
β Adrenoceptor is expressed in a number of tissues such as heart, adipose tissue, colon and other tissues. It is associated with many different biological functions. β Adrenoceptor fills in as an objective for treating type 2 diabetes, heart failure, cachexia, obesity, metabolic disorder, issues related with bladder, colon and malignant tumor growth. Depression and anxiety can also be treated via β adrenoceptor. CL 316,243 is known to have antidiabetic action via β adrenoceptor. It is a potent stimulator of lipolysis. It also activates β3- adrenoceptors on neurons in hypothalamic areas that are important in the central regulation of appetite.
human ... ADRB3(155)
C9498 CL-82198 ≥98% (HPLC), powder CL-82198 is a selective inhibitor of MMP-13 that displays no activity at MMP-1, MMP-9 or TACE. It is also a selective S1′ pocket binder, binding within the entire S1′ pocket of MMP-13, docking with the morpholine ring adjacent to the catalytic zinc atom without zinc chelation.
SML1545   Claramine trifluoroacetate salt ≥98% (HPLC) Claramine is a more conveniently-manufactured lead compound for the derivation of therapeutic agents. It is believed to be useful for the treatment of type II diabetes. Claramine is capable of crossing blood brain barrier (BBB) and is thought to mediate its action through hypothalamus, which is responsible for maintaining metabolic homeostasis. Claramine A1 is found effective against multidrug resistant bacteria and nosocomial diseases.
Claramine is a protein tyrosine phosphatase 1B (PTP1B) inhibitor, an analog of Trodusquemine. Like Trodusquemine, Claramine is a selective inhibitor of protein tyrosine phosphatase 1B (PTB1B), and not its closest related phosphatase TC-PTP. Claramine activated insulin signaling, increasing phosphorylation of insulin receptor-β (IRβ), Akt and GSK3β. It improved insulin sensitivity, restoring glycemic control in diabetic mice, and caused weight loss by suppressing food intake.
L7035 clasto-Lactacystin β-lactone Cell-permeable and irreversible proteasome inhibitor. Lactacystin acts as a precursor for clasto-lactacystin β-lactone.
SML1798 10-Cl-BBQ ≥98% (HPLC) 10-Cl-BBQ is an orally bioavailable, non-toxic benzimidazoisoquinoline derivative that acts as an aryl hydrocarbon receptor (AhR) agonist via directly binding to AhR (IC50  = 2.6 nM in a competitive binding assay) and induces its nuclear translocation. 10-Cl-BBQ is shown to increase CD4+  T-cells that co-express CD25, CTLA-4 and ICOS, as well as several other genes associated with regulatory T cell (Treg) function in a graft versus host response model (GVH, C57BI/6 T cells injected into B6D2F1 host mice). 10-Cl-BBQ displays good pharmacokinetic profile in mice (t1/2 = 2 h, Cmax = 21.5 μg/L, 10 mg/kg, i.p.). Also shown to prevent insulitis in a NOD T1D mouse model which is independent of Fox3 +  Tregs (60 mg/kg, p.o, q.o.d.).
SML0445 Clemastine fumarate salt ≥98% (HPLC) Clemastine fumarate is an antihistamine H1-antagonist and anticholinergic that also has antipruritic activity.
human ... HRH1(3269)
SML1447 Clemizole hydrochloride ≥98% (HPLC) Clemizole is a potent and preferring inhibitor of TRPC5 that efficiently blocks heterologously expressed homomeric TRPC5 channels as well as heteromeric TRPC1:TRPC5 channels. Clemizole is a potent and selective H1 histamine receptor antagonist. Clemizole inhibited binding of HCV RNA by NS4B inhibit HCV RNA replication in cell culture.
Clemizole is an antihistamine and an inhibitor of NS4B (nonstructural protein 4B) RNA of HCV (hepatitis C virus). Studies in Scn1α (sodium channel, voltage-gated, type I, α) Zebrafish mutant show that this drug has the potential as a therapeutic agent in Dravet Syndrome treatment.
C5423 Clenbuterol hydrochloride ≥95% Clenbuterol hydrochloride is a β2-adrenoceptor agonist and bronchodilator. It is effective in improving peak expiratory flow rate (PEFR) in asthma patients. Clenbuterol is also a performance-enhancing drug as it stimulates the central nervous system and improves oxygen transport. Clenbuterol elicits cardio protective functionality in patients with dilated cardiomyopathy.
human ... ADRB2(154)
SML2607 Clevidipine Butyrate ≥98% (HPLC) Clevidipine is a short acting, third generation dihydropyridine calcium channel blocker that is highly selective for vascular L-type calcium channels. Clevidipine has no effect on myocardial contractility or cardiac conduction.
C8414 Clobazam Clobazam interacts at α and γ2 subunits junction of the GABAA receptor. It is less sedative and elicits anxiolytic and anticonvulsant effects. Clobazam is more selective on the α2 subunit of the GABAA receptor than the α1 subunit. It is an antiseizure drug and is associated with antiepileptic activity. Clobazam is useful in treating chronic epileptic encephalopathy disorder, Lennox‐Gastaut syndrome. It is employed in epilepsy and seizure prevention adjunctive therapy.
human ... GABRA1(2554), GABRA2(2555), GABRA3(2556), GABRA4(2557), GABRA5(2558), GABRA6(2559), GABRB1(2560), GABRB2(2561), GABRB3(2562), GABRD(2563), GABRE(2564), GABRG1(2565), GABRG2(2566), GABRG3(2567), GABRP(2568), GABRQ(55879)
C7495 Clofarabine ≥98% (HPLC) Clofarabine is a purine nucleoside antimetabolite. Clofarabine is toxic to nondividing lymphocytes and monocytes.
Clofarabine is a second-generation nucleoside analog, used in cancer treatments. Clofarabine is metabolized to 5′-triphosphate and is known to block DNA synthesis. The human equilibrative nucleoside transporters (hENT1 and hENT2) and human concentrative nucleoside transporter (hCNT2 and hCNT3) mediates clofarabine transport into the cell. It also serves as a substrate for mitochondrial deoxyguanosine kinase. Clofarabine is an inhibitor of ribonucleotide reductase. It resists the phosphorolytic cleavage catalyzed by purine nucleoside phosphorylase of bacterias. Clofarabine also withstands deamination by adenosine deaminase.
human ... POLA1(5422), POLA2(23649), POLD1(5424), POLD2(5425), POLD3(10714), POLD4(57804), POLE(5426), POLE2(5427), POLE3(54107), PRIM1(5557), PRIM2(5558), RRM1(6240), RRM2(6241), RRM2B(50484)
C8895 Clofazimine    
C6643 Clofibrate liquid Peroxisome proliferator-activated receptor-α (PPARα) agonist. Antihyperlipoproteinemic believed to act by inhibiting cholesterol biosynthesis.
human ... PPARA(5465)
mouse ... Ppara(19013)
C2365 Clofilium tosylate >97%, solid K+ channel blocker; cardiac depressant; anti-arrhythmic
C7291 Clomipramine hydrochloride ≥98% (HPLC), powder Clomipramine hydrochloride (CLP) is a amphiphilic drug, with two benzene rings in its structure. It exhibits anti-depressant property by restoring the equilibrium of certain natural materials in the human being. CLP acts as a potential therapeutic for obsessive compulsive disorder.
Tricyclic antidepressant; inhibits serotonin and norepinephrine transporters.
human ... HTR1A(3350), HTR1B(3351), HTR1D(3352), HTR1E(3354), HTR1F(3355), HTR2A(3356), HTR2B(3357), HTR2C(3358), HTR3A(3359), HTR3B(9177), HTR3C(170572), HTR3D(200909), HTR3E(285242), HTR4(3360), HTR5A(3361), HTR5B(645694), HTR6(3362), HTR7(3363), SLC6A4(6532)
C1277 Clonazepam powder Anticonvulsant; ligand for the GABAA receptor benzodiazepine modulatory site.
human ... GABRA1(2554), GABRA2(2555), GABRA3(2556), GABRA4(2557), GABRA5(2558), GABRA6(2559), GABRB1(2560), GABRB2(2561), GABRB3(2562), GABRD(2563), GABRE(2564), GABRG1(2565), GABRG2(2566), GABRG3(2567), GABRP(2568), GABRQ(55879)
rat ... Tspo(24230)
C7897 Clonidine hydrochloride solid α2-adrenoceptor agonist; I1 imidazoline binding site ligand.
Clonidine hydrochloride is used for management of hypertension in pregnant women. In addition, it also acts as a therapeutic for neonatal abstinence syndrome. Clonidine hydrochloride binds to central α-adrenergic receptors and reduces the efferent sympathetic neuronal vasoconstrictor tone to the heart, kidneys and peripheral vasculature leading to vasodilatation and reduction in the blood pressure.
human ... ADRA2A(150), ADRA2B(151), ADRA2C(152)
SML0530 Clonixin ≥98% (HPLC) Clonixin is a non steroidal anti inflammatory drug (NSAID) with analgesic properties. The compound has been reported to block prostaglandin synthesis, and to block inward calcium currents.
SML0004 (S)-(+)-Clopidogrel hydrogensulfate ≥98% (HPLC) (S)-(+)-Clopidogrel hydrogen sulfate is an antithrombotic antiplatelet agent. It specifically and irreversibly inhibits the Purinoceptor P2Y12 subtype which inhibits ADP-induced platelet aggregation. (S)-(+)-Clopidogrel hydrogen sulfate is the active isomer.
human ... P2RY12(64805)
C0614 (±) Clopidogrel hydrogensulfate ≥98% (HPLC), powder Inhibits ADP-induced platelet aggregation; anti-thrombotic drug.
C6116 (+/-)-Cloprostenol sodium salt hydrate ≥98% (HPLC), powder Cloprostenol is a potent FP prostanoid receptor agonist. It is 2- to 3-fold more potent than fluprostenol but less selective. Cloprostenol is similar in potency to PGF at EP and TP prostanoid receptors. It is used for the treatment of infertility in sows and gilts.
C4615 Cloricromene ≥98% (HPLC), solid Antithrombotic coumarin derivative that inhibits platelet and leukocyte function and suppresses arachidonic acid liberation by interfering with PLA2 activation.
SML1154   Clostridium difficile Toxin A ≥95% (SDS-PAGE) Clostridium difficile Toxin A and B, cation-dependent UDP-glucose glucosyltransferases, are cellular toxins that inactivate Rho (and Rho family small GTPases) through monoglucosylation of these family members. TcdA elicits effects primarily within the intestinal epithelium. Effects of this monoglucosylation include disregulation of the actin cytoskeleton, cell rounding, cytotoxicity, and altered cellular signaling. Rho proteins are monoglucosylated by Toxin A and B using UDP-glucose as a cosubstrate. Rho, Rac and Cdc42 are included in the Rho subfamilies targeted by both toxins. Low molecular mass GTP-binding proteins that are not modified by Toxin A and B include Ras, Rab, Arf, or Ran subfamilies as well as heterotrimeric G proteins.
SML1153   Clostridium difficile Toxin B ≥95% (SDS-PAGE) Clostridium difficile Toxin A and B, cation-dependent UDP-glucose glucosyltransferases, are cellular toxins that inactivate Rho (and Rho family small GTPases) through monoglucosylation of these family members. Effects of this monoglucosylation include disregulation of the actin cytoskeleton, cell rounding, cytotoxicity, and altered cellular signaling. Rho proteins are monoglucosylated by Toxin A and B using UDP-glucose as a cosubstrate. Rho, Rac and Cdc42 are included in the Rho subfamilies targeted by both toxins. Low molecular mass GTP-binding proteins that are not modified by Toxin A and B include Ras, Rab, Arf, or Ran subfamilies as well as heterotrimeric G proteins.
Inactivates Rho (and Rho family small GTPases). Causes disregulation of the actin cytoskeleton, cell rounding, cytotoxicity, and altered cellular signaling.

Clostridium difficile is a bacteria that causes antibiotic-associated pseudomembranous colitis. This bacterium produces two high molecular weight exotoxins, toxin A and B. Toxin B is more effective than toxin A in disrupting human colonic epithelium in vitro.
Toxin B is 100-1,000-fold more cytotoxic than toxin A in inducing rounding-up of cells and destruction of the actin cytoskeleton.
C6019 Clotrimazole Clotrimazole is a specific inhibitor of Ca2+-activated K+ channels. It is an antifungal azole. Clotrimazole is a derivative of imidazole and has similar antimicrobial action and activity to ketoconazole. It inhibits cytochrome P450-dependent 14α-demethylase, which is critical to ergosterol biosynthesis. The accumulated 14α-methylated sterols change the membrane structure of sensitive fungi, altering cell membrane permeability.
human ... ABCB1(5243), CYP17A1(1586), CYP3A4(1576)
mouse ... Abcb1a(18671), Abcb1b(18669)
C6305 Clozapine Atypical antipsychotic compound. Selective antagonist for D4-dopamine receptor. Antagonist at 5-HT2A, 5-HT2C, 5-HT3, 5-HT6, and 5-HT7 serotonin receptors.
human ... ADRA1A(148), ADRA2A(150), ADRA2C(152), CHRM1(1128), DRD2(1813), DRD3(1814), DRD4(1815), HRH1(3269), HRH4(59340), HTR2A(3356), HTR2C(3358), HTR3A(3359), HTR3B(9177), HTR3C(170572), HTR3D(200909), HTR3E(285242), HTR6(3362), HTR7(3363), KCNH1(3756), KCNH2(3757), UGT1A4(54657)
rat ... Adra1a(29412), Adra2a(25083), Adrb1(24925), Chrm1(25229), Drd1a(24316), Drd2(24318), Drd3(29238), Drd4(25432), Hrh1(24448), Htr1a(24473), Htr1b(25075), Htr2a(29595), Htr2b(29581), Htr2c(25187), Htr3a(79246), Htr7(65032), Slc6a4(25553)
C0832 Clozapine N-oxide 5-HT2 serotonin receptor antagonist; major metabolite of clopazine that can be monitored by HPLC.
SML1368 CLP257 ≥98% (HPLC) CLP257 is a selective K+-Cl cotransporter KCC2 activator that restored impaired Cl transport in neurons with reduced KCC2 activity. Apparently, CLP257 modulates plasmalemmal KCC2 protein turnover post-translationally.
In streptozotocin treated rats, by activating a K+- Cl- cotransporter 2 (KCC2) in the arginine-vasopressin neuron, CLP257 mediates γ-aminobutyric acid (GABA)ergic excitation. It is however inactive with KCC1, KCC3 and KCC4.
SML2172 CLP290 ≥98% (HPLC) CLP290 is a small molecule enhancer of KCC2 activity. It is an orally active and more bioavailable precursor of the selective K+-Cl- cotransporter KCC2 activator CLP257. CLP290 was recently shown to restore Cl- transport and rescue morphine-induced hyperalgesia (MIH) in morphine-treated rats.
SML1359 CM037 ≥97% (HPLC) CM037 is a potent and selective inhibitor of human aldehyde dehydrogenase 1A1 (ALDH1A1). CM037 binds to the aldehyde binding pocket of ALDH1A1.
SML2784 CMPD101 hydrochloride ≥98% (HPLC) CMPD101 is an active site-targeting, potent and subtype-selective G protein-coupled receptor kinase GRK2 & GRK3 inhibitor (human GRK2/3 IC50 = 54/32 nM with 3 μM ATP and tubulin dimer as substrate; bovine GRK2 IC50 = 290 nM with 0.5 mM ATP and bROS as substrate; no GRK1/5 inhibition at 125 μM). CMPD101 selectively inhibits GPR39 agonist-induced β-arrestin recruitment (by 94% at 10 μM against 30 μM GPR39-C3/50 μM ZnCl2), but not cAMP pathway desensitization in cultures and prevents β-arrestin2-biased D2R ligand UNC9994(1 μg/side bilateral local injection) from blocking NMDAR antagonist PCP (6 mg/kg i.p.)-induced locomotion (60%/12% blockage without/with 0.5 μg CMPD101 co-injection) in mice in vivo.
SML1584 CMPPE ≥95% (HPLC) CMPPE is a GABAB receptor positive allosteric modulator (PAM). GABAB receptor positive allosteric modulators have potential for treatment of many neuro-psychiatric disorders as well as drug dependence and seizures. The receptor is a GPCR expressed throughout the CNS; it acts as both an auto-receptor and heteroreceptor to mudulate GABA release and regulate K+ channels and Ca++ channels. CMPPE has the highest hypoactivity/anticonvulsant ratio.
SML0302 4-CMTB ≥98% (HPLC) 4-CMTB is a phenylacetamide compound that acts as an allosteric modulator for the activity of short-chain fatty acid ligand in the FFA2 receptor.
4-CMTB is a potent allosteric agonist of free fatty acid receptor 2 (FFA2).
C127 CNQX ≥98% (HPLC), solid Potent, competitive AMPA/kainate glutamate receptor antagonist.
rat ... Gria1(50592), Grik1(29559), Grik2(54257), Grik4(24406), Grin2a(24409)
C239 CNQX disodium salt hydrate ≥98% (HPLC), solid CNQX(6-cyano-7-nitroquinoxaline-2,3-dioneis) is a potent, competitive AMPA/kainate receptor antagonist. It is a quinoxaline derivative and also an antagonist for non-N-methyl-d-aspartate (non-NMDA) glutamate receptor. CNQX mediates depolarization thalamic reticular nucleus via α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid receptors (AMPARs). It displays micromolar affinity towards AMPA/kainate receptor.
Potent, competitive AMPA/kainate receptor antagonist.
human ... ADORA1(134), ADORA2A(135), ADORA2B(136), ADORA3(140), GRIA1(2890), GRIA2(2891), GRIA3(2892), GRIA4(2893)
C4238 CNS-1102 >98% (HPLC), solid Noncompetitive NMDA glutamate receptor antagonist.
C8912 Cocaine free base Inhibits the dopamine, norepinephrine, and serotonin transporters with Kis of about 300 nM, 900 nM, and 400 nM, respectively. Unlike amphetamines, it has no effect on catecholamine release.
human ... DRD3(1814), KCNH1(3756), KCNH2(3757), SCN10A(6336), SCN11A(11280), SCN5A(6331), SLC6A2(6530), SLC6A3(6531), SLC6A4(6532)
mouse ... Slc6a2(20538)
rat ... Chrm1(25229), Slc6a3(24898), Slc6a4(25553)
C5776 Cocaine hydrochloride Inhibits the dopamine, norepinephrine, and serotonin transporters with Kis of about 300 nM, 900 nM, and 400 nM, respectively. Unlike amphetamines, it has no effect on catecholamine release.
C8081 Coenzyme Q2 ≥90% Acts as an electron carrier and antioxidant in humans
C9538 Coenzyme Q10 ≥98% (HPLC) Coenzyme Q10 is an endogenous cellular antioxidant and an essential component of the electron transfer chain. CoQ10 takes part in aerobic cellular respiration and generation of energy in the form of ATP.
SML2264 Col003 ≥98% (HPLC) Col003 is a cell penetrant, selective and potent inhibitor of the interaction of Hsp47 with collagen. It binds to the collagen binding site on Hsp47. Col003 inhibits a collagen secretion by destabilization the collagen triple helix. Additionally Col003 weakly inhibits interaction of collagen with prolyl 4-hydroxylase (P4H).
C9754 Colchicine ≥95% (HPLC), powder Antimitotic agent that disrupts microtubules by binding to tubulin and preventing its polymerization. Stimulates the intrinsic GTPase activity of tubulin. Induces apoptosis in several normal and tumor cell lines and activates the JNK/SAPK signaling pathway.
human ... ABCB1(5243), CYP3A4(1576), TUBA1A(7846), TUBA1B(10376), TUBA1C(84790), TUBA3C(7278), TUBA3E(112714), TUBA4A(7277), TUBB(203068), TUBB1(81027), TUBB2A(7280), TUBB2B(347733), TUBB3(10381), TUBB4A(10382), TUBB4B(10383), TUBB6(84617), TUBB8(347688)
mouse ... Abcb1a(18671), Abcb1b(18669)
C7744 Combretastatin A4 ≥98% (HPLC), powder Combretastatin A4 is a potent microtubule targeting agent (MTA).
Combretastatin A4 is a vascular disrupting agent (VDA) that targets tumor vasculature to inhibit angiogenesis. It inhibits tubulin polymerization at the colchicine-binding site of beta-tubulin. It has antitumor activity by inhibiting AKT function in human gastric cells. The inhibited AKT activation causes decreased cell proliferation, cell cycle arrest, and reduced in vitro migration/invasiveness and in vivo metastatic ability. Combretastatin A4 is a natural stilbenoid phenol.
C2313   Compound 48/80 Compound 48/80 (C 48/80) is a hypotensive agent, which promotes release of histamine. C 48/80 reduces the phagocytic ability of hemocytes in Styela plicata. C 48/80 promotes degranulation of mast cells. It Inhibits calmodulin, phospholipase C, endoplasmic reticulum (ER) Ca2+ ATPase and activates G proteins.
SML2858 Compound 8918 ≥98% (HPLC) New Compound 8918 is an orally active, non-cytotoxic, phosphopantethein (Ppt)-binding pocket-targeting, non-competitive M. tuberculosis (Mtb) Ppt transferase (PptT) inhibitor (IC50 = 2.5 μM, Emax 80-90%) that exhibits mycobactericidal activity (MIC90 = 0.56-3 μM/29 clinical Mtb isolates; MBC99 = 6.25 μM/Mtb, 3.13 μM/M. smegmatis) with no bactericidal potency against S. aureus, E. coli, P. aeruginosa, Streptomyces or C. albicans. Oral administration is efficacious against H37Rv replication in mouse lung in vivo (by 100%; 100 mg/kg/d, 4 d/wk for 2 wks). Mutations in MtbH37Rv rv2794c (PptT) or rv279c (Ppt hydrolase, PptH) gene confers 8918 resistance.
SML2017 Compound C108 ≥98% (HPLC) C108 is a small molecule that exhibits cancer-selective cytotoxicity (Viability = 100%/MCF-10A vs. 50%/BT-474, 67%/4T1, 70%/MDA-MB-231 & MDA-MB-453 post 48 h 1 μM C108 treatment) and synergizes with low dose paclitaxel in reducing ALDH-positive tumor-initiating cells (TIC poulation = 56.6%/control, 60.6%/0.1 μM paclitaxel alone, 47.4%/1 μM C108 alone, 7.3%/combined treatment for 24 h in BT474 breast cancer cultures) by targeting stress granule-associated protein G3BP2 (GAP SH3 domain-binding protein 2). Likewise, C108 pretreatment prior to xenografting greatly reduces BT-474 tumor-initiating frequency (from 1/175 to 1/1103 by limiting dilution xenograft assays) in mice in vivo. G3BP2 is reported to bind and stabilize SART3 mRNA, thereby indirectly regulating the core pluripotency transcription factors Oct-4 and Nanog critically involved in ESC self-renewal and breast tumor initiation.
C1733 [Glu3,4,7,10,14]-Conantokin G >90% (HPLC) Highly conserved polypeptide NMDA glutamate receptor antagonist; acts through a potent noncompetitive inhibition of polyamine responses; approximately 7-fold more potent than spermine
C9705 Concanamycin A ≥70% (HPLC) Concanamycin A (ConA) inhibits acidification of organelles and perforin-mediated cytotoxicity. It is a vacuolar-type v-ATPase inhibitor. ConA possesses antiprotozoal and antineoplastic properties. It mediates inhibition of the negative factor (Nef) protein of the human immunodeficiency virus.
SML0095 Conessine ≥97% (HPLC) Conessine is a plant steroid alkaloid that acts as a potent and specific antagonist of histamine H3 receptors (Ki = 5.37 and 24.5 nM for human and rat receptors, respectively). Conessine is 1860-fold selective for H3 over H4 and does not bind to H1 or H2 receptors. The molecule also binds to the human α2C4 adrenergic receptor (pKi = 7.98).
SML2261 Conivaptan hydrochloride ≥98% (HPLC) Conivaptan hydrochloride is a novel dual Arginine vasopressin receptor (AVP-R) antagonist for AVP-R types 1a (V1a) and V2-R. Conivaptan potently inhibits AVP-induced intracellular signaling through human V2 and V1a receptors with no agonistic activity.
SML2627   Connexin43 mimetic peptide 5 trifluoroacetate salt ≥95% (HPLC) Connexin43 mimetic peptide 5 is a blocker of connexin43 hemichannels that inhibits gap junction channels following CNS injury. Peptide 5 was designed to bind to extracellular regions of the connexin43 protein.
C3394 Cordycepin from Cordyceps militaris Cordycepin is an adenosine analogue that is readily converted to cordycepin 5′-triphosphate; can be used for 3′-end labeling of RNA.
rat ... Adora1(29290)
SML0496   CORM-3 CO possesses anti apoptotic function and offers protection against oxidative damage, promoting endothelial healing. CORM-3 is known to have therapeutic effects in transplantation, myocardial infarction and rheumatoid arthritis.
CORM-3 is a water-soluble carbon monoxide (CO) releasing molecule that can be used to study the effects of CO on cellular systems. Carbon monoxide (CO), produced during the degradation of heme by the enzyme heme oxygenase, has recently been found to be an important gaseous signaling mediator in mammalian cells CORM-3 has been shown to have anti-inflammatory and cardioprotective activity.
SML1930 CORM-401 CORM-401 (Mn(CO)4(S2CNMe(CH2CO2H))) is a manganese-containing carbon monoxide-releasing molecule (CORM) that generates at least three molar equivalents of CO. Due to reversible binding of CO, CORM-401 is relatively stable in solution (0.33 mol eq of CO loss after 4 h in PBS; [CORM-401] = 1 mM at time zero), while increased CO release occurs in the presence of a CO receptor or a ligand to prevent the rebinding of CO (3.2 mol eq of CO transferred to iron with a t1/2 of 0.8 min in the presence of 44 μM myoglobin; [CORM-401] = 10 μM at time zero). CO administration by CORM-401 is reported to uncouple mitochondrial respiration and inhibit glycolysis in human endothelial cells (10-100 μM), and relax isolated rat aortic rings (25 μM) pre-contracted with phenylephrine.
SML0315 CORM-A1 ≥95% (NMR) CORM-A1 is a water-soluble carbon monoxide (CO) releasing molecule that can be used to study the effects of CO on cellular systems. Carbon monoxide (CO), produced during the degradation of heme by the enzyme heme oxygenase is an important gaseous signaling mediator in mammalian cells CORM-A1 has anti-oxidant and anti-inflammatory activity.
It mediates the release of CO in a pH and temperature-dependent manner, thus favoring mild vasorelaxation and hypotension. During oxidative stress, CORM-A1 is reported to provide cytoprotection in astrocyte primary cultures. This boron-containing CORM promotes autophagy.
C2505 Corticosterone ≥92% Corticosterone is a glucocorticoid secreted by the adrenal cortex that activates both mineralocorticoid and glucocorticoid receptors.
Corticosterone is synthesized from 11-deoxycortisone by the action of enzyme 11β-hydroxylase majorly in adrenal glands. However, it may also be synthesized in non-adrenal tissues including leydig cells of testes and in murine thymus. Corticosterone is released post activation of hypothalamus-pituitary-adrenal (HPA) axis. It is a key player regulating metabolism, immune function and response to stress. It is produced by HPA activation in response to stress in myeloid cells. Elevated levels of corticosterone is observed in Huntington′s disease (HD).
human ... EBP(10682), SERPINA6(866)
rat ... Ar(24208), Nr3c1(24413)
C174   Corticosterone: HBC complex free flowing powder    
C2755 Cortisone ≥98% Cortisone (11 dehydro 17 hydroxycortico-sterone) is an anti-inflammatory glucocorticoid that delays wound healing after surgeries. It postpones the healing process by affecting the appearance of inflammatory cells, ground substance, fibroblasts, collagen, regenerating capillaries, and epithelial migration. Glucocorticoids have anti-inflammatory, anti-allergic and immunosuppressive properties and are extensively used in treatment and therapy.
Cortisone is a glucocorticoid; a corticosterone analog that has approximately twice the anti-inflammatory potency as corticosterone but much lower Na2+ retention potency.
human ... SERPINA6(866)
C3130 Cortisone 21-acetate ≥99%   human ... FNTA(2339), NR3C1(2908)
SML0417 Costunolide ≥97% (HPLC) Costunolide is a sesquiterpene lactone originally isolated from plants widely used in many herbal medicines. It has a variety of effects. Costunolide is a potent inducer of apoptosis, a potent anti-cancer agent, has anti-inflammatory, anti-viral, anti-fungal, antimycobacterial activity and has been shown to inhibit telomerase activity.
C5923 (−)-Cotinine ≥98% Major metabolite of nicotine in humans.
human ... CYP1A2(1544), CYP2A6(1548)
mouse ... Cyp2a5(13087)
PZ0136 CP-100263 dihydrochloride hydrate ≥97% (HPLC) CP-100263 is an NK-1 neurokinin receptor antagonist.
PZ0171 CP-100356 monohydrochloride >98% (HPLC) CP-100356 is a specific inhibitor of MDR1 (P-Gp), the protypical ABC transporter. The compound has low uM to nM potency for inhibiting several MDR-1 substrates (calcein-AM, digoxin) in transfected MDCKII cells. CP-100356 also inhibits prazosin transport in human breast cancer resistance protein (BCRP)-transfected MDCKII cells, suggesting that it acts as a dual inhibitor. CP-100356 does not inhibit multidrug resistance-associated protein 2 (MPR2 IC50 >15 mM).
PZ0107 CP-101537 ≥98% (HPLC) CP-101537 is a MMP inhibitor, candidate drug for myocardial infarction therapy, and antibacterial.
SML0053 CP-101,606 ≥98% (HPLC) CP-101,606 (Traxoprodil) plays a role in inhibiting glutamate-induced death in rats. It may exhibit therapeutic effects against human ischemia and neurodegenerative disorders. Traxoprodil is metabolized by cytochrome P450 (CYP) 2D6.
Traxoprodil (CP-101,606) is a potent noncompetitive antagonist of N-methyl-D-aspartate (NMDA) receptors, selective for the NR2B subunit. It has been shown to be neuroprotective in animal models of brain injury and stroke.
human ... GRIN1(2902), GRIN2B(2904)
PZ0255 CP-101606 mesylate ≥98% (HPLC) CP-101,606 is an NR2B (N-methyl D-aspartate receptor subtype 2B) subunit antagonist, that can increase dyskinesia. It reduces Ca2+/calmodulin-dependent protein kinase II level, at threonine-286 hyperphosphorylation (pCaMKII-Thr286). It has no effect on the α1-adrenergic receptors. CP-101,606 has the ability to inhibits the habits, stimulated by cocaine. It also possesses hallucinogenic properties.
CP-101606 mesylate (Traxoprodil mesylate) is a potent noncompetitive antagonist of N-methyl-D-aspartate (NMDA) receptors, selective for the NR2B subunit. CP-101606 mesylate has been shown to be neuroprotective in animal models of brain injury and stroke.
PZ0363 CP-105,696 ≥98% (HPLC) CP-105,696 is an orally active, potent and selective leukotriene B4 receptor (LTB4R) antagonist (IC50 against [3H]LTB4 = 5.6 nM for binding human neutrophils; IC50 = 9.7 nM & 30.3 nM, respectively using guinea pig spleen or mouse membranes) that targets LTB4R high- and low-affinity binding sites in a LTB4 non-competitive and competitive manner, respectively. CP-105,696 inhibits 5 nM LTB4-induced human neutrophils chemotaxis and CDllb upregualtion (IC50 = 5.2 nM and 430 nM, respectively) without inhibiting cyclooxygenase activity or affecting chemotaxis induced by C5a, PAF, IL-8. Oral administration is efficacious against intradermal LTB4 (100 ng/mouse), but not IL-1, injection-induced neutrophil accumulation in mice and guinea pigs (ED50 = 4.2 and 0.26 mgkg, respectively). CP-105,696 in vivo efficacy is also demonstrated in other animal models, including collagen-induced arthritis (CIA; 0.3-10 mg/kg in mice), allergic encephalomyelitis (ED50= 8.6 mg/kg; mice), and asthma (10-30 mg/kg; primate).
Orally active, potent and selective LTB4 receptor (LTB4R) antagonist with in vitro and in vivo anti-inflammatory efficacy.
PZ0121 CP-135807 ≥98% (HPLC) CP-135807 is a selective 5-HT1D agonist.
PZ0100 CP-154526 hydrochloride ≥98% (HPLC) CP-154526 is a selective, non-peptide antagonist of corticotropin releasing factor receptors (CRF1).
PZ0101 CP-226269 ≥98% (HPLC) CP-226269 is a D4 dopamine receptor agonist with EC50 of 32 nM.
C9115 CP-24879 hydrochloride ≥98% (HPLC), powder delta5/delta6 (Δ5/Δ6) desaturase inhibitor.
PZ0115 CP-31398 dihydrochloride hydrate ≥98% (HPLC) CP-31398 dihyrochloride hydrate is a p53 stabilizer; apoptosis inducer.
human ... TP53(7157)
mouse ... TP53(22059)
rat ... TP53(24842)
PZ0189 CP-316819 ≥98% (HPLC) CP-316819 belongs to the family of indole-2-carboxamide series of phosphorylase inhibitors. It has an ability to regulate interaction of glycogen targeting subunit (GL) 16mer peptide with phosphorylase a.
CP-316819 is a potent glycogen phosphorylase inhibitor. (IC50 = 40 nM against human liver GPα.) Under low glucose conditions, CP-316819 facilitates glycogen utilization in the brain, prevents neuronal cell death and maintains brain electrical currents.
PZ0108 CP-335963 ≥98% (HPLC) CP-335963 is an aurora 2 kinase inhibitor, PDGF inhibitor, and anti-proliferative.
C2499 CP-339818 ≥98% (HPLC) CP-338818 blocks both Kv1.3 and Kv1.4. Kv1.3 is expressed in brain and in effector memory T (Tem) cells, and Kv1.4 is expressed in brain cells. Kv1.3 and Kv1.4 are members of the Shaker family of voltage-gated potassium channels. Both channels are involved in setting the membrane potential of neurons. In addition, Kv1.3 maintains the membrane potential for T memory cells and is up-regulated upon T cell activation, contributing to multiple immune processes and disorders. Blockers of Kv1.3 have long been sought for therapeutic benefit, and they are also valuable tools for studying the immune system. CP-339818 is valuable for immune system studies, where the absence of Kv1.4 makes it functionally selective for Kv1.3, and it has shown suppression of T cell activation. CP-339818 is also valuable for the study of Kv1.4 function.
PZ0103 CP-346086 dihydrate ≥97% (HPLC) CP-346086 is microsomal triglyceride transfer protein (MTP, MTTP) inhibitor.
PZ0365 CP-376395 hydrochloride ≥98% (HPLC) CP-376395 is a potent and selective antagonist of the CRF1 receptor, which has been shown to play an important role in mediating behavioral and endocrine responses to fear and stress.
PZ0129 CP-380736 ≥98% (HPLC) CP-380736 is an inhibitor of the epidermal growth factor receptor (EGFR). EGFR is a tyrosine kinase that activates MAPK, JNK, and Akt pathways, and is an important mediator of several types of cancer, including lung cancer and glioblastoma multiforme.
PZ0347 CP-424,174 ≥98% (HPLC) CP-424,174 is a cytokine release inhibitory drugs (CRID) that inhibits the post-translational processing and secretion of IL-1b in response to LPS and ATP in human monocytes. It is quite possible that similarly to CP-456,773 (termed CRID3), CP-424,174 inhibits both NLRP3 and AIM2 inflammasomes by preventing ASC oligomerisation.
PZ0280 CP-456773 sodium salt ≥98% (HPLC) CP-456773 is known to inhibit the release of other proinflammatory cytokines such as IL-1α and IL-18. It is also referred to as MCC950.
CP-456773 sodium salt (CRID3) was found to act as a cytokine release inhibitory drug and inhibitor of the NLRP3 inflammasome. CP-456773 sodium salt inhibits interleukin 1β (IL-1β) secretion and caspase 1 processing.
SML1115 CP466722 ≥98% (HPLC) CP466722 is a competetive, reversible inhbitor of Ataxia telangiectasia (A-T) mutated (ATM) kinase. The compound CP466722 disrupts ATM-dependent checkpoint cell cylce events, and reverses ATM-dependent substrate phosphorylation and downstream signaling events following exposure to ionizing radiation.
PZ0137 CP-471474 ≥98% (HPLC) CP-471474 is a broad spectrum inhibitor of matrix metalloproteinases. CP-471474 has a low nM IC50 efficacy for MMP-2, MMP-3, MMP-9, and MMP-13. CP-471474 has low potency against MMP-1 (IC50 > 1 uM). CP-471474 prevents left ventricular remodeling after experimental myocardial infarction in mice. CP-471474 also inhibits cigarette smoke-induced lung inflammation and the progression of emphysema in guinea pig models.
PZ0225 CP 532623 ≥98% (HPLC) CP-532623 is a potent inhbitor of cholesteryl ester transfer protein (CETP) that leads to elevated high-density lipoprotein cholesterol levels. CP-532623 is structurally related to Torcetrapib (Cat. No. PZ0170).
PZ0125 CP-53631 ≥98% (HPLC) CP-53631 is a selective serotonin reuptake inhibitor (SSRI); antidepressant.
PZ0264 CP-547632 hydrochloride ≥98% (HPLC) CP-547632 hydrochloride is a well-tolerated, orally-bioavailable ATP-competitive kinase inhibitor. It is currently in clinical trials for the treatment of human malignancies.
CP-547632 is a potent inhibitor of the VEGFR-2 and basic fibroblast growth factor (FGF) kinases (IC50 = 11 and 9 nM, respectively). The compound CP-547632 inhibits VEGF and basic FGF-induced angiogenesis in animal models, and inhibits growth of xenograft tumors in mice.
C1112 CP-55940 >98% (HPLC), powder CP-55940 is a nonclassical cannabinoids (NCCs), which lack the tetrahydropyran ring. CP-55940, a derivative of CP-47,497 is enantioselective. Due to its amphipathic nature, CP-55940 tethers in biological membrane making it favourable for the cannabinoid receptor interaction. CP-55940 belongs to the cyclohexylphenol category and modulates the brain lipidome leading to dysregulation especially during adolescence. It inhibits capsaicin-evoked sensitization of nociceptive and spinal dorsal horn neurons.
CP-55940 is a selective cannabinoid receptor agonist.
human ... CNR1(1268), CNR2(1269)
rat ... Cnr1(25248)
PZ0362 CP-640186 hydrochloride ≥95% (HPLC) CP-640186 is a potent and orally active acetyl-CoA carboxylase 1/2 (ACC-alpha/beta, ACC1/2) inhibitor (IC50 ~50 nM) that targets the carboxyltransferase (CT) domain at the ACC dimer interface (via tight interactions with the putative biotin-binding site) in a reversible manner, uncompetitive with respect to ATP, and non-competitive with respect to bicarbonate, acetyl-CoA, and citrate. CP-610431 inhibits fatty acid (FA) synthesis, triglyceride (TG) synthesis, TG and apoB secretion (IC50 = 1.6, 1.8, 3.0, and 5.7 μM, respectively), but not cholesterol synthesis or apoC3 secretion in HepG2 cells (ACC1), as well as stimulates FA oxidation in C2C12 cells (ACC2) and in rat epitrochlearis muscle strips (EC50 = 57 nM and 1.3 μM, respectively). Oral administration is shown to inhibit FA synthesis in rats, CD1 mice, and ob/ob mice (ED50 = 13, 11, and 4 mg/kg, respectively) and stimulate rat whole body FA oxidation (ED50 ∼30 mg/kg) in vivo.
PZ0130 CP-64434 hydrate ≥98% (HPLC) CP-064434 is an antibiotic; anti-proliferative HDAC inhibitor.
PZ0124 CP-66713 ≥98% (HPLC) CP-66713 is an adenosine A2 receptor antagonist.
PZ0335 CP724714 ≥98% (HPLC) CP724714 is a potent and selective inhibitor of HER2/ErbB2 with an IC50 value of 10 nM. CP724714 is >640-fold selectivity against EGFR, and >1000-fold selective against InsR, IRG-1R, PDGFR, VEGFR2, Abl, Src, c-Met, JNK-2, JNK-3, ZAP-70, CDK-2 and CDK-5 in in vitro kinase assays. CP724714 had antiproliferative effects in a panel of human breast cancer cell lines.
human ... ERBB2(2064)
PZ0127   CP-74416 methanesulfonate hydrate ≥98% (HPLC) CP-74416 is a primary Danofloxacin metabolite. The compound belongs to a group of quinolone antibiotic. CP-74416 is an inhibitor of the bacterial DNA gyrase.
PZ0173 CP-775146 ≥98% (HPLC) CP-775146 is a potent and selective PPARα agonist.
PZ0148 CP-802079 hydrochloride hydrate ≥98% (HPLC) CP-802079 is a potent and selective glycine transporter type 1 (GlyT1) antagonist. Antagonists of GlyT1 increase levels of glycine in the synaptic cleft and, like direct glycine site agonists, they can augment NMDAR currents and NMDAR-mediated functions. CP-802,079 significantly increases the amplitude of the NMDAR currents and LTP.
PZ0378   CP-809,101 fumarate ≥98% (HPLC) CP-809,101 is a potent and high-affinity 5-hydroxytryptamine receptor 2C (5-HT2C) full agonist with only weaker partial agonist activity toward 5-HT2A & 5-HT2B (cellular Ca2+ mobilization EC50 in nM/efficiency = 0.11/93% and 0.06/97% with human and rat 5-HT2C, respectively; 153/67%/human 5HT2A, 65.3/57%/human 5HT2B, 119/79%/rat 5HT2A) and much reduced or little affinity toward other receptors, ion channels and uptake sites tested. CP-809,101 exhibits antipsychotic efficacy in reducing conditioned avoidance response/CAR (ED50 = 4.8 mg/kg s.c.) and locomotor activity (ED50 in mg/kg via s.c. = 2/rats, 1/mice; no effect up to 10 mg/kg in 5-HT2C-knockout mice), while oral administration is reported to suppress spontaneous and nocturnal food intake as well as fasting-induced refeeding in rats (∼8% and ∼24% reduction of cumulative food intake and body weight in 4 days, respectively; 30 mg/kg/day p.o.).
PZ0236 CP-863187 ≥98% (HPLC) CP-863187 is a potent p38α (p38α) inhibitor (IC50 = 5.8 nM) with 44-fold selectivity over p38β (p38β) and no inhibitory potency against p38γ (p38γ) and p38δ (p38δ) isoforms. CP-863187 effectively inhibits LPS-stimulated cellular TNF-α production in vitro (IC50 = 259 and 25 nM, using human whole blood and isolated mononuclear cells, respectively) and in rats in vivo (ED50 = 0.3 mg/kg p.o.) with good pharmacokinetic profile and oral availability (F = 87%/dog, 40%/monkey, 30%/rat with 5 mg/kg oral dosage; F = 66%/rat with 50 mg/kg oral dosage).
PZ0149 CP-868388 ≥98% (HPLC) CP-868388 is a potent PPARα agonist with a Ki of 10.8 nM.
PZ0104 CP-91149 ≥98% (HPLC) CP-91149 is a selective glycogen phosphorylase inhibitor.
PZ0102 CP-93129 dihydrochloride hydrate ≥98% (HPLC) CP-93129 is a potent and selective 5-HT1B agonist.
SML0588 CP-94,253 dihydrochloride ≥98% (HPLC) CP-94,253 is a potent and selective serotonin 5-HT1B receptor agonist with approximately 25x and 40x selectivity over the closely related 5-HT1D and 5-HT1A receptors. Ki values are 89, 2, 860, 49 and 1,600 nM for 5-HT1A, 5-HT1B, 5-HT1C, 5-HT1D and 5-HT2 receptors respectively. CP-94,253 was found to be anxiolytic in animal models; dose-dependently enhanced reinforcing effects of cocaine (self-administration);and reduced food intake.
PZ0019   CP-945,598 ≥98% (HPLC) CP-945,598 is a potent, selective, high affinity and competitive cannabinoid type 1 (CB1) receptor antagonist. CP-945,598 inhibits both basal and cannabinoid agonist-mediated CB1 receptor signaling in vitro and in vivo. CP-945,598 exhibits anorectic activity in two models of acute food intake in rodents, fast-induced re-feeding and spontaneous, nocturnal feeding.
CP-945,598 is also known as 1-(8-(2-Chlorophenyl)-9-(4-chlorophenyl)-9H-purin-6-yl)-4-(ethylamino)piperidine-4-carboxamide. This orally active antagonist of the cannabinoid CB-1 receptor may be used in the treatment of obesity.
C9373 CP-96345 ≥98% (HPLC) CP-96345 is a selective NK1 antagonist. CP96345 inhibits substance P-induced salivation in the rat by classical in vivo bioassay, but did not inhibit NK2, NK3, or numerous other receptors.
SML0752   (+)-CP-99994 dihydrochloride ≥98% (HPLC) (+)-CP-99994 dihydrochloride is an effective and selective non-peptide substance P receptor antagonist. It is synthesized from allylic and homoallylic C-H diamination of 4-phenyl-1-butene. (+)-CP-99994 exhibits anti-emetic activity in ferrets.
(+)-CP-99994 is a selective neurokinin (NK)-1 tachykinin antagonist. (+)-CP-99994 binds selectively and with high affinity with a Ki of 0.25 nM in a human cell line.
SML0125 CPA 1 hydrate ≥98% (HPLC) CPA 1 is a potent, selective, ATP-competitive dual inhibitor of protein kinase casein kinase 2 (CK2) and proviral insertion Moloney virus kinases (Pim kinases). CPA 1 is selective for CK2 and Pim kinases (Pim-1, Pim-2, and Pim-3) when evaluated against a panel of 112 protein kinases.
SML1124 CPCCOEt ≥98% (HPLC) CPCCOEt is a selective non-competitive metabotropic glutamate receptor mGluR1 antagonist with no agonist or antagonist activity at mGlu2, 4a, 5a, 7b, 8a or ionotropic receptors at concentrations of up to 100 μM.
SML0351 CPDT ≥96% (HPLC) 5,6-dihydrocyclopenta-1,2-dithiole-3-thione (CPDT) is a phase II enzyme inducer. It exhibits protective actions against chemical carcinogens.
CPTD (SNU2A) is a cytoprotective agent that protects mitochondria during cell stress by increasing antioxidant capacity. CPTD inhibits phosphorylation and activation of Fyn, which maintains AMPK activity and activation of Nrf2.
SML2571 CPHPC ≥98% (HPLC) CPHPC (Miridesap; Ro 63-8695) is an orally active serum amyloid P (SAP) blocker that targets the ligand-binding site on the SAP planar binding (B) face with each of its two D-proline moieties (up to two SAP per CPHPC), being able to crosslink and dimerize two SAP pentamers to form B face-to-B face decamers. CPHPC potently inhibits SAP binding to amyloid fibrils in vitro (IC50 = 0.9 μM using AD Aβ amyloid fibrils) and exhibits in vivo efficacy toward liver & circulating SAP clearance as well as SAP removal from tissue amyloid deposits (1-5 mg/mL in drinking water; human SAP transgenic mice).
SML1212 CPI203 ≥98% (HPLC) CPI203 is an analog of the BET inhibitor (BETi) (+)-JQ1 and is bioavailable via oral or intraperitoneal administration. It plays an important role in lenalidomide and dexamethasone functions in in vitro and in vivo models of multiple myeloma. CPI203 inhibits proliferation, apoptosis and cell cycle arrest in A431 cell line and primary skin squamous cell carcinoma (SCC) cells.
CPI203 is an inhibitor of BRD4, a bromodomain-containing protein that binds to histones to regulate recruitment of transcription factors. BRD4 is also an RNA Pol II kinase. CPI203 blocks BRD4 kinase activity in cells and in vivo. It has shown synergistic antitumor activity with lenalidomide in bortezomib-resistant mantle cell lymphoma.
SML2213 CPI-637 ≥98% (HPLC) CPI-637 is a cell penetrant, selective and potent CBP/p300 bromodomain inhibitor.
C3118 CPNQ ≥98% (HPLC), solid Misfolded proteins accumulate in many neurodegenerative diseases, including huntingtin in Huntington′s disease and alpha-synuclein in Parkinson′s disease. The disease-causing proteins can take various conformations and are prone to aggregate and form larger cytoplasmic or nuclear inclusions. CPNQ (B2) was identified as a compound that promotes inclusion formation in cellular models of both Huntington′s disease and Parkinson′s disease. Despite the aggregate-forming specifics the compound prevents huntingtin-mediated proteasome dysfunction and reduces alpha-synuclein-mediated toxicity. These results demonstrate that compounds that increase inclusion formation may actually lessen cellular pathology in both Huntington′s and Parkinson′s diseases, suggesting a therapeutic approach for neurodegenerative diseases caused by protein misfolding. The ability of B2 to prevent toxicity, despite increasing inclusions, suggests that inclusions are beneficial rather than toxic, which will be further explored as the molecular target and mechanism. CPNQ (B2) is a desirable tool for both Huntington′s and Parkinson′s research.
SML0804 (S)-CPP sodium salt ≥96% (HPLC) (S)-CPP is an inhibitor of branched-chain α-ketoacid dehydrogenase complex (BCKDC) kinase, also know as BDK, or keto acid dehydrogenase kinase. BDK is a negative regulator of BCKDC activity. Inhibition of BDK by (S)-CPP (IC50 = 6.3 μM) leads to complex activation, and significant reduction of plasma levels of leucine/isoleucine and valine in wild type mice.
SML0258 CPPG ≥98% (HPLC) CPPG is a potent group II/III metabotropic glutamate receptor antagonist, with approximately 20-fold selectivity for mGlu group III over group II (IC50 values of 2.2 and 46.2 nM respectively).
C2247 CPPHA ≥98% (HPLC) CPPHA is a selective positive allosteric modulator of mGluR5 receptor. It has no agonist activity alone, but reduces threshold response and shifts dose-response curves to glutamate, quisqualate, and DHPG by 4- to 7-fold to the left in recombinant CHO cells expressing human or rat mGluR5.
C156 D-CPT tartrate >94%, solid Binds to the cocaine receptor site on the dopamine transporter and blocks dopamine uptake.
C9873 CPTH2 ≥98% (HPLC), powder CPTH2 is a histone acetyltransferase (HAT) inhibitor modulating the Gcn5 network. Histone Acetyltransferase (HAT) inhibitor modulating Gcn5 network. Histone acetyltransferases (HATs) act as transcriptional coactivators. Histone acetylation plays an important role in regulating the chromatin structure and is tightly regulated by two classes of enzyme, histone acetyltransferases (HAT) and histone deacetylases (HDAC). Deregulated HAT and HDAC activity plays a role in the development of a range of cancers. Consequently, inhibitors of these enzymes have potential as anticancer agents.
C3249 CR8 ≥95% (HPLC) CR8 is a potent and selective inhibitor of cyclin dependent kinase (CDK1, 2, 5, 7, and 9). CR8 is a more potent pyridyl analogue of roscovitine (Cat. No. R7772). In comparison to roscovirtine, the compound gains in potency toward CK1, which is involved in amyloid-β formation. The R-CR8 enantiomer is slightly more potent than S. CR8 is around 30 times more potent at cellular assay then roscovitine. Acts as a molecular glue to induce cyclin K degradation.
SML0842   CRANAD 2 ≥98% (HPLC) CRANAD 2 is a near-infrared (NIR) Aβ plaque-specific fluorescent probe. CRANAD 2 penetrates the blood brain barrier and has a high affinity for Aβ aggregates with a Kd of 38 nM. Upon interacting with Aβ aggregates, CRANAD 2 exhibits a 70-fold increase in fluorescence intensity accompanied by a 90 nm blue shift from 805 to 715 nm and a large increase in quantum yield. CRANAD 2 has been used to detect Aβ deposits noninvasively in vivo in transgenic Tg2576 mice.
PZ0037 Crisaborole ≥98% (HPLC) Crisaborole is a non-steroidal anti-inflammatory phosphodiesterase 4 (PDE4) inhibitor. Crisaborole has an IC50 value of 490 nM for PDE4 with similar IC50 values for release of cytokines TNF-α, IL-2, and IFN-γ, and shows little inhibition against other PDE isozymes. Crisaborole has been approved as a topical treatment for atopic dermatitis.
PZ0191 Crizotinib ≥98% (HPLC) Crizotinib (PF-02341066) is an ATP-competitive inhibitor of the receptor tyrosine kinases (RTKs) c-Met (hepatocyte growth factor receptor) and anaplastic lymphoma kinase (ALK). Crizotinib is a highly specific inhibitor of c-Met and ALK among > 120 different RTKs surveyed. Crizotinib was approved for treatment of a subtype of nonsmall-cell lung cancer (NSCLC) with ALK fusion mutations.
human ... ALK(238), MET(4233)
PZ0240 (S)-Crizotinib ≥98% (HPLC) (S)-Crizotinib has a distinctly different profile from its (R)-enantiomer, the clinically approved anticancer agent Xalkori. Instead of targeting ALK, MET and ROS1, (S)-Crizotinib is a highly selective inhibitor of human 7,8-Dihydro-8-oxoguaninetriphosphatase MTH1 (NUDT1) with an IC50 value of 330 nM, 16-fold higher affinity towards MTH1 compared to the clinically used (R)-isomer. MTH1 hydrolyzes oxidized purine nucleoside triphosphates that might otherwise be incorporated into DNA/RNA and contribute to DNA damage. MTH1 removal of oxidized nucleotides that result from increased levels of reactive oxygen species (ROS) in fast-proliferating cancer cells helps protect cancer cells from proliferative stress and prevent cancer cell death. It is considered a new target for cancer therapy. In mouse xenograft studies using SW480 cells, (S)-crizotinib but not the (R)-enantiomer, was able to impair overall tumour progression as well as specifically reduce tumour volume by more than 50%.
C1055 Cromakalim Cromakalim is an activator of the potassium channel. It is involved in the relaxation of the vascular smooth muscles. Cromakalim exhibits anti-hypertensive activity.
rat ... Kcna1(24520), Kcnj1(24521), Kcnj5(29713), Kcnj8(25472)
C0399 Cromolyn sodium salt ≥95% Cromolyn blocks the release of histamine and other pro-inflammatory mediators from mast cells.
C2401 Crotaline Crotaline induces pulmonary vascular syndrome in rats. It is considered toxic and results in hepatic cirrhosis, enlarged liver, sinusoidal obstruction syndrome and right ventricular hypertrophy.
C0496 CRT0044876 ≥98% (HPLC) CRT0044876 targets the apurinic endonuclease (APE1) active site and inhibits its 3′-phosphodiesterase and 3′-phosphatase activities—essential steps in excision repair—with minimal effects on endonuclease IV, BamH1 restriction endonuclease, or topoisomerase I even at concentrations as high as 100 μM. At non-cytotoxic concentrations, CRT0044876 potentiates the cytotoxicity of several DNA base-targeting compounds, with accumulation of apurinic sites.
SML1507   CRT0066101 hydrochloride ≥98% (HPLC) CRT0066101 is a very potent inhibitor of Protein Kinase D (PKD) isoforms with IC50 values for PKD-1, -2 and -3 = 1, 2.5 and 2 nM, respecitively. CRT0066101 has been shown to have anticancer activity. CRT0066101 potently inhibits proliferation of PANC-1 pancreatic cells, and blocks migration and invasion of U87MG glioblastoma cells. CRT0066101 has also been shown to decrease growth of primary tumors and metastasis of ER(-) breast cancers.
C7124 Cryptolepine hydrate ≥98% (HPLC) Cryptolepine hydrate is a cytoxic, anti-cancer, antimalarial agent
C5624 Cryptotanshinone ≥98% (HPLC) Cryptotanshinone is a quinoid diterpene isolated from the root of the Asian medicinal plant, Salvia miotiorrhiza bunge. Recently it was discovered that the compound is a potent STAT3 inhibitor. Cryptotanshinone rapidly inhibited STAT3 Tyr705 phosphorylation through a JAK2-independent mechanism. Cryptotanshinone selectively inhibits STAT3-activated cell lines through binding to monomer STAT3, subsequently blocking the dimerization and inhibiting STAT3 transcriptional regulatory activity. Previously, it was reported that the compound counteracts inflammation through the inhibition of cyclooxygenase II activity and endothelin-1 expression. In traditional oriental medicine dried roots of Salvia Miltiorrhiza Bunge (Danshen) have commonly been used for the treatment of circulatory disorders, liver disease, coronary heart disease, hepatitis, and chronic renal failure.
SML1511 CS1 ≥98% (HPLC) CS1 is a selective and potent inhibitor of topoisomerase IIα (TopoIIα) that potently inhibits a proliferation of cancer cell lines including MDA-MB-231 and A548 cells, with less toxicity than etoposide. CS1 is a nonintercalating topoisomerase IIα (Topo IIα) inhibitor, which stabilizes the DNA-Topo IIα cleavage complex.
SML2608 CSRM617 Hydrochloride ≥98% (HPLC) CSRM617 is an ONECUT2 (OC2) inhibitor that directly targets OC2 HOX domain (KD = 7.43 μM) and disrupts OC2 target genes promoter binding. CSRM617 blocks OC2-dependent prostate cancer growth in cultures (IC50 = 4-50 μM; 48 h) via apoptosis induction (fold of untreated annexin V population = 2.3/10 μM, 3.5/20 μM; 22Rv1) and exhibits in vivo efficacy against metastases as well as the growth of established 22Rv1 tumor in mice in vivo (50 mg/kg/day ip.).
C6499   CTB ≥98% (HPLC) CTPB was a first known small molecular activator of histone acetyltransferase p300. CTB is a simplified analog of CTPB with comparable or higher activity. The compound activates the histone acetyltransferase (HAT) activity of p300/EP300/E1A binding protein.
Small molecule activators of HAT such as CTB (N-(4-Chloro-3-trifluoromethyl-phenyl)-2-ethoxy-benzamide) is useful for altering chromatin acetylation directly. It might serve as a therapeutic agent for treating the complications of cognitive dysfunction including neuropsychiatric, neurodevelopmental and neurodegenerative diseases.
SML2306 CTEP ≥98% (HPLC) CTEP is a high-affinity, orally active, potent and selective metabotropic glutamate receptor 5 (mGlu5 or mGluR5) negative allosteric modulator (NAM) and inverse agonist (human/mouse/rat mGlu5 Kd = 1.7/1.8/1.5 nM; IC50 against quisqualate stimulation = 6.4/16.8/8/8 by IP accumulation or 11.4/42/4/6.9 by Ca2+ mobilization using human/mouse/rat mGlu5 HEK293 transfectants; IC50 = 40.1 nM against constitutive IP level in human mGlu5 HEK293) with >1000-fold selectivity over 103 molecular targets, including all known mGluRs. CTEP is an excellent tool compound for long-term in vivo studies (in mice and rats) with good pharmacokinetic properties (B/P ratio = 2.6, oral bioavailability ~100%, T1/2 ~18 hrs post 4.5 mg/kg p.o. in mice) and reported to display 30- to 100-fold higher in vivo potency than MPEP and fenobam in two rodent behavioral models sensitive to antianxiety drugs.
SML0068 CTP Inhibitor ≥98% (HPLC) CTP Inhibitor is an inhibitor of mitochondrial citrate transport protein, was the first purely competitive inhibitor to be discovered and is more potent than BTC.
CTP inhibitor blocks the exchange of tricarboxylates the key intermediates in anabolism and catabolism by mitochondrial citrate transport protein (CTP).
SML1754   CTX1 ≥95% (HPLC) CTX1 is a potent HdmX inhibitor that overcomes HdmX-mediated p53 repression. CTX1 inhibits proliferation and induces apoptosis in number of cancer cell lines. CTX1 inhibits growth of primary human AML in immunodeficient mice.
SML0769   Cu-ATSM ≥98% (HPLC) Cu-ATSM is an orally bioavailable, blood-brain barrier permeable complex that specifically inhibits the action of peroxynitrite on Cu,Zn superoxide dismutase (SOD1) and subsequent nitration of cellular proteins. CuII(ATSM) significantly delayed onset of disease (paralysis and prolonged lifespan) in amyotrophic lateral sclerosis (ALS) mice model. Also, Cu-ATSM was reported to lower lipid peroxidation in a model of ischemicreperfusion injury. Cu-ATSM subsequently was shown to inhibit ferroptosis with a potency similar to Liproxstatin-1.
SML2221 CU-CPT9a ≥98% (HPLC) CU-CPT9a is a potent and selective inhibitor of Toll-like receptor 8 (TLR8). It binds to TLR8 at a site different from current small-molecule TLR7/8 agonists, stabilizing the TLR8 dimer in its resting state, thus preventing TLR8 activation It exhibited an IC50 value of 0.5 nM and blocked TLR8 activation induced by either resiquimod (R848) or ssRNA without affecting the closely related TLR7 or cells expressing other TLRs. CU-CPT9a also suppressed TNF-α levels in a dose-dependent manner in cells from patients with rheumatoid arthritis.
C8499 Cucurbitacin B hydrate ≥97% (HPLC) Cucurbitacin B also exhibits anti-cancer activity by inhibiting telomerase and c-Myc in breast cancer. It also exhibits anti- artherosclerotic activity. Cucurbitacin B also possesses anti-inflammatory and anti-microbial activity.
Cucurbitacin B is a triterpenoid constituent of Cucurbitaceae plant species. Cucurbitacin B inhibits proliferation in a wide variety of tumor cell lines (IC50 15-30 nM) by inducing apoptosis and inducing cell cycle arrest at G2/M phase. Although the mechanism of action is unclear, Cucurbitacin B inhibits STAT 3 phosphorylation and expression levels and has been shown to block JAK2 activity. Curcubitacin B also inhibits the transcriptional activity of HIF1a and Nf-KB. Curcubitacin B is structurally similar to the JAK inhibitor Curcubitacin I.
SML0577 Cucurbitacin E ≥95% (HPLC) Cucurbitacin E is a potent inhibitor of actin depolymerization. Cucurbitacin E is more active than jasplakinolide, and has a different mechanism of action, binding to a different site. Cucurbitacin E binds specifically to filamentous actin (F-actin) forming a covalent bond at residue Cys257, but not to monomeric actin (G-actin), stabilizing F-actin, without affecting actin polymerization or nucleation.
C4493 Cucurbitacin I hydrate ≥95% (HPLC), solid Cucurbitacin I (JSI-124) is a novel selective inhibitor of the janus kinase 2/signal transducer and activator of transcription 3 (JAK2/STAT3) signaling pathway with anti-proliferative and anti-tumor properties.
SML2675 CuET ≥97% (HPLC) CuET, a metabolite of disulfiram, is an inhibitor of p97 segregase adaptor NPL4 that exhibits potent anti-cancer effects. Apparently CuET binds NPL4 and induces its aggregation, which disables the vital p97–NPL4–UFD1 pathway and induces to cell death.
C1386 Curcumin from Curcuma longa (Turmeric), powder A natural phenolic compound. Potent anti-tumor agent having anti-inflammatory and anti-oxidant properties. Curcumin has been cited as a potential chemopreventive agent, in addition to its chemotherapeutic activity. Induces apoptosis in cancer cells and inhibits phorbol ester-induced protein kinase C (PKC) activity. Reported to inhibit production of inflammatory cytokines by peripheral blood monocytes and alveolar macrophages. Potent inhibitor of EGFR tyrosine kinase and IκB kinase. Inhibits inducible nitric oxide synthase (iNOS), cycloxygenase and lipoxygenase. Easily penetrates into the cytoplasm of cells, accumulating in membranous structures such as plasma membrane, endoplasmic reticulum and nuclear envelope.
Curcumin (diferuloylmethane) is a constituent of the yellow powder extracted from the roots of Curcuma longa Linn, also known as tumeric or turmeric. It is used as a spice and coloring agent for centuries. In addition, it is used to treat various diseases including, hepatic disorders, anorexia, diabetic wounds and rheumatism.
human ... APP(351), CYP1A2(1544)
C7821   Curdlan from Alcaligenes faecalis Curdlan is a (1,3)-β-glucan. It is a pathogen-associated molecular-pattern (PAMP) recognized by the receptor dectin-1. Activation of dectin-1, together with TLR2/TLR6, promotes signaling resulting in the production of pro-inflammatory cytokines, thus inducing inflammation.
SML0772 Curvularin from Penicillium citrinum, ≥98% (HPLC) S - Curvularin is a macrocyclic lactone with cytotoxic activity. Curvularin inhibits cell division as well as expression of human inducible nitric oxide synthase (iNOS), an enzyme critically involved in pro-inflammatory immune processes. Curvularin anti-inflammatory activity was demonstrated in chronic inflammatory disease models in mice such as Chronic Induced Arthritis (CIA) as well as in human alveolar epithelial A549/8 cells.
SML1215 Cuspin-1 ≥98% (HPLC) Cuspin-1 (Chemical Upregulator of SMN Protein-1) is an upregulator of the Survival of Motor Neuron protein (SMN), necessary for survival of motor neurons. SMN is decreased in the neurodegenerative disease Spinal Muscular Atrophy (SMA), an autosomal recessive disease caused by a genetic defect in the SMN1 gene. SMA is the second leading cause of neuromuscular disease, after Duchenne muscular dystrophy. Cuspin-1 increased SMN levels by 50-100% in SMA patient fibroblast cells accompanied by an increase in the phosphorylation of Erk, suggesting inbvolvement of the Ras-Raf-MEK cascade.
SML1366 CVT-10216 ≥98% (HPLC) CVT-10216 is a selective reversible inhibitor of aldehyde dehydrogenase-2 (ALDH-2), thereby inhibiting dopamine synthesis. CVT-10216 is active in suppressing alcohol and cocaine use, and anxiety.
CVT-10216 possesses unequivocal anxiolytic properties. It will not affect the suppression of locomotor activity by mCPP (m-chlorophenylpiperazine).
SML2602 CW3388 ≥98% (HPLC) CW3388 is a cell active and highly potent enhancer of oligodendrocyte formation. CW3388 potently inhibits the cholesterol biosynthesis enzyme Δ8,7-sterol isomerase (EBP). It promotes myelination in vitro.
SML1056   CX4338 ≥98% (HPLC) CX4338 is a CXCR2 receptor antagonist. In cell based assays, CX4338 blocks CXCL8-induced receptor internalization and β-arrestin recruitment, but enhances G-protein-mediated signaling events such as calcium mobilization and ERK phosporylation. The comopund inhibits CXCL8-induced neutrophil chemotaxis, and LPS-induced PMN migration in a mouse airway inflammaiton model.
SML1191 CX516 ≥98% (HPLC) CX516 is a positive allosteric modulator at AMPA receptor that inhibits the deactivation of AMPA receptors. CX-516 is a nootropic and ampakine agent.
C271 CX546 ≥98% (HPLC), solid CX546 has antipsychotic functionality and has the potential to treat schizophrenia. It improves the defects associated with the prepulse inhibition (PPI) and latent inhibition (LI) in mice lacking metabotropic glutamate receptor type 5 (mGluR5). Additionally, CX546 potentiates synaptic plasticity, elicits neuroprotection and promotes the neurotrophin expression.
Positive AMPA glutamate receptor modulator.
human ... GRIA1(2890), GRIA2(2891), GRIA3(2892), GRIA4(2893)
SML2646 CX614 ≥98% (HPLC) CX614 (BDP-37) is a brain-penetrant class I ampakine (benzoxazine subgroup of benzamide-type) with AMPA receptor (AMPAR; iGluR) positive allosteric modulator (PAM) activity via targeting a binding site shared by cyclothiazide (CTZ), but distinct from that of GYKI 52466. CX614 enhances field excitatory postsynaptic potentials (amplitude & duration) in rat hippocampal slices and autaptically evoked excitatory postsynaptic currents in neuronal cultures (EC50 of 20-40 μM) by blocking desensitization and slowing deactivation of responses to glutamate. CX614 is also widely employed for studying AMPAR-mediated physiological responses in vivo (1-10 mg/kg n rats and mice via i.p.).
SML2465 CY-09 ≥98% (HPLC) CY-09 is an NLRP3 inflammasone inhibitor. CY-09 binds directly to the ATP-binding motif of NLRP3 NACHT domain and inhibits its ATPase activity, blocking NLRP3 inflammasome assembly and activation. In mouse models CY-09 showed therapeutic effects in type 2 diabetes and cryopyrin-associated auto-inflammatory syndrome (CAPS), which is caused by gain-of-function mutations of NLRP3.
SML0321 Cyamemazine ≥98% (HPLC) Cyamemazine belongs to the class of phenothiazine drugs. It is known to treat severe depression, schizophrenia and bipolar disorder.
Cyamemazine is a potent antagonist of 5-HT2C and 5-HT3 receptors with antipsychotic and anxiolytic properties.
UC455 3-Cyano-7-ethoxycoumarin ≥97% (HPLC) Fluorescent probe useful in microsomal dealkylase studies. Typical drug-drug interactions resulting from enzyme inhibition.
C2020 α-Cyano-4-hydroxycinnamic acid ≥98% (TLC), powder α-Cyano-4-hydroxycinnamic acid acts as a specific inhibitor of monocarboxylic acid transport, including lactate and pyruvate transport. It is also reported to block β-cell apical anion exchange (IC50 of 2.4 mM).
UC454 3-Cyano-7-methoxycoumarin Fluorescent CYP1A1 &1A2 substrate
C238 S(−)-Cyanopindolol hemifumarate salt solid, ≥98% (HPLC) 5-HT1A/1B serotonin receptor antagonist; β3-adrenoceptor antagonist.
C247 Cyclazosin hydrochloride solid α1B-adrenoceptor antagonist.
SML1228 Cyclic-di-GMP sodium salt ≥98% (HPLC) Cyclic-di-GMP is a naturally occurring small molecule that acts as a bacterial second messenger to regulate important signaling mechanisms in prokaryotes that control bacterial survival, adhesion, colonization, biofilm formation, and virulence factors production. During infections Cyclic-di-GMP is bound by host STING (stimulator of interferon genes) leading to expression of interferon genes, activating innate immune responses. c-di-GMP has been found in eukarotic systems acting not only in immune response, but as an inhibitor of the pacemaker I(f) current in the heart.
P4236 Cyclic Pifithrin-α hydrobromide ≥98% (HPLC) A stable analog of Pifithrin-α (Product Code P4359) with similar biological activities and lower cellular toxicity.
SMB00372 Cycloastragenol ≥98% (HPLC) Cycloastragenol is used as a nutraceutical (e.g. TAT2) and seems to moderately increase the telomerase activity and proliferative capacity of both CD4 and CD8 T-cells. Cycloastragenol possesses antiviral, antimicrobial, anti-inflammatory, anti-hepatotoxic, anti-leukemia, antitumor and antinociceptive activity. It also acts as an immunomodulator.
SML1448 Cycloastragenol ≥98% (HPLC) Cycloastragenol is an aglycone of astragaloside IV isolated from Astragalus species that exhibits anti-inflammatory properties and promotes and wound gap closure. Cycloastragenol enhances the antiviral response in human CD8+ T-lymphocytes. Cycloastragenol induces telomerase activity and induces CREB (cAMP response element binding) activation in human neonatal keratinocytes, PC12 cells, and primary neurons.
C4542 Cyclobenzaprine hydrochloride Cyclobenzaprine hydrochloride is a type of tricyclic skeletal drug, which is commonly used as a muscle relaxant. It is very effective in treating intractable pain of cervical and lumbar origin caused by skeletal muscle spasm. cyclobenzaprine hydrochloride inhibit tonic α-mononeuronal excitation mediated by descending serotonergic systems by interacting with serotonin receptors at the spinal cord level.
Skeletal muscle relaxant; reduces muscle spasm by depression of brainstem neurons; 5-HT2 serotonin receptor antagonist.
human ... HTR2A(3356), HTR2B(3357), HTR2C(3358)
SML2386 Cycloguanil hydrochloride ≥95% (HPLC) Cycloguanil is it a potential antimalarial drug. It is hydrophilic in nature. Cycloguanil acts as a substrate for the enzyme organic cation transporter 1 (OCT1).
Cycloguanil, a metabolite of proguanil, is a potent dihydrofolate reductase inhibitor.
C7698 Cycloheximide from microbial, ≥94% (TLC) Cycloheximide (CHX) is an antibiotic produced by S. griseus. Its main biological activity is translation inhibition in eukaryotes resulting in cell growth arrest and cell death. CHX is widely used for selection of CHX-resistant strains of yeast and fungi, controlled inhibition of protein synthesis for detection of short-lived proteins and super-induction of protein expression, and apoptosis induction or facilitation of apoptosis induction by death receptors.
human ... FKBP1A(2280), PIN1(5300)
C4859 Cycloheximide solution Ready-Made Solution, microbial, 100 mg/mL in DMSO, 0.2 μm filtered Cycloheximide (CHX) is an antibiotic produced by S. griseus. Its main biological activity is translation inhibition in eukaryotes resulting in cell growth arrest and cell death. CHX is widely used for selection of CHX-resistant strains of yeast and fungi, controlled inhibition of protein synthesis for detection of short-lived proteins and super-induction of protein expression, and apoptosis induction or facilitation of apoptosis induction by death receptors.
human ... FKBP1A(2280), PIN1(5300)
C9901 N6-Cyclohexyladenosine Selective A1 adenosine receptor agonist.
human ... ADORA1(134)
rat ... Adora1(29290), Adora2a(25369), Adora3(25370)
C4116 Cyclopamine hydrate ≥98% (HPLC) Cyclopamine is a Hedgehog signaling pathway inhibitor; inhibits the growth of medulloblastoma cells.
human ... EBP(10682)
SML2972 Cyclopentenyl uracil ≥98% (HPLC) New Cyclopentenyl uracil is a non-cytotoxic inhibitor of uridine kinase that act as a potent inhibitor of pyrimidine salvage in the intact mouse. Combination of Cyclopentenyl uracil with GSK983 significantly reduces viral infection of dengue serotype 2 (DENV-2) strain 16681 in cultures of the A549 lung carcinoma cell line. Cyclopentenyl uracil in combination with GSK983 enhances therapeutic index of viral RdRp inhibitor R1479.
C4479 9-Cyclopentyladenine monomethanesulfonate ≥98% (HPLC) A stable, cell-permeable, non-competitive adenylyl cyclase inhibitor that targets the P-site domain. IC50 = 100 μM in detergent-dispersed rat brain preparation.
C8031 N6-Cyclopentyladenosine solid N6-Cyclopentyladenosine (CPA) is an adenosine derivative and a potent A1 adenosine receptor agonist. It acts as an anticonvulsant and might exhibit protective actions against aminophylline (AMPH)-induced seizures.
N6-Cyclopentyladenosine also exhibits analgesic effect against acute, arthritis-induced and neuropathic pain.
human ... ADORA1(134), ADORA2A(135), ADORA3(140)
mouse ... Adora1(11539)
rat ... Adora1(29290), Adora2a(25369), Adora3(25370)
C102 8-Cyclopentyl-1,3-dimethylxanthine ≥98% (HPLC), powder Selective A1 adenosine receptor antagonist.
human ... ADORA1(134)
C101 8-Cyclopentyl-1,3-dipropylxanthine solid 8-Cyclopentyl-1,3-dipropylxanthine (DPCPX) is a selective A1 adenosine receptor antagonist. DPCPX possesses anti-cancer functionality. It induces apoptosis in breast cancer cells and favors mRNA expression of caspases.
human ... ADORA1(134), ADORA2A(135), ADORA2B(136), ADORA3(140)
rat ... Adora1(29290), Adora2a(25369), Adora2b(29316), Adora3(25370)
C8863 7-Cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3‑d]pyrimidin-4-ylamine ≥98% (HPLC) A potent and selective pyrrolo[2,3-d]pyrimidine Lck inhibitor.
human ... KDR(3791), LCK(3932), TEK(7010)
C0768 Cyclophosphamide monohydrate bulk package Cyclophosphamide is a cytotoxic nitrogen mustard derivative widely used in cancer chemotherapy. It cross-links DNA, causes strand breakage, and induces mutations. Its clinical activity is associated with a decrease in aldehyde dehydrogenase 1 (ALDH1) activity.
human ... ALDH1A1(216), ALDH1B1(219)
C1530 Cyclopiazonic acid from Penicillium cyclopium ≥98% (HPLC), powder Inhibits the sarcoplasmic reticulum Ca2+-pump.