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SML1837 K-604 ≥98% (HPLC) K-604 inhibits against acyl-coenzyme A (acyl-CoA):cholesterol O-acyltransferase-1 (ACAT1, SOAT1) activitiy in a selective (IC50 = 450 nM vs. 102.85 μ M against human ACAT1 and ACAT2, respectively) and acyl-CoA-competitive (Ki = 378 nM against oleoyl-coA) manner. K-604 inhibits cholesterol esterification in human monocyte-derived macrophages (IC50 = 68.0 nM) and enhances cholesterol efflux from THP-1 macrophages in response to HDL3 or apolipoprotein A-I. Oral administration is efficacious against macrophage foam cell formation and atherosclerosis progression among F1B hamsters on a high-fat diet (1-10 mg/kg/day) and apoE-knockout mice (60 mg/kg/day) without affecting plasma cholesterol levels. K-604 is also reported to stimulate autophagy-mediated P301L-Tau degradation in cortical neurons from 3XTg-AD mice (500 nM).
SML1775 K-756 ≥98% (HPLC) K-756 is an orally available, potent and selective tankyrase inhibitor, which binds to the induced-pocket of tankyrase. K-756 is a selective Wnt/β-catenin pathway inhibitor that stabilizes Axin and reduces active β-catenin. K-756 inhibits the proliferation of APC mutant colorectal cancer COLO 320DM and SW403 cell lines.
K3644 K 858 ≥98% (HPLC) Eg5 is a key protein involved in the formation of bipolar spindles. K858 is a selective ATP-uncompetitive mitotic kinesin Eg5 inhibitor. The compound induces mitotic arrest, caspase-3 activation and cell growth inhibition in HCT116 cells.
SML1307 K02288 >98% (HPLC) K02288 is a selective and potent inhibitor of the bone morphogenetic protein (BMP) type I receptor kinases with IC50s in the range 1–2 nM against ALK1 and ALK2. K02288 has IC50 values of 1.1, 1.8, 6.4 nM for ALK2, ALK1 and ALK6 respectively and IC50s of 34.4, 302, 321 and 220 nM for other ALKs (3, 4, 5) and ActRIIA. K02288 specifically inhibited the BMP-induced Smad pathway without affecting TGF-β signaling and induced dorsalization of zebrafish embryos.
K02288 is functionally similar to dorsomorphin, which is known to be the first small-molecule for BMP signaling inhibition.
BMP signalling is associated with many important physiological processes. It acts a central regulator of developmental processes such as organogenesis, gastrulation, mesoderm induction and endochondral bone formation. BMP signals are also related to diseases including pulmonary hypertension, juvenile polyposis syndrome, fibrodysplasia ossificans progressiva and hereditary hemorrhagic telangiectasia syndrome. BMP signaling inhibition might serve as a tool to study its role in other biological processes.
SML2971 K03861 ≥98% (HPLC) New K03861 is an ATP site-binding, cyclin-competitive, type II CDK2 inhibitor that selectively targets and locks the kinase in its inactive DFG-out conformation (CDK2 Kd = 50 nM, DFG-out stabilizing CDK2-C118L/A144C mutant Kd = 9.7 nM without vs. 134.1 nM with bound cycB; CDK2-C118L/A144C-cycA IC50 = 0.8 μM), rendering it incompatible for cyclin bining. K03861 selectively inhibits CDK2-C118L/A144C over CycA-bound wt CDK2 by in vitro kinase assay (IC50 = 0.8 vs. >10 μM) and inhibits the proliferation of immortalized multipotent otic progenitor (iMOP) murine cell line (by 81% and 92%, resepectively, at 0.1 and 1.0 μM).
SML1003   K145 hydrochloride ≥98% (HPLC) It has the ability to prevent leukemia cell growth in vitro.
K145 (3-(2-amino-ethyl)-5-[3-(4-butoxyl-phenyl)-propylidene]-thiazolidine-2,4-dione) is a selective inhibitor of sphingosine kinase-2 (SphK2) and an anticancer agent. K145 selectively inhibited SphK2 in a dose-dependent manner with an IC50 of 4.30 +/- 0.06 μM with no inhibition of SphK1 at concentrations up to 10 μM. K145 significantly suppressed the growth of U937 tumors in nude mice and the growth of JC tumor cells in BALB/c mice.
K1888   K 185 solid Melatonin receptor antagonist.
human ... MTNR1A(4543), MTNR1B(4544)
K2015 K-252a Ready Made Solution, from Nonomuraea longicatena, >98% K-252a is also a specific inhibitor of Trk (tyrosine kinase) receptors and selectively blocks the effect of nerve growth factor. At lower concentrations, K-252a acts as a neuroprotective compound prompting survival of primary neuronal cultures. K-252a induces cell cycle arrest and apoptosis by inhibiting both Cdc2 and Cdc25c. K-252a improves psoriasis in a SCID mouse-human skin model and also suppresses referred mechanical hypersensitivity and neuropeptide up-regulation associated with acute pancreatitis.
human ... NTRK1(4914)
rat ... Prkca(24680)
K1639 K-252a from Nonomuraea longicatena, ≥98% (HPLC)   human ... NTRK1(4914)
rat ... Prkca(24680)
SML1922 K67 ≥98% (HPLC) K67 is a specific inhibitor against the interaction between KEAP1 (Kelch-like ECH-associated protein 1) DC (double glycine repeat and C-terminal region) domain and S349-phosphorylated (human Ser349, mouse Ser351) KIR (Keap1-interacting region) of p62/SQSTM1, thereby preventing phospho-p62 from blocking KEAP1-DC and NRF2 (nuclear factor erythroid 2-related factor 2) DLGex motif association. K67 effectively inhibits the proliferation of HCC (hepatocellular carcinoma) cultures (by 59% of Huh7 cells post 72 h 50 μM K67 treatment) with high cellular p62 S351-phosphorylation by restoring KEAP1-driven NRF2 ubiquitination and degradation.
SML1709 K6PC-5 ≥98% (HPLC) K6PC-5 is a potent and selective sphingosine kinase 1 (SphK1 or SK1) activator that increases keratin 1 and involucrin expression in normal human epidermal keratinocytes cultured in vitro. K6PC-5 promotes differentiation and proliferation of keratinocytes via intracellular Ca2+ signaling.
SML2543 KA-11 ≥98% (HPLC) KA-11 is a broad-spectrum anticonvulsant hybrid molecule that joins the chemical fragments of well-known anti-epileptic drugs such as ethosuximide, levetiracetam, and lacosamide. KA-11 was shown to have antiepileptogenic and antinociceptive properties in animal models. Its mechanism of action is believed to involve influence on the neuronal voltage-sensitive sodium and L-type calcium channels.
K4269 KAB-18 hydrochloride ≥98% (HPLC), powder KAB-18 is a negative allosteric modulator (NAM) at Hα2 β4 nChR nicotinic cholinergic receptors.
SML1853 Kaempferitrin ≥97% (NMR) Kaempferitrin (Lespenefril) is a naturally-occurring kaempferol glycoside with antimicrobial, antioxidant, and anti-inflammatory activities.
Kaempferitrin is a flavonol glycoside, present in several plants, predominant in Bauhinia. It is known to stimulate insulin signaling pathway and induces glucose uptake, by mediating GLUT4 (glucose transporter 4) translocation to adipocyte membrane.. Kaempferitrin aids in lowering blood glucose level and therefore helps to improve the glycemic condition in diabetic animals.
K0250 Kainic acid monohydrate ≥99% (TLC) Kainic acid monohydrate is an agonist at the kainate class of ionotropic glutamate receptors, which induces seizures and neurodegeneration in vivo and is used to induce experimental epilepsy in rodents and study the mechanisms of excitation-induced neuronal apoptosis.
human ... GRIA1(2890), GRIA2(2891), GRIA4(2893), GRIK1(2897), GRIK2(2898), GRIK3(2899), GRIK4(2900), GRIK5(2901), SLC1A1(6505), SLC1A2(6506), SLC1A3(6507)
mouse ... Gria1(14799)
rat ... Gria1(50592), Grik1(29559), Grik4(24406), Grin2a(24409)
K2389 Kainic acid monohydrate ≥98% (HPLC), from Digenea simplex Ionotropic glutamate receptors form ion channels, and conduct Na+ and K+ fluxes. The receptors possess an agonist binding site and it encounters a conformational change upon agonist binding to it. Kainate gated channels participate in glutamate-induced excitatory postsynaptic neuronal potential.
Kainic acid monohydrate is an agonist at the kainate class of ionotropic glutamate receptors, which induces seizures and neurodegeneration in vivo and is used to induce experimental epilepsy in rodents and study the mechanisms of excitation-induced neuronal apoptosis.
SML0370 Kartogenin ≥98% (HPLC) Kartogenin induces the selective differentiation of multipotent mesenchymal stem cells (MSCs) into chondrocytes. Kartogenin binds to filamin A, and disrupts the specific interaction between filamin A and CBFβ (core-binding factor β subunit). Apparently, kartogenin induces chondrogenesis by regulating the nuclear localization of CBFβ.
Kartogenin is a small heterocyclic compound. It is involved in regulating runt-related transcription factor 1 (RUNX1), which plays an important role in chondrocyte proliferation and survival.
SML0525 kb-NB142-70 ≥97% (HPLC) kb-NB142-70 is a derivative of the PKD1 inhibitor CID755673, with approximately 6-fold greater potency (IC50 for inhibition of PKD1 = 28.3 nM vs. 182 nM for CID755673). kb-NB142-70 dose dependently inhibits proliferation of PC3 prostate cancer cell, and blocks migration of the prostate cancer lines PC3 and DU145.
K4144 KB-R7943 ≥98% (HPLC), powder KB-R7943 inhibits the reversed Na(+)/Ca(2+) exchanger, NCX. In cardiomyocytes, Ca2+ is released from intracellular stores during contraction, and sequestered again during relaxation. NCX is the primary mechanism that prevents Ca2+ overload due to influx of calcium across the plasma membrane.
SML1043 KC7F2 ≥98% (HPLC) KC7F2 is a cell permeable potent HIF-1 pathway inhibitor. KC7F2 inhibits the activation of HIF-target genes such as carbonic anhydrase IX, matrix metalloproteinase 2 (MMP2), enolase 1, and endothelin 1. KC7F2 suppresses the protein accumulation of HIF-1? in cancer cell lines by inhibition of its protein synthesis at the translation level. KC7F2 is preferentially cytotoxicity to cancer cells, an effect that is increased in hypoxia.
SML2547 KCC-07 ≥98% (HPLC) KCC-07 is a brain penetrant, potent and selective inhibitor of MBD2 (methyl-CpG-binding domain protein 2) that inhibits binding of MBD2 to methylated DNA and activates brain specific angiogenesis inhibitor 1 (BAI1) inducing anti-proliferative BAI1/p53/p21 signaling. KCC-07 inhibits medulloblastoma cell proliferation, and inhibits tumor growth in mice xenograft models of medulloblastoma.
SML2774 KDOAM25 hydrochloride hydrate ≥98% (HPLC) KDOAM25 is a selective inihbitor of the KDM5 family histone demethylases JARID1A, JARID1B, JARID1C and JARID1D with IC50 values < 60 nM. JARID1A and JARID1B are independently overexpressed in some cancers with JARID1B (KDM5B, PLU1) also identified as a potential oncogene, a repressor of tumour repressor genes. JARID1C (KDM5C) and JARID1D (KDM5D) are located on the X- and Y-chromosomes respectively. KDOAM25′s closest off-target is JMJD2C (selectivity >400 fold). It shows no activity on other tested 2-OG family members, including FIH, NO66, MINA53 and PHD2. KDOAM25 is active in cells.
SML2612 KDS2010 ≥98% (HPLC) KDS2010 is a highly selective, substrate-competitive, potent and reversible monoamine oxidase MAO-B inhibitor (IC50 = 7.6 nM/MAO-B vs >100 μM/MAO-A; little affinity toward 99 kinases and 84 non-kinase targets) with excellent ADME/Tox profiles (IC50 >10 μM/P450, >50 μM/hERG), brain permeability and oral availability ([rat F = 123.5%; 10 mg/kg p.o.). KDS2010 restores memory impairments in APP/PS1 mice following either short- or long-term treatment (3-d or 4-wk 10 mg/kg/day p.o.) without aberrant GABA levels observed with prolonged irreversible inhibition by selegiline (MAO-B/MAO-A IC50 = 10 nM/1.5 μM) due to compensatory diamine oxidase (DAO) induction.
SML2375 KDU691 ≥98% (HPLC) KDU691 is an orally active imidazopyrazine class antiparasitic that inhibits Plasmodium & Cryptosporidium phosphatidylinositol-4-OH kinase, PI(4)K, in an ATP-competitive, highly potent and selective manner (IC50/[ATP] = 1.5 nM/10 μM/P. vivax & 17 nM/3 μM/C. parvum PI(4)K) with little or no activity against human PI3Kα/β/γ/δ, PI4KIIIβ, VPS34, and 36 human protein kinases. KDU691 is effective against human pathogens P. falciparum, P. vivax, C. parvum and C. hominis, as well as simian parasite P. cynomolgi. KDU691 blocks Plasmodium development in all life-cycle stages and displays in vivo efficacy in murine models of malaria and cryptosporidiosis.
SML2180 KEA1-97 ≥98% (HPLC) KEA1-97 is a Thioredoxin-Caspase 3 interaction disruptor. It was found to target lysine 72 of thioredoxin, inhibiting its interactions with caspase 3 and inducing apoptosis without affecting other thioredoxin activity. KEA1-97 induced apoptosis in breast cancer cells and treatment of immune-deficient SCID mice at 5 mg/kg ip impaired breast tumor xenograft growth.
K3888 Kenpaullone ≥98% Kenpaullone is a potent inhibitor of CDK1/cyclin B (IC50 = 400 nM), CDK2/cyclin A (IC50 = 680 nM), CDK2/cyclin E (IC50 = 7.5 uM) and CDK5/p25 (IC50 = 850 nM).
human ... CDC2(983)
mouse ... Gsk3b(56637)
rat ... Gsk3b(84027)
K2753 (±)-Ketamine hydrochloride solid Selective NMDA glutamate receptor antagonist; veterinary anesthetic.
human ... GRIN1(2902), GRIN2A(2903), GRIN2B(2904), GRIN2C(2905), GRIN2D(2906), GRIN3A(116443), GRIN3B(116444)
K1884 S-(+)-Ketamine hydrochloride Selective NMDA glutamate receptor antagonist.
human ... GRIN1(2902), GRIN2A(2903), GRIN2B(2904), GRIN2C(2905), GRIN2D(2906), GRIN3A(116443), GRIN3B(116444)
K113 Ketamine hydrochloride/xylazine hydrochloride solution This is a solution of ketamine hydrochloride, an NMDA receptor antagonist, and xylazine hydrochloride, an α2- adrenergic receptor agonist.
K4138 Ketamine hydrochloride/xylazine hydrochloride solution This is a solution of ketamine hydrochloride, an NMDA receptor antagonist, and xylazine hydrochloride, an α2- adrenergic receptor agonist.
UC280 Ketoconazole Antifungal agent
Ketoconazole is an imidazole derivative. It plays an important role in inhibiting the conversion of lanosterol to ergosterol in the cell wall of fungi. Ketoconazole has therapeutic effects against dermatophytosis, superficial candidiasis, and paracoccidioidomycosis.
human ... ABCB1(5243), CYP11B1(1584), CYP11B2(1585), CYP17A1(1586), CYP19A1(1588), CYP1A2(1544), CYP24A1(1591), CYP26A1(1592), CYP3A4(1576), CYP51A1(1595), KCNH1(3756)
mouse ... Abcb1a(18671), Abcb1b(18669)
rat ... Alox5(25290), Cyp17a1(25146), Cyp51(25427), Cyp7a1(25428)
K1751 Ketoprofen ≥98% (TLC) It serves as an efficient drug to treat ankylosing spondylitis, rheumatoid arthritis and osteoarthritis. It also has antipyretic and analgesic effects. Ketoprofen prevents the action of prostaglandin synthetase.
Non-steroidal anti-inflammatory compound that is selective for COX-1.
human ... ALB(213), IL8RA(3577), PTGS1(5742), PTGS2(5743)
SML1654 R-Ketorolac ≥95% (HPLC) Ketorolac ((rac)-5-benzoyl-1,2-3H-pyrrolo[1,2a] pyrrole1-carboxylic acid) is a non-steroidal anti-inflammatory drug (NSAID). It is used as a racemic mixture that contains a 1:1 ratio of the R(+) and S(−) stereoisomers. It is broadly used off-label as a parenteral analgesic in children. Ketorolac serves as a non-narcotic analgesic. It prevents the synthesis of prostaglandins, peripheral to the central nervous system.
R-Ketorolac is potent and selective Rho-family GTPases Cdc42 (cell division control protein 42) and Rac1 (Ras-related C3 botulinum toxin substrate 1) allosteric inhibitor that modulates downstream GTPase-dependent physiologic responses critical to tumor metastasis. R-ketorolac significantly inhibits ovarian cancer cell adhesion, migration, and invasion.
K8250 11-Ketotestosterone 11-Ketotestosterone is a minor androgen in humans, but a major androgen in fish.
K2628   Ketotifen fumarate salt H1 histamine receptor antagonist.
Ketotifen fumarate plays a key role in preventing histamine release by blocking the histamine H1 receptors. It interferes with the release of histamine, serotonin and other inflammatory mediators from mast cells. It exhibits with anti-allergic activity, anti-inflammatory effects including mast cell stabilization. It has been widely used for ophthalmic allergic conjunctivitis.
human ... HRH1(3269), PDE7B(27115)
SML2184 Kevetrin hydrochloride ≥98% (HPLC) Kevetrin is an activator/stabilizer of wild type p53 tumor suppressor protein in human lung carcinoma and ovarian cancer cells that induces cell cycle arrest and apoptosis. Additionally Kevetrin down-regulates oncogenic mutant p53 in OVCAR-3 ovarian cancer cells. Kevetrin inhibits tumor growth in xenograft model of ovarian cancer.
SML0619   KG-548 ≥97% (HPLC) KG-548 is an inhibitor of the hypoxia signaling transcription factor complex. Hypoxia inducible factor (HIF) is a heterodimer of two bHLH-PAS (basic Helix Loop Helix - Per-ARNT-Sim) subunits, including a HIF-α paralog (HIF-1α, -2α, -3α) and aryl hydrocarbon receptor nuclear translocator (ARNT, also known as HIF-β. KG-548 selectively binds within the ARNT PAS domain of the ARNT subunit of the HIF activator that recruits TACC3 (Transforming Acidic Coiled Coil Containing Protein 3) coactivator, competing with TACC3 for binding to the ARNT PAS-B domain and thus acting as as an ARNT/TACC3 disruptor.
K3394 KH7 ≥98% (HPLC) KH7 is a selective inhibitor of soluble adenylyl cyclase. Soluble adenylyl cyclase (sAC) is an ubiquitously expressed, essential component of cAMP-signaling.
K4019 KHS101 ≥98% (HPLC) KHS101 is a small molecule that drives neuronal differentiation of hippocampal neuronal progenitor cells (NPC). Treatment of NPCs with KHS101 induces expression of the neurogenic transcription factor NeuroD and the neuronal marker Tuj1, and exhibit neuronal morphology and spiking activity (EC50 1 uM). KHS101 binds tightly to TACC3, which is a structural component of the centrosome and mitotic spindle apparatus. TACC3 loss of function studies in mice and stem cells suggest that TACC3 controls progenitor cell expansion and terminal differentiation during development.
SML1161 Ki11502 ≥98% (HPLC) Ki11502 is a potent, ATP-competitive multikinase inhibitor that is selective for PDGF receptor. Ki11502 inhibits malignant hematopoietic cells proliferation and induces their apoptosis. Ki11502 is effective against colorectal cancer SW480 cell line.
SML0971   Ki 16425 ≥98% (HPLC) Ki 16425 possesses a short-lived inhibitory activity. It has been studied that Ki 16425 is effective in the inhibition of neuropathic pain‐like behaviors.
Ki16452 is a potent antagonist of the lysophosphatidic acid receptors LPA1 and LPA3, with greater than 30-fold selectivity for LPA1 over LPA2. The Ki values for LPA1 and LPA3 are 250 nM and 360 nM, respectively.
SML2674 Ki20227 ≥98% (HPLC) Ki20227 is an orally active, potent and selective M-CSF receptor c-Fms (CSF-1R) tyrosine kinase inhibitor (IC50 = 2 nM vs. 12 nM/KDR, 451 nM/c-Kit, 217 nM/PDGFβ; >1 μM/BTK, EGFR, FGFR2, FLT3, Fyn, Met, c-Src, PKA, PKCα) that inhibits M-CSF-dependent (50 ng/mL) c-Fms phosphorylation (by >90% at 10 nM; RAW264.7) and cell growth (IC50 = 14 nM; M-NFS-60). Ki20227 prevents osteolysis in a rat model of bone metastasis (50 mg/kg/day p.o.) by inhibiting A375 tumor-induced osteoclast formation and decreases the number of osteoclast-like cells on bone surfaces in ovariectomized rats (20 mg/kg/day p.o.) in vivo.
SML1871 KIN1400 ≥98% (HPLC) KIN1400 is innate immune agonists of IRF3 activation that induces IRF3 and MAVS dependent innate immune antiviral genes and IFNβ expression. KIN1400 is a broad spectrum antiviral compound that suppresses replication of hepatitis C virus, West Nile virus, dengue virus and other Flaviviridae, as well as Filoviridae (EV), Orthomyxoviridae (influenza A virus), Arenaviridae (LV) and Paramyxoviridae (RCV, NV).
SML1866 KIN1408 ≥98% (HPLC) KIN1408 is a small molecule that targets factors at or above the level of MAVS in the RLR signaling pathway to drive IRF3 activation (IRF3 nuclear translocation ECmax = 5 μM in 20 h; Huh7 cells) without significant cytotoxicity (50 μM/20 h in Huh7 or 20 μM/36 h in HEK293 cultures). KIN1408 induces cellular transcription of innate immune genes (Eff. conc. 1.25-20 μM in 20 h; PMA-differentiated THP-1 cells) in a MAVS- and IRF3-dependent manner and exhibits broad-spectrum anti-viral activity (Eff. conc. 1-5 μM), including dengue virus 2 (DV2; Huh7), influenza A (IAV H3N2; HEK293), RSV (A2 strain; HeLa), Ebola (EBOV strain Zaire; HUVECs), Nipah virus (NiV; HUVECs), and Lassa virus (LASV; HUVECs). MAVS signaling activation upon Zika virus infection or KIN1408 treatment is reported to result in pTBK1 mitochondria relocalization and caspase 3-mediated apoptosis in human neuroepithelial stem (NES) cells.
SML2361 Kinesore >97% (HPLC) Kinesore is a cell penetrant and potent activator of kinesin-1 that induces kinesin light chain tetratricopeptide repeat domain-dependent kinesin-1 activation in the absence of organelle cargo-adaptor engagement. It inhibits kinesin-1 interaction with peptide fragment of organelle-specific cargo adaptors. Kinesore induces kinesin light chain conformational switch that causes remodeling of the microtubule network in cells.
SML2098 KINK-1 hydrochloride ≥98% (HPLC) KINK-1 (Kinase Inhibitor of NF-ΚB-1; Bay 65-1942; CmpdA; Compound A) is an ATP-competitive, IKKβ-selective IΚB kinase (IKK) inhibitor (Ki against ATP = 2 nM/IKKβ and 135 nM/IKKα) that potently inhibits IKKβ-catalyzed GST-IΚBα(1–54) phosphorylation (IC50 = 4 nM, 200 nM ATP) without affecting (IC50 >10μM) IKK3 or 27 other kinases, lipases, phosphatases, caspases, and MMPs. KINK-1 effectively inhibits NF-ΚB activation and cytokines production in various human and murine cultures (IC50 from 18 to 502 nM) and is efficacious against LPS-induced plasma TNF-α production in mice and rats in vivo (EC50 = 9.1 and 6.6 mg/kg p.o., repectively) with good pharmacokinetic profile and oral availability. KINK-1 is also shown to effectively inhibit OVA-induced lung inflammation in a rat model of asthma (ED50 <0.3 mg/kg p.o.) without adverse effects to the animals.
SML2903 KIRA8 ≥98% (HPLC) New KIRA8 is an ATP-competitive, potent and selective IRE1α kinase inhibitor (IRE1α/β Ki = 2/120 nM) that attenuates IRE1α endonuclease activity (IRE1α/β IC50 = 5/55 nM) with good kinome selectivity. KIRA8 inhibits thapsigargin-induced UPR (IC50 = 99 nM; HT1080 XBP1-Luc cells) and shows therapeutic efficacy in murine models of type 1 diabetes (T1D), pulmonary fibrosis, multiple myeloma (MM), and pancreatic neuroendocrine tumors (PanNET) in vivo (30-50 mg/kg/day i.p.).
SML0960   KKL-35 ≥98% (HPLC) KKL-35 is a small molecule that blocks bacterial trans-translation, a proof-reading mechanism that eliminates mRNAs lacking stop codons from translation complexes. KKL-35 inhibits trans-translation, and subsequent cell growth in a broad spectrum of bacterial strains.
SML2538 KL-2 ≥98% (HPLC) Disruptor of SEC (super elongation complex)
KL-2 is a disruptor of the super elongation complex (SEC). KL-1 blocks the interactions of positive transcription elongation factorb (P-TEFb) and the SEC-scaffolding protein AFF4 resulting in decreased Polymerase II (Pol II) activity and production of Pol II-transcribed genes. KL-2 was shown to cause downregulation of heat shock genes, and was non-toxic and active in an animal model of cancer.
SML1032   KL001 ≥98% (HPLC) KL001 stabilizes cryptochrome (CRY), preventing ubiquitin-dependent degradation. CRY proteins are part of a feedback loop, acting as transcription repressors to inhibit CLOCK-BMAL1 components of the circadian clock. KL001 stabilization of CRY proteins results in lengthening of the circadian period, and also inhibited glucagon-induced gluconeogenesis in primary hepatocytes. Other compounds affecting circadian rhythms include Casein kinase I (CKI) inhibitors such as longdaysin (Sigma Prod. No. SML0127) and synthetic ligands for the nuclear receptors REV-ERB such as SR8278 (Sigma Prod. No. S9576), but KL001 appears to be the first small molecule that specifically acts on CRY proteins.
SML1998 KLH45 ≥98% (HPLC) KLH45 is an in vivo-active, potent and selective irreversible inhibitor of DDHD2. KLH45 inactivates brain levels of DDHD2 and increases levels of triglycerides in mouse brain.
SML2166 KML29 ≥98% (HPLC) KML29, an O-hexafluoroisopropyl (HFIP) carbamate analogue of JZL184. is a potent and orally active monoacylglycerol lipase (monoglyceride lipase; MAGL; MGLL; MGL) inhibitor (IC50 = 5.9/15/43 nM against human/mouse/rat MAGL) that targets MAGL active site with greatly improved selectivity (rat/mouse ABHD6 IC50 = 1.60/4.87; no inhibitory activity against human/rat/mouse fatty acid amide hydrolase (FAAH) up to 50 &mu;M). KML29 in vivo treatment results in a selective upregulation of 2-arachidonoyl glycerol (2-AG), but not N-arachidonoyl-ethanolamine (AEA) in mice (brain Emax &sim;20 mg/kg p.o. or i.p.; peripheral Emax &sim;1 mg/kg p.o.) and rats (brain Emax &sim;40 mg/kg i.p.). KML29 reduces inflammatory and neuropathic nociceptive behaviour in animal studies without cannabimimetic side effects seen with dual FAAH & MAGL inhibition, chronic administration, however, leads to CB1 receptor desensitization as observed with other MAGL inhibitors.
I2142 KN-62 ≥95%, powder Selectively inhibits rat brain Ca2+/calmodulin-dependent protein kinase II.
human ... P2RX7(5027)
K1385 KN-93 ≥98% (HPLC) KN-93 is a selective Ca2+/calmodulin-dependent protein kinase II inhibitor, which has been implicated in the regulation of smooth muscle contractility. CaM kinase II activation was inhibited by KN-93 pretreatment (IC50 ~1 μM). KN-93 inhibited histamine-induced tonic force maintenance, whereas early force development and MLC20 phosphorylation responses during the entire time course were unaffected. Both force development and maintenance in response to KCl were inhibited by KN-93. Rapid increases in KCl-induced MLC20 phosphorylation were also inhibited by KN-93, whereas steady-state MLC20 phosphorylation responses were unaffected. In contrast, phorbol 12,13-dibutyrate (PDBu) did not activate CaM kinase II and PDBu-stimulated force development was unaffected by KN-93. Thus KN-93 appears to target a step(s) essential for force maintenance in response to physiological stimuli, suggesting a role for CaM kinase II in regulating tonic contractile responses in arterial smooth muscle. Pharmacological activation of protein kinase C bypasses the KN-93 sensitive step.
SML0964   KNK437 ≥98% (HPLC) KNK437 inhibits the accumulation of heat shock proteins (including hsp -27, -40, -70, -72 and -105). KNK437 inhibits thermotolerance in cells with greater potency than quercetin.
KNK437 is a benzylidene lactam compound.
K2144 Ko143 hydrate ≥98% (HPLC) Ko143 has been used as a positive control inhibitor on functions of BCRP in MCF7 and BCRP over-expressing MCF7/MX100 cell lines using a BCRP prototypical substrate mitoxantrone. The ABCG2 transporter breast cancer resistance protein (BCRP) plays an important role in disposition of many drugs and environmental toxins. Ko143 displays > 200-fold selectivity over P-gp and MRP-1 transporters. It increases intracellular drug accumulation and reverse BCRP-mediated multidrug resistance. It blocked topotecan and ABZSO transport in a concentration-dependent manner. Ko143 is reported to be a more specific inhibitor of BCRP than other known inhibitors of BCRP such as fumitremorgin C and GF120918.
Ko143 has been used as a positive control inhibitor on functions of breast cancer resistance protein (BCRP) using a BCRP prototypical substrate mitoxantrone. BCRP, an ABCG2 transporter, plays an important role in disposition of many drugs and environmental toxins. Ko143 displays > 200-fold selectivity over P-gp and MRP-1 transporters and thus is more specific than other known BCRP inhibitors such as fumitremorgin C and GF120918. It increases intracellular drug accumulation and reverses BCRP-mediated multidrug resistance. It blocks topotecan and ABZSO transport in a concentration-dependent manner.
SML0961   Kobe0065 ≥98% (HPLC) Kobe0065 binds to Ras-GTP, blocking interactions with Raf kinase. Kobe0065 inhibits anchorage-dependent and -independent growth, blocks MEK/ERK activity and induces apoptosis in H-rasG12V transformed NIH3T3 cells. The compound Kobe0065 also inhibts tumor growth in SW480 colon cancer cell xenografts.
K3125 Kojic acid Kojic acid is derived from some fungal species such as, Aspergillus, Acetobacter and Penicillium.. It halts melanin synthesis by inhibiting tyrosinase enzyme. It is used in the preparation of skin whitening cosmetics. However, kojic acid usage is minimal in cosmetics, as it induces skin irritation by its unstability and cytotoxic nature during long storage. It is an antioxidant and elicits radioprotective effects on chelating with manganese and zinc.
Tyrosinase inhibitor.
SML1029   KP372-1 ≥98% (HPLC) KP372-1 is a potent inhibitor of AKT and PKD. KP-372-1 blocks PI3K/AKT/mTOR signaling pathways, and induces apoptosis in leukemia cell lines and primary tumor cells from patients with AML.
SML2411 KPR-2579 ≥98% (HPLC) KPR-2579 does not distress temperature of the body at any given dose. It helps to block the activation of C-fiber single-unit afferent activities (SAAs), stimulated by acetic acid (AA).
KPR-2579 is a potent and selective transient receptor potential melastatin 8 (TRPM8; CRM1) antagonist (IC50 = 80/89 nM against EC80 MeOH-induced Ca2+ response in human/rat CRM1 HEK293T transfectants) with good selectivity (IC50 >30 μM against ligand-induced Ca2+ influx using hTRPA1, hTRPV1, or hTRPV4 transfectants) and oral availability (59% post 10 mg/kg p.o.; rats). KPR-2579 exhibits in vivo efficacy against icilin-induced wet-dog shakes (WDS; by 31/73/100% with 1/3/10 mg/kg p.o. 1h prior to icilin i.p.; female rats) and distension-induced rhythmic bladder contraction (by 70/89% with 0.1/0.3 mg/kg i.v.; male rats) without negative cardiovascular effects.
K4389 KR-32568 ≥98% (HPLC), solid Sodium/hydrogen exchanger-1 (NHE-1) inhibitor; IC50 = 0.23 μM; inhibited NHE-1-mediated rabbit platelet swelling; in anesthetized rats, reduced infarct size from 67% (control) to 43% (at 0.1 mg/kg) and 24% (at 1.0 mg/kg); reduced number of ventricular premature beats from 530 to 266 (at 0.1 mg/kg) and 115 (at 1.0 mg/kg); reduced ventricular fibrillation incidence from 17 to 8 (0.1 mg/kg) and 0 (1.0 mg/kg); implications for research and treatment of myocardial ischemic diseases.
human ... SLC9A1(6548)
K4264 KR-62436 hydrate ≥95%, powder KR-62436 is a competitive inhibitor of dipeptidyl peptidase-IV (DPP-IV). DPP-IV is a serine protease which inactivates glucagon-like peptide (GLP-1); IC50 0.1-0.8 μM; GLP-1 is a potent stimulus for insulin secretion and inducer of satiety after food intake, but it has a very short action (1 min) because it is rapidly degraded by DPP-IV; blocking DPP-IV increases GLP-1 action and increases plasma insulin levels; DPP-IV inhibitors and KR-62436 have clinical potential as anti-diabetic agents
SML1905   KR7 trifluoroacetate salt ≥98% (HPLC) KR7 is a non-toxic and serum stable heptapeptide that inhibits insulin amyloid fibrillation. KR7 primarily targets the fiber elongation step.
SML1304   KRCA-0008 ≥98% (HPLC) KRCA-0008 is a potent and selective ALK (aplastic lymphoma kinase) and Ack1 inhibitor that exhibits in vivo efficacy in xenograft mice model. KRCA-0008 potently inhibits ALK mutants L1196M, C1156Y, F1174L and R1275Q.
SML1412 KRIBB11 trifluoroacetate salt ≥98% (HPLC) KRIBB11 is an inhibitor of the transcription factor Heat Shock Factor 1 (HSF1) with an IC50 value of 1.2 μM. KRIBB11 blocks induction of HSF1 downstream target proteins such as HSP27 and HSP70 by impairing the recruitment of Positive Transcription Elongation Factor b (P-TEFb) to the HSF1 transcriptional complex, preventing HSF1-mediated gene expression KRIBB11 inhibits tumor growth in vivo and acts synergistically to increase apoptosis in cancer cells treated with the HSP90 inhibitors Geldanamycin and 17-AAG.
KRIBB11 is capable of preventing the proliferation of cancer cells. It has the ability to stimulate apoptosis and can arrest the cell cycle at G2/M phase.
K3519 KRM-III ≥98% (HPLC) KRM-III is an inhibitor of T cell antigen receptor (TCR), an inhibitor of phorbol myristate acetate (PMA) /ionomycin-induced nuclear factor of activated T cells (NFAT) activation and T cell proliferation.
SML2464 KRN2 ≥98% (HPLC) KRN2 is a specific and potent inhibitor of nuclear factor of activated T cells 5 (NFAT5) that inhibits formation of NF-κB p65-DNA complexes. KRN2 suppresses migration of Fibroblast-like synoviocytes stimulated with TGF-β. KRN2 ameliorates experimental arthritis in mice.
SML0957   KRN633 ≥98% (HPLC) KRN633 is a cell-permeable; reversible and ATP-competitive inhibitor of vascular endothelial growth factor receptor tyrosine kinase (VEGFR) with IC50 values of 170, 160, and 125 nM for VEGFR-1, -2, -3, respectively. Krn633 inhibits PDGFR-α and c-Kit only at higher concentrations (IC50 = 0.97 and 4.33 μM, respectively) and is inactive towards a panel of 17 other kinases (IC50 >/= 10 μM).
SML0484 KS-176 ≥98% (HPLC) KS-176 is a potent specific inhibitor of Breast Cancer Resistance Protein (BCRP) / ATP-binding cassette sub-family G member 2 (ABCG2) with no inhibition of the ATP binding cassette (ABC) transporters P-gp and MRP1.
SML1436 KS 370G ≥98% (HPLC) KS370G is a synthetic caffeamide derivative that exhibits hypoglycemic effects in mice model of diabetes. Recent study indicates that KS370G exhibits antifibrotic properties in the murine unilateral ureteral obstruction (UUO) model by reduction of inflammation and oxidative stress.
SML1364 KT109 ≥98% (HPLC) KT109 is a potent and selective inhibitor of Diacylglycerol lipase DAGLβ. Diacylglycerol lipases DAGLα and DAGLβ are serine hydrolases that biosynthesize the endocannabinoid 2-arachidonoylglycerol (2-AG). A lack of selective inhibitors has hampered study of these lipases. KT109 is a potent and selective DAGLβ inhibitor with an IC50 of 42 nM, ~60-fold selectivity for DAGLβ over DAGLα, and negligible activity against FAAH, MGLL and ABHD11, other key enzymes involved in endocannabinoid signaling. KT109 shows some inhibitory activity against PLA2G7 (IC50 = 1 μM) but no inhibitory activity against cytosolic phospholipase A2 (cPLA2 or PLA2G4A). The main off target inhibition against ABHD6 (IC50 = 16 nM) can be controlled for by use of the related compound, KT195, a potent (IC50 = 10 nM) and selective ABHD6 inhibitor with negligible activity against DAGLβ. KT109 disrupts the lipid network involved in macrophage inflammatory responses, lowering 2-AG, as well as arachidonic acid and eicosanoids, in mouse peritoneal macrophages.
SML1688 KT172 ≥98% (HPLC) KT172 is a Diacylglycerol lipase (DAGL) inhibitor selective for DAGLβ. Diacylglycerol lipases DAGLα and DAGLβ are serine hydrolases that biosynthesize the endocannabinoid 2-arachidonoylglycerol (2-AG). A lack of selective inhibitors has hampered study of these lipases. KT172 is a new potent and selective DAGLβ inhibitor with an IC50 of 60 nM for recombinant DAGLβ vs 140 nM for DAGLα, although it is not active against DAGLα in vivo, and negligible activity against FAAH, MGLL and ABHD11, other key enzymes involved in endocannabinoid signaling or against cytosolic phospholipase A2 (cPLA2 or PLA2G4A). The main off target inhibition against ABHD6 (IC50 values of 5 nM) can be controlled for by use of the related compounds, KT195 SML1308 or KT185 SML1249, potent and selective ABDH6 inhibitors with negligible activity against DAGLβ. KT172 disrupts the lipid network involved in macrophage inflammatory responses, lowering 2-AG, as well as arachidonic acid and eicosanoids, in mouse peritoneal macrophages.
SML1248 KT182 ≥98% (HPLC) KT182 is a very potent, orally bioavailable, selective inhibitor of ABHD6 (a/b-Hydrolase Domain Containing 6). IC50 = 1.7 nM. KT182 inhibits ABHD6 activity in the brain and liverin mice (ip administration).
SML1249   KT185 ≥98% (HPLC) KT185 is a very potent, selective inhibitor of a/b-Hydrolase Domain Containing 6 (ABHD6). The compond KT185 is orally bioavailable and inhibits ABHD6 activity in the brain and liver of mice.
SML1308   KT195 ≥98% (HPLC) KT195 is a potent (IC50 = 10 nM) and selective inhibitor of α/β-hydrolase domain-containing 6 (ABHD6), a serine hydrolase that acts as an alternative hydrolase of the endocannabinoid 2-arachidonoylglycerol (2-AG). KT195 has negligible activity against other serine hydrolases such as DAGLβ and has been used as a control probe for studies of DAGLβ as well as being a probe on its own to study ABHD6. KT195 treatment of Neuro2A cells caused significant accumulation of 2-AG. KT195 also lowered interleukin-1β (IL-1β) secretion from lipopolysaccharide-treated macrophages suggesting ABHD6 involvement in this activity as well.
SML1250 KT203 ≥98% (HPLC) KT203 is a very potent, selective inhibitor of ABHD6 (IC50 = 0.82 nM). KT203 inhibits ABHD6 activity in the liver, but not the brain following ip injection in mice.
K3761 KT 5720 ≥98% (HPLC), powder Specific, cell-permeable inhibitor of protein kinase A (PKA). No significant effect on protein kinase C (PKC), protein kinase G (PKG) or myosin light chain kinase (MLCK).
K1388 KT 5823 ≥85% (HPLC), lyophilized powder Selective inhibitor of PKG.
SML1257 KU-0060648 ≥98% (HPLC) KU-0060648 is a very potent dual inhibitor of DNA-PK and PI3K. The IC50 values for inhibition of DNA-PK in MCF7 and SW620 cells are 19 and 170 nM, respectively. The compound KU-0060648 inhibits MCF7 PI3K activity with an IC50 of 39 nM, but is inactive against PI3K in SW620, suggesting a cell-dependent mechanism of inhibition. KU-0060648 increases sensitivity to DNA damaging cytotoxic drugs such as etoposide and doxorubicin in tumor cell lines expressing DNA-PK. KU-0060648 stimulates Cas9 (CRISPR associated protein 9) mediated genome editing by enhancing the rate of homology directed-repair (HDR) and decreasing the rate of NHEJ (non-homologous end-joining).
KU-0060648 is observed to inhibit proliferation and initiate apoptosis in hepatocellular carcinoma. KU-0060648 is useful in chemotherapy as it increases the efficiency of double stranded breaks initiated by anticancer drugs.
SML0382 KU 0063794 ≥98% (HPLC) KU 0063794 induces autophagy. It is cell-permeant and suppresses activation and hydrophobic motif phosphorylation of protein kinase B (Akt), p70 ribosomal S6 kinase (S6K) and serum and glucocorticoid protein kinase (SGK).
KU 0063794 is a potent and selective inhibitor of mammalian target of rapamycin (mTOR) (IC50 ~10 nM for both mTORC1 and mTORC2) that inhibits both mTORC1 and mTORC2 in vitro and in vivo (IC50 ~10 nM for both mTORC1 and mTORC2). KU 0063794 does not significantly inhibit 76 other protein kinases tested as well as seven lipid kinases including PI3K and AKT.
SML1109 KU-55933 ≥98% (HPLC) KU-55933 is a very potent, specific inhibitor of Ataxia telangiectasia (A-T) mutated (ATM) kinase (IC50 = 13 nM). KU-22933 treatment sensitizes cancer cells to ionizing radiation and cytotoxic drugs. The compound KU-22933 blocks ATM-mediated phosphorylyation of p53, gH2AX, NBS1, and SMC1.
SML1416 KU-60019 ≥97% (HPLC) KU-60019 is a potent inhitor of ATM (ataxia telangiectasia mutated) kinase, a member of phosphatidylinositol-3-kinase-related kinase family that is critical in regulating cell cycle checkpoints and DNA repair. KU-60019 has an IC50 value of 6.3 nM. KU-60019 radiosensitizes U1242 human glioma cells, and also blocks U1242 cell migration and invasion through matrigel.
SML2273 KUNB31 ≥98% (HPLC) KUNB31 is an isoform-selective inhibitor of Hsp90β with an IC50 value of 180 nM and > 50-fold selectivity over closely related isoforms Hsp90α and GRP94.Hsp90 inhibitors currently in clinical trials are all pan-inhibitors with multiple side effects including induction of the pro-survival heat shock response. KUNB31 was shown to induce the degradation of Hsp90β-dependent client proteins, but not those of Hsp90α and GRP94, and did not induce production of Hsp90. It showed anti-proliferative activity against NCI H23 (non-small cell lung cancer), UC3 (bladder cancer), and HT-29 (colon adenocarcinoma) cells with low micromolar IC50 values, while requiring more than 100 μM against non-cancerous human embryonic kidney HEK-293 cells.
SML1843 Kurarinone ≥98% (HPLC) Kurarinone, a flavanone from Sophora flavescens roots, is a potent activator of the large-conductance calcium-activated potassium channel (BKCa channel). Kurarinone exhibits strong preference to potentiate the homomeric BKCa channel composed only of the α subunits. Kurarinone reduces acetylcholine induced contraction of rat urinary bladder strips and decreased the voiding frequency in a rat OAB model. Kurarinone exhibits cytotoxic and antiinflamatory activity. Kurarinone sensitizes TRAIL-induced tumor cell apoptosis via suppression of NF-KB-dependent cFLIP expression.
K3769 KW-3902 ≥98% (HPLC) KW-3902 is an A1 adenosine receptor antagonist and is over 800 fold more selective for an A1 receptor versus the A2A receptor.
SML0948   KY02111 ≥98% (HPLC) KY02111 promotes differentiation of human pluripotent stem cells (hPSCs) to cardiomyocytes by inhibiting WNT signaling in hPSCs in a manner that is distinct from that of previously studied WNT inhibitors. The substantial (98%) differentiation of hPSCs to cardiomyocytes with KY02111 is achieved in xeno-free and cytokine-free conditions.
SML1506 KY-05009 ≥98% (HPLC) KY-05009 is a Traf2- and Nck-interacting kinase (TNIK) inhibitor that inhibits the epithelial-to-mesenchymal transition (EMT) in cancer cells.
KY-05009 is also known as (5-(4-methylbenzamido)-2-(phenylamino) thiazole-4-carboxamide). It prevents the proliferation induced by interleukin-6 and promotes cell death by blocking Wnt signaling in multiple myeloma (MM) cells. KY-05009 is a novel aminothiazole, which possesses anti-cancer activity in human colorectal cancer cells. KY-05009 prevents migration and invasion stimulated by TGF-β1 (transforming growth factor beta 1).
SML1831 KYA1797K potassium salt ≥98% (HPLC) KYA1797K is an inhibitor of both Wnt/β-catenin and Ras pathways. It binds to the axin regulators of the G-protein signaling (RGS) domain enhancing formation of the β-catenin destruction complex and inducing activation GSK3β, which results in phosphorylation and subsequent degradation of both β-catenin and K-Ras. KYA1797K was show to suppress tumor growth and progression in mouse xenografts of CRC cells that had APC and K-Ras mutations.
SML1378   KYL trifluoroacetate salt ≥95% (HPLC) KYL is a potent and selective EphA4 receptor tyrosine kinase antagonist that inhibits EphA4-EphrinA5 interactions. KYL binds to the ephrin-binding domain of EphA4.
K3375 Kynurenic acid ≥98% Kynurenic acid (KynA) is a non-selective antagonist of N-methyl-d-aspartate (NMDA), α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) and kainate receptors. It blocks kainic acid neurotoxicity. Kynurenic acid also blocks nicotinic acetylcholine receptors. It is a by-product of tryptophan catabolic pathway. Kynurenic acid is a neuromodulator and controls the levels of glutamate, dopamine, acetylcholine and α-aminobutyric acid (GABA). KynA controls neuroendocrine functions and altered levels of KynA is a potential marker in depression, schizophrenia Alzheimer′s and Huntington′s diseases. Normal levels of KynA in the brain is crucial for the cognitive function.
human ... CHRNA1(1134), CHRNA10(57053), CHRNA2(1135), CHRNA3(1136), CHRNA4(1137), CHRNA5(1138), CHRNA6(8973), CHRNA7(1139), CHRNA9(55584), CHRNB1(1140), CHRNB2(1141), CHRNB3(1142), CHRNB4(1143), GRIA3(2892), GRIA4(2893), GRIK1(2897), GRIK2(2898), GRIK3(2899), GRIK4(2900), GRIK5(2901), GUCA2A(2980), GUCA2B(2981), NGFR(4804), SLC23A2(9962)
rat ... Gria1(50592), Grik1(29559), Grin2a(24409)
SML1461 Kyotorphin acetate salt ≥98% (HPLC) Kyotorphin is a neuroactive dipeptide (Tyr-Arg) shown to have analgesic, neuroprotective, and neuromodulatory properties. It is synthesized in nerve terminals and found in the brain and in cerebro-spinal fluid (CSF). Kyotorphin indirectly stimulates opioid receptors by releasing methionine enkephalin (met-enkephalin). CSF levels are lower in patients with persistent pain and in patients with Alzheimer’s disease.
SML0208 KYP-2047 ≥95% (HPLC) KYP-2047 clears the α-synuclein aggregates induced by oxidative stress in the neuronal cells. α-synuclein is the main component of Lewy bodies in Parkinson′s disease that cause neuronal cell death and dementia.
KYP-2047 is a very potent, selective inhibitor of Prolyl oligopeptidase (POP), also known as prolyl endopeptidase (PEP or PE). Ki = .023nM (porcine). KYP-2047 has been found to be neuroprotective against glutamate and oxygen, glucose deprivation in vitro. It has also been used to inhibit the formation of AcSDKP from its precursor 43-mer thymosin β4 (Tβ4). Ac-SDKP is involved in hemopoietic stem cell differentiation, is pro-angiogenic and antifibrogenic.
PZ0245   PF-05105679 ≥98% (HPLC) PF-05105679 is an antagonist of the TRP (transient receptor potential) channel, also known as the cold and menthol receptor 1 (CMR1), with an IC50 value of 103 nM. PF-05105679 is in clinical trials for neuropathic pain. Participants taking PF-05105679 could hold their hands in a bucket of ice water for a long time before feeling pain, and pain-alleviating effects matched those of oxycodone for about one hour after administration.
PF-05105679 is an antagonist of the TRP (transient receptor potential) channel, also known as the cold and menthol receptor 1 (CMR1), with an IC50 value of 103 nM. PF-05105679 is in clinical trials for neuropathic pain. Participants taking PF-05105679 could hold their hands in a bucket of ice water for a long time before feeling pain, and pain-alleviating effects matched those of oxycodone for about one hour after administration.
Transient receptor potential cation channel subfamily M member 8 (TRPM8) antagonist, PF-05105679 [(R)-3-[(1-(4-fluorophenyl)ethyl)(quinolin-3-ylcarbonyl)amino]methylbenzoic acid] acts as a clinical tool to assess the function of TRPM8 in modulating the body temperature. It also helps to determine its role in the treatment of pain in humans.
PZ0242   PF-06658607 ≥98% (HPLC) PF-06658607 is an alkynylated irreversible Brutons tyrosine kinase (BTK) inhibitor that covalently reacts with active-site cysteine residues in the ATP binding pocket. PF-06658607 has been used as a probe for proteomic analysis to identify off-target binding substrates. The alkyne moiety allows for addition of an azide-based detection probe via copper-catalyzed click chemistry methods.
PZ0243 PF-06672131 ≥95% (HPLC) PF-06672131 is a selective EGFR kinase inhibitor thought to covalently react with active-site cysteine residues in the ATP binding pocket. PF-06672131 has been used as a probe for proteomic analysis to identify off-target binding substrates. The dimethylaminomethyl (DMAM) group appears to increase compound stability in cancer cells with a resultant increase in protein reactivity from selective EGFR binding to widespread proteome-wide reactivity after treatment.
SML2528 K-TMZ ≥98% (HPLC) K-TMZ is a more potent, more brain-penetrable, less toxic analog of temozolomide (TMZ). It showed superior activity to TMZ in a mouse model of glioblastoma with significantly less myelotoxicity.