CI-CZ

Product #

Image

Product Name

Biochem/physiol Actions

Gene Symbol (ID)

Add to Cart

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.
 
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.
 
C1618 Cibenzoline succinate ≥97% (NMR), 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.
 
SML0545   CID 1067700 ≥98% (HPLC) 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.
 
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.
 
SML0516 CID 5380390 ≥98% (HPLC) CID 5380390 (trans-2,3-Dimethoxy-ß-nitrostyrene) 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 5380390 has an IC50 values of 23 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.
 
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)
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.
 
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) 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 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.
human ... CACNA1A(773), DRD2(1813), HRH1(3269)
C1272 Cinobufagin    
C1147 Cinobufotalin    
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)
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.
 
C5976 CL 316,243 hydrate ≥98% (HPLC), powder CL 316,243 is a β3 adrenoceptor agonist; anti-obesity agent.
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 for the treatment of type II diabetes. It 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 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.).
 
SML1063 CLEFMA ≥98% (HPLC) CLEFMA is a curcumin analog that elevates ROS levels and induces oxidative stress and apoptosis in lung cancer cell lines. CLEFMA inhibits tumor growth in lung cance xenografts.
 
SML0445 Clemastine fumarate salt ≥98% (HPLC) Clemastine fumarate is an antihistamine H1-antagonist and anticholinergic that also has antipruritic activity.
 
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% β2-adrenoceptor agonist, bronchodilator.
 
C8414 Clobazam Anxiolytic; ligand for the GABAA receptor benzodiazepine modulatory site.
 
C209 Clobenpropit dihydrobromide solid Selective H3 histamine receptor antagonist that crosses the blood-brain barrier.
 
C7495 Clofarabine ≥98% (HPLC) Clofarabine is a purine nucleoside antimetabolite. Clofarabine is toxic to nondividing lymphocytes and monocytes.
 
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 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)
C1277 Clonazepam powder Anticonvulsant; ligand for the GABAA receptor benzodiazepine modulatory site.
rat ... Tspo(24230)
C7897 Clonidine hydrochloride solid α2-adrenoceptor agonist; I1 imidazoline binding site ligand.
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.
 
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.
 
C3977   Clostridium difficile Toxin A lyophilized powder 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.
 
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. 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.
 
C4102   Clostridium difficile Toxin B lyophilized powder 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.
Toxin B is 100-1,000-fold more cytotoxic than toxin A in inducing rounding-up of cells and destruction of the actin cytoskeleton.
 
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.
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.
 
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.
 
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 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 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.
 
C6903   α-Cobratoxin from Naja naja kaouthia Long chain post-synaptic neurotoxin that binds nicotinic receptors and blocks cholinergic neurotransmission at the neuromuscular junction; binding is irreversible.
 
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.
 
C122   Codeine sulfate salt Narcotic analgesic and selective μ agonist whose activity is due to its conversion (demethylation) to morphine in vivo.
 
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.
 
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)
mouse ... Abcb1a(18671), Abcb1b(18669)
C7744 Combretastatin A4 ≥98% (HPLC), powder 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 Promotes release of histamine. Inhibits calmodulin and activates G proteins.
 
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) Cytotoxic. Inhibits acidification of organelles and perforin-mediated cytotoxicity.
 
C2108 Condelphine ≥95%, solid Nicotinic acetylcholine receptor antagonist.
 
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).
 
C2005 Coprostane    
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 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.
 
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.
 
C2505 Corticosterone ≥92% Corticosterone is a glucocorticoid secreted by the adrenal cortex that activates both mineralocorticoid and glucocorticoid receptors.
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)
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) 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.
 
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 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.
 
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 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.
 
PZ0226 CP 524515 ≥98% (HPLC) CP-524515 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).
 
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 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 selective cannabinoid receptor agonist.
human ... CNR1(1268), CNR2(1269)
rat ... Cnr1(25248)
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.
 
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.
 
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.
 
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 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) 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.
 
SML1212 CPI203 ≥98% (HPLC) 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.
 
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.
 
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) New 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.
 
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 a compound that causes vasodilation by activation of potassium channels.
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    
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.
 
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.
 
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) New 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-ASTM ≥98% (HPLC) Cu-ASTM 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-ASTM was reported to lower lipid peroxidation in a model of ischemicreperfusion injury.
 
SML0722 CU-CPT22 ≥98% (HPLC) CU-CPT22 is the first probe for the complex between toll-like receptors TLR1 and TLR2. CU-CPT22 binds at the interface of TLR1 and TLR2.
 
C8499 Cucurbitacin B hydrate ≥97% (HPLC) 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.
 
SML0386 CUR61414 ≥98% (HPLC) CUR61414 specifically binds to, and antagonizes the activity of smoothened (Smo) in the hedgehog signaling pathway. CUR61414 inhibits proliferation and induces apoptosis in tumor cells without affecting non-tumor cells.
 
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.
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.
 
C7238 CV-3988 hydrate ≥98% (HPLC) Competitive PAF receptor antagonist. Inhibits PAF-induced human platelet aggregation (3-30 μM) and bronchoconstriction in the guinea pig.
human ... PTAFR(5724)
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.
 
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 Positive AMPA glutamate receptor modulator.
human ... GRIA1(2890), GRIA2(2891), GRIA3(2892), GRIA4(2893)
SML0321 Cyamemazine ≥98% (HPLC) 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.
 
C2612 3-Cyano-7-ethoxycoumarin ≥90% (at 254 nm, 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 Specific inhibitor of monocarboxylic acid transport, including lactate and pyruvate transport. 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. Recently 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.
 
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 Skeletal muscle relaxant; reduces muscle spasm by depression of brainstem neurons; 5-HT2 serotonin receptor antagonist.
human ... HTR2A(3356), HTR2B(3357), HTR2C(3358)
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)
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 Selective A1 adenosine receptor agonist.
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 Selective A1 adenosine receptor antagonist.
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.
human ... ADORA1(134), ADORA2A(135), ADORA3(140)
mouse ... Adora1(11539)
rat ... Adora1(29290), Adora2a(25369), Adora3(25370)
C1368 Cyclopropanecarboxylic acid {3-[4-(3-trifluoromethyl-phenylamino)-pyrimidin-2-ylamino]-phenyl}-amide ≥98% (HPLC), solid ATP-competitive Aurora A kinase inhibitor with IC50 = 42 nM
 
C3662 Cyclosporin A from Tolypocladium inflatum, ≥95% (HPLC), solid A fungal metabolite possessing potent immunosuppressive properties. It inhibits the T-cell receptor signal transduction pathway via the formation of cyclosporin A−cyclophilin complex that inhibits calcineurin (protein phosphatase 2B). Inhibits nitric oxide synthesis induced by interleukin 1α, lipopolysaccharides and TNFα. Can block cytochrome c release from mitochondria.
human ... PPP3CA(5530), PPP3CB(5532), PPP3CC(5533), PPP3R1(5534), PPP3R2(5535)
SML0192   Cyclosporin C ≥95% (HPLC), from Acremonium luzulae Cyclosporins are a family of neutral, highly lipophilic, cyclic undecapeptides containing some unusual amino acids. Cyclosporin A (CsA) is the main representative of cyclosporins. It has antifungal activity and is the strongest immunosuppressive compound discovered so far. Cyclosporin C has the same activity with reduced potency. CsA has potent anti-Hepatitis C Virus (HCV) activity towards both HCV replicons. Cyclophilins are intracellular proteins, highly conserved, involved in cis-trans isomerization of peptidyl-prolyl bonds and protein folding which bind cyclosporins and as a complex inhibit the activity of calcineurin, a phosphatase necessary for T-cell activation. Cyclosporin is therefore used for treating autoimmune disorders such as rheumatoid arthritis, systemic lupus erythematosus (SLE), and psoriasis.
 
SML1575   Cyclosporin H ≥97% (HPLC) Cyclosporin H is a selective inhibitor of formyl peptide receptor-1 (FPR-1) and formyl peptide-induced superoxide formation in neutrophils. Cyclosporin H does not bind cyclophilin or evoke an immunosuppressant response. Cyclosporin H has been reported to inhibit tumor promoting phorbol ester TPA/PMA in mouse skin cells and to inhibit calcium/calmodulin-dependent EF-2 phosphorylation.
 
SML1018   Cyclosporin A, Ready Made Solution 1 mg/mL in DMSO (0.2 μm-filtered) Cyclosporin A is a non-polar cyclic oligopeptide produced by the fungus Tolypocladium inflatum. It is a potent immunosuppressive agent, affecting primarily T-lymphocytes. It has been shown to inhibit the functioning of several nuclear proteins involved in T-cell activation at the level of mRNA transcription. It forms a complex with its intracellular receptor cyclophilin, which can then bind to calcineurin, a Ca2+- and calmodulin-dependent protein phosphatase, inhibiting its enzymatic activity. CsA was found to suppress the replication of hepatitis C virus genome in cultured hepatocytes. At concentrations >10 nM, CsA protected isolated hepatocytes against the action of phalloidin. CsA can inhibit IL2 production resulting from T cell activation via Calcineurin inhibition.
An extensive list of references has been reported, including a comprehensive review of analytical properties.
 
C9847 Cyclothiazide Blocks the rapid desensitization of the AMPA glutamate receptors and markedly prolongs the decay time of the evoked excitatory post-synaptic current.
human ... CA1(759), CA4(762), GRIA1(2890), GRIA2(2891), GRIA3(2892), GRIA4(2893)
rat ... Gria1(50592)
SML1769   Cyclotraxin-B trifluoroacetate salt ≥95% (HPLC) Cyclotraxin-B is a potent and selective Trk B (BDNF/NT-3) receptor inhibitor. Cyclotraxin-B prevents receptor activation by BDNF without interfering with BDNF binding. Cyclotraxin-B has an IC50 value < 1 nM. In rodent studies Cyclotraxin-B, sometimes fused with tat-protein for increased brain permeability, has been shown to have anxiolytic properties, prevent cold hypersensitivity induced by BDNF, and to reduce cocaine self-administration.
 
SML0799   CYM 50179 ≥98% (HPLC) CYM50179 is a potent, selective agonist of the sphingosine-1-phosphate receptor 4 (S1P4). CYM50179 activates S1P4 with an IC50 of 46 nM, with no affect on other S1P receptors at concentrations up to 25 μM.
 
SML1066 CYM50358 ≥98% (HPLC) CYM50358 is a potent, selective antagonist of the sphingosine-1-phosphate receptor 4 (S1P4). CYM50358 inhibits S1P4 with an IC50 of 25 nM.
 
SML1067 CYM50769 ≥98% (HPLC) CYM50769 is a potent, specific antagonist of the Neuropeptide B and Neuropeptide W receptor, NPBWR1 (IC50 = 120 nM).
 
SML0980   CYM51010 ≥98% (HPLC) CYM51010 is a biased ligand of μ-opioid receptor – δ-opioid receptor heterodimers. CYM51010 exhibits anti-nociceptive activity similar to morphine, but with a decreased levels of tolerance development and withdrawal symptoms.
 
C1997 CYM-5442 ≥98% (HPLC) CYM-5442 is a highly-selective S1P1 (Spingosine 1-Phosphate Receptor 1) agonist that activates S1P1-dependent pathways in vitro and to levels of full efficacy in vivo through a hydrophobic pocket, separable from the orthosteric site of S1P binding that is headgroup dependent. This is a different site from those involved in the activities of other agonists such as FTY720 and SEW2871.
 
SML1014   CYM-5520 ≥98% (HPLC) CYM-5520 is a specific, noncompetitive allosteric agonist of sphingosine 1-phosphate receptor 2 (S1PR2; EC50 = 1.0 μM). The compound CYM-5520 does not show any agonsit activity towards S1PR1, S1PR3, S1PR4 or S1PR5.
 
SML0680   CYM-5541 ≥98% (HPLC) CYM-5541 is an allosteric agonist selective for the Sphingosine 1-phosphate (S1P) S1P3 receptor subtype. CYM-5541 occupies a different chemical space in the ligand binding pocket of S1P3 than S1P does, a lower hydrophobic region around transmembrane helix TM6. CYM-5541 shows great selectivity and stability with an EC50 of between 72 and 132 nM compared to S1P1 EC50 > 10 μM, S1P2 EC50 > 50 μM, S1P4 EC50 > 50 μM, and S1P5 EC50 > 25 μM and no significant activities for a panel of 55 GPCRs, ion channels, and transporters.
 
C2490 CYN 154806 trifluoroacetate salt ≥98% (HPLC) Potent and selective sst2 somatostatin receptor antagonist.
 
PZ0195 CYP3cide ≥98% (HPLC) CYP3cide is a mechanism-based inhibitor of cytochrome P4503A4 that can be used to distinguish the contributions of CYP3A4 versus CYP3A5 on drug metabolism. The IC50 values for inhibition of Midazolam 1’-Hydroxylase activity of recombinant CYP3A4 and CYP3A5 by CYP3cide are 0.3 and 17 mM, respectively.
 
C5493 CyPPA ≥98% (HPLC), solid CyPPA is a positive modulator of small conductance Ca2+-activated K+ channels; selective for SK3 and SK2. CyPPA is a first subtype selective SK channel positive modulator with an EC50 of 5.6 μM and 14 μM, efficacy 90% and 71% for hSK3 and hSK2, respectively. CyPPA is a tool for distinguishing SK2 and SK3 from SK1 and IK; no other agents distinguish these channels.
 
C6022 Cyproheptadine hydrochloride sesquihydrate ≥98% (TLC), solid 5-HT2/5-HT1C serotonin receptor antagonist; H1 histamine receptor antagonist; antipruritic.
human ... HRH1(3269), HTR2A(3356), HTR2B(3357), HTR2C(3358)
30120 L-Cysteine hydrochloride anhydrous, ≥99.0% (RT) NMDA glutamatergic receptor agonist that is also an agonist at AMPA glutamatergic receptors at high concentrations.
 
C0256 Cytidine 5′-diphosphocholine sodium salt dihydrate ~98%, from yeast, solid Neuroprotective in situations of hypoxia and ischemia; biosynthetic intermediate of membrane phospholipids; cerebral vasodilator; inhibits PLA2 activation.
 
C0985 Cytidine 3′,5′-cyclic mono­phos­phate sodium salt ≥98% (HPLC) Produced by the hydrolysis of cytidine 5′-triphos­phate by the enzyme cytidylyl cyclase.
 
C1506 Cytidine 5′-triphosphate disodium salt ≥95% P2X4 purinergic receptor agonist.
 
C2899 Cytisine ≥99%, powder Potent agonist at α3β4 and α7 nicotinic acetylcholine receptors and partial agonist at α4β2 nicotinic acetylcholine receptors.
rat ... Chrna2(170945), Chrna3(25101), Chrna4(25590)
C8273 Cytochalasin D from Zygosporium mansonii, ≥98% (TLC and HPLC), powder Cell permeable fungal toxin; potent inhibitor of actin polymerization. Disrupts actin microfilaments and activates the p53-dependent pathways causing arrest of the cell cycle at the G1-S transition. Inhibits smooth muscle contraction. Inhibits insulin-stimulated, but not basal, transport of glucose.
Potent inhibitor of actin polymerization; disrupts actin microfilaments; activates the p53-dependent pathways; inhibits smooth muscle contraction; inhibits insulin-stimulated glucose transport.
 
C6637 Cytochalasin A from Drechslera dematioidea Cytochalasin A reacts with sulfhydryls, and inhibits growth and glucose transport in Saccharomyces. Cytochalasin A is an oxidizing analog of cytochalsin B.
 
C2149 Cytochalasin E from Aspergillus clavatus Cytochalasin E is a cell-permeable fungal toxin that inhibits actin polymerization stimulated by F-actin. Cytochalasin E does not inhibit glucose transport.
 
C0889 Cytochalasin H from Phomopsis sp. Cytochalasin reported to have CNS activity
 
C1768 Cytosine β-D-arabinofuranoside crystalline, ≥90% (HPLC) Ara-C incorporates into DNA and inhibits DNA replication by forming cleavage complexes with topoisomerase I resulting in DNA fragmentation; does not inhibit RNA synthesis. Anti-leukemia agent.
human ... POLB(5423)
mouse ... Cda(72269)
C2997 Cytosporone B ≥98% (HPLC) Cytosporone B (Csn-B) is the first naturally occurring agonist for nuclear orphan receptor Nur77. It binds with high affinity (IC50=0.278 nM) to the ligand-binding domain of Nur77 and stimulates Nur77-dependent activities.

Nur77 is a nuclear receptor/transcription factor. A physiological ligand for Nur77 is as yet unknown, but there is increasing interest in Nur77 because of its known activities. Translocation of Nur77 from the nucleus to mitochondria initiates cell apoptosis, making it a potential target for cancer treatment. Nur77 is also involved in glucose homeostasis; it induces genes involved in gluconeogenesis. Csn-B physically binds to Nur77 and activates its transactivational activity and translocation to mitochondria to induce apoptosis. It inhibits cancer cell proliferation and tumor growth.
Cytosporone B is a fungal metabolite closely related to phomposin C. It is the first known agonist for the nuclear orphan receptor Nur77. It binds with high affinity (IC50 = 0.278 nM) to the ligand-binding domain of Nur77 and stimulates Nur77-dependent activities.

Nur77 is a nuclear receptor/transcription factor with no known physiological ligand, but there is increasing interest in Nur77 because of its known activities. Translocation of Nur77 from the nucleus to mitochondria initiates apoptosis, making it a potential target for cancer chemotherapy. Nur77 also induces genes involved in gluconeogenesis. Csn-B activates the Nur77 translocation to mitochondria to induce apoptosis, inhibiting cancer cell proliferation and tumor growth.
 
SML1214 CZC24832 ≥98% (HPLC) CZC24832 is a potent and selective inhibitor of phosphoinositide 3-kinase γ (PI3Kγ) with Kd app of 19 nM. CZC24832 is said to be the first selective PI3Kγ inhibitor with efficacy in in vitro and in vivo models of inflammation. CZC24832 strongly inhibited T-cell interleukin 17A (IL-17A) production by inhibiting expression of retinoic acid receptor–related orphan receptor γt (RORγt), a transcription factor that drives TH17 differentiation, showing a new role for PI3Kγ.
 
SML0373 CZC-25146 hydrochloride ≥98% (HPLC) CZC-25146 is a potent selective and metabolically stable inhibitor of leucine-rich repeat kinase-2 (LRRK2) also known as dardarin or PARK8, a kinase with mutations linked to Parkinson’s disease. Because the most common mutation, G2019S, enhances LRRK2 kinase activity, it is hoped that LRRK2 inhibitors may be useful in treating the disease. CZC-25146 was shown to prevent mutant LRRK2-induced injury of cultured rodent and human neurons with mid-nanomolar potency.
 
D0447 D12-116 trifluoroacetate salt ≥98% (HPLC), powder D12-116 is a specific allosteric modulator of the glycine receptor (GlyR). The peptide D12-116 produces a marked enhancement of GlyR function while not affecting a1b2g2S GABAA receptors.