New Products

PI3K/Akt/mTOR
Catalog No. Product Name Information Added
S8456 VPS34 inhibitor 1 (Compound 19, PIK-III analogue) VPS34 inhibitor 1 (Compound 19, PIK-III analogue) is a potent and selective inhibitor of VPS34 with an IC50 of 15 nM. Feb 22 2017
S8339 Miransertib (ARQ 092) ARQ 092 is a novel, orally bioavailable and selective AKT pathway inhibitor exhibiting a manageable safety profile among patients with advanced solid tumors. Feb 09 2017
S7937 GSK2269557 Nemiralisib, also known as GSK-2269557, is a potent and selective PI3Kδ inhibitor(pKi = 9.9). Jan 24 2017
S7865 740 Y-P (PDGFR 740Y-P) 740 Y-P is cell-permeable phosphopeptide activator of PI3K. Jan 16 2017
S8163 GDC-0084 GDC-0084 is a brain penetrant inhibitor of PI3K and mTOR. Jan 09 2017
S8298 CZ415 CZ415, a potent ATP-competitive mTOR inhibitor with very good cell permeability. Jan 09 2017
S8132 Deguelin Deguelin, a natural product isolated from plants in the Mundulea sericea family, is an PI3K/AKT Inhibitor. Nov 21 2016
S7966 AZD8835 AZD8835 ia a novel mixed inhibitor of PI3Kα and PI3Kδ with IC50 of 6.2 nM and 5.7 nM, respectively, also with selectivity against PI3Kβ (IC50=431 nM) and PI3Kγ (IC50=90 nM). Nov 03 2016
S8322 LY3023414 LY3023414 is an oral ATP competitive inhibitor of the class I PI3K isoforms, mTOR and DNA-PK. Sep 21 2016
S7938 GSK2292767 GSK2292767 is a potent and selective PI3Kδ inhibitor. Aug 17 2016
JAK/STAT
Catalog No. Product Name Information Added
S7923 SH5-07 (SH-5-07) SH5-07 is a robust hydroxamic acid-based STAT3 inhibitor, which induce antitumor cell effects in vitro and antitumor response in vivo against human glioma and breast cancer models. Mar 02 2017
S7769 BP-1-102 BP-1-102 is a potent, orally bioavailable and selective STAT3 inhibitor, binds Stat3 with an affinity Kd of 504 nM and blocks Stat3-phospho-tyrosine (pTyr) peptide interactions and Stat3 activation at 4-6.8 μM. Feb 22 2017
S7144 BMS-911543 BMS-911543 is a potent and selective inhibitor of JAK2 with IC50 of 1.1 nM, ~350-, 75- and 65-fold selective to JAK1, JAK3 and TYK2, respectively. Phase 1/2. Nov 21 2016
S8197 APTSTAT3-9R APTSTAT3-9R is a specific STAT3-binding peptide with addition of a cell-penetrating motif. The treatment of APTSTAT3-9R in various types of cancer cells blocks STAT3 phosphorylation and reduces expression of STAT targets. Aug 05 2016
S8195 Oclacitinib Oclacitinib is a novel inhibitor of JAK family members with IC50 ranging from 10 to 99 nM and JAK1-dependent cytokines with IC50 ranging from 36 to 249 nM, which did not inhibit a panel of 38 non-JAK kinases. Jun 12 2016
S7951 STA-21 STA-21 is a selective STAT3 inhibitor. Apr 20 2016
S7541 Decernotinib (VX-509) Decernotinib (VX-509) is a potent and selective JAK3 inhibitor with Ki of 2.5 nM, >4-fold selectivity over JAK1, JAK2, and TYK2, respectively. Phase 2/3. Feb 02 2016
S7650 Peficitinib (ASP015K, JNJ-54781532) Peficitinib (ASP015K, JNJ-54781532) is an orally bioavailable JAK inhibitor. Phase 3. Dec 16 2015
S7977 Napabucasin Napabucasin is an orally available Stat3 and cancer cell stemness inhibitor. Nov 30 2015
S7259 FLLL32 FLLL32 is a potent JAK2/STAT3 inhibitor with IC50 of <5 μM. Sep 14 2015
Cell Cycle
Catalog No. Product Name Information Added
S4743 Wogonin Wogonin, a natural and biologically-active flavonoid found in plants, is an inhibitor of CDK9 and does not inhibit CDK2, CDK4 and CDK6 at doses that inhibit CDK9 activity; Also inhibitsN-acetyltransferase. Mar 02 2017
S7740 SAR-020106 SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC50 of 13.3 nM. Feb 22 2017
S7549 THZ1 THZ1 is a covalent CDK7 inhibitor which has the unprecedented ability to target a remote cysteine residue located outside of the canonical kinase domain, providing an unanticipated means of achieving selectivity for CDK7. Jan 24 2017
S8448 ZINC00881524 (ROCK inhibitor) ZINC00881524 is a ROCK inhibitor. Jan 19 2017
S7935 Y-39983 HCl Y-39983 is a selective rho-associated protein kinase(ROCK) inhibitor with an IC50 of 3.6 nM. Jan 16 2017
S8226 Netarsudil (AR-13324) Netarsudil (a.k.a. AR-13324) is ROCK inhibitor with Ki value of 0.2-10.3 nM. It is currently in clinical trials for the treatment of glaucoma and ocular hypertension. Dec 29 2016
S7687 GSK269962 GSK269962 is a selective ROCK(Rho-associated protein kinase) inhibitor with IC50 values of 1.6 and 4 nM for ROCK1 and ROCK2, respectively. Dec 08 2016
S8246 RK-33 RK-33 is a first-in-class small molecule inhibitor of DDX3 (a RNA helicase) and causes G1 cell cycle arrest, induces apoptosis, and promotes radiation sensitization in DDX3-overexpressing cells. Nov 03 2016
S8303 Kobe0065 Kobe0065 is H-Ras-cRaf1 interaction inhibitor, exhibiting potent activity to competitively inhibit the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki value of 46 ± 13 μM. Sep 07 2016
S8148 PD0166285 PD0166285 is a potent Wee1 and Chk1 inhibitor with activity at nanomolar concentrations.PD0166285 is a novel G2 checkpoint abrogator. Jul 05 2016
DNA Damage
Catalog No. Product Name Information Added
S8270 SRT2183 SRT2183 is a small-molecule activator of the sirtuin subtype SIRT1, currently being developed by Sirtris Pharmaceuticals. Jan 24 2017
S4737 Psoralen Psoralen is a naturally occurring furocoumarin that intercalates with DNA, inhibiting DNA synthesis and cell division. Jan 24 2017
S8328 CeMMEC1 CeMMEC1 is an N-methylisoquinolinone derivative that inhibits the second bromodomain of TAF1 (IC50=0.9 μM). Jan 19 2017
S7891 CC-115 CC-115 is a dual inhibitor of DNA-dependent protein kinase (DNA-PK) and mammalian target of rapamycin (mTOR), with potential antineoplastic activity. Jan 09 2017
S8376 Rbin-1 Rbin-1(ribozinoindole-1) is a potent chemical inhibitor of eukaryotic ribosome assembly. It inhibits recombinant full-length Mdn1's ATPase activity in vitro. Dec 29 2016
S8370 BGP-15 BGP-15, is a nicotinic amidoxime derivative with PARP inhibitory activity. It has been demonstrated that BGP-15 protects against ischemia-reperfusion injury. Dec 29 2016
S2741 MK-4827 (Niraparib) MK-4827 is a selective inhibitor of PARP1/2 with IC50 of 3.8 nM/2.1 nM, with great activity in cancer cells with mutant BRCA-1 and BRCA-2. It is >330-fold selective against PARP3, V-PARP and Tank1. Phase 3. Dec 08 2016
S8375 AZD0156 AZD0156 is a potent and selective inhibitors of ATM kinase, with potential chemo-/radio-sensitizing and antineoplastic activities. Nov 21 2016
S4710 Picolinamide Picolinamide is found to be a strong inhibitor of poly (ADP-ribose) synthetase of nuclei from rat pancreatic islet cells. Nov 21 2016
S8118 RHPS4 RHPS4 is a potent inhibitor of Telomerase at submicromolar. Nov 03 2016
TGF-beta/smad
Catalog No. Product Name Information Added
S7959 SIS3 SIS3, a novel specific inhibitor of Smad3, inhibits TGF-β and activin signaling by suppressing Smad3 phosphorylation without affecting the MAPK/p38, ERK, or PI3-kinase signaling pathways. Oct 20 2016
S7663 LY333531 LY333531 is a β-specific protein kinase C inhibitor. It competitively and reversibly inhibits PKCβ1 and PKCβ2 with IC50 values of 4.7 and 5.9 nM respectively. Oct 10 2016
S7627 LDN-214117 LDN-214117 is a potent and selective BMP type I receptor kinase ALK2 inhibitor with IC50 of 24 nM. Apr 30 2015
S7624 SD-208 SD-208 is a selective TGF-βRI (ALK5) inhibitor with IC50 of 48 nM, >100-fold selectivity over TGF-βRII. Feb 02 2015
S7658 Kartogenin Kartogenin is an activator of the smad4/smad5 pathway, and promotes the selective differentiation of multipotent mesenchymal stem cells into chondrocytes. Nov 27 2014
S7530 EW-7197 EW-7197 is a highly potent, selective, and orally bioavailable TGF-β receptor ALK4/ALK5 inhibitor with IC50 of 13 nM and 11 nM, respectively. Phase 1. Nov 27 2014
S7119 Go6976 Go6976 is a potent PKC inhibitor with IC50 of 7.9 nM, 2.3 nM, and 6.2 nM for PKC (Rat brain), PKCα, and PKCβ1, respectively. Also a potent inhibitor of JAK2 and Flt3. Sep 15 2014
S1421 Staurosporine Staurosporine is a potent PKC inhibitor for PKCα, PKCγ and PKCη with IC50 of 2 nM, 5 nM and 4 nM, less potent to PKCδ (20 nM), PKCε (73 nM) and little active to PKCζ (1086 nM) in cell-free assays. Also shows inhibitory activities on other kinases, such as PKA, PKG, S6K, CaMKII, etc. Phase 3. Aug 13 2014
S7146 DMH1 DMH1 is a selective BMP receptor inhibitor with IC50 of 107.9 nM for ALK2, exhibiting no inhibition on AMPK, ALK5, KDR (VEGFR-2) or PDGFR. May 20 2014
S7147 LDN-212854 LDN-212854 is a potent and selective BMP receptor inhibitor with IC50 of 1.3 nM for ALK2, about 2-, 66-, 1641-, and 7135-fold selectivity over ALK1, ALK3, ALK4, and ALK5, respectively. May 20 2014
GPCR & G Protein
Catalog No. Product Name Information Added
S2879 AMD3465 AMD3465 is a monomacrocyclic CXCR4 antagonist with IC50 of 0.75 nM. Mar 22 2017
S8414 PACAP 1-27 Pituitary adenylate cyclase activating polypeptide (PACAP 1-27) is a potent PACAP receptor antagonist. Feb 22 2017
S8345 ONO-7300243 ONO-7300243 is a novel, potent LPA1(Lysophosphatidic Acid Receptor) antagonist with an IC50 of 160 nM. Dec 08 2016
S8324 ZK756326 ZK756326 is a full agonist of CCR8(Chemokine receptor 8) with an IC50 of 1.8 μM, dose-responsively eliciting an increase in intracellular calcium and cross-desensitizing the response of the receptor to CCL1. Nov 21 2016
S8309 ATI-2341 ATI-2341, pepducin targeting the C-X-C chemokine receptor type 4 (CXCR4), is an allosteric agonist activating the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization. Nov 03 2016
S8283 SQ22536 SQ22536 is an inhibitor of adenylyl cyclase with an IC50 of 1.4 μM. It can inhibit PGE1-stimulated increases in cAMP levels in intact human platelets. Oct 10 2016
S4679 Terazosin Terazosin is a selective alpha-1 antagonist used for treatment of symptoms of an enlarged prostate (BPH). It works by blocking the action of adrenaline on smooth muscle of the bladder and the blood vessel walls. Sep 20 2016
S8314 5-Iodotubercidin 5-Iodotubercidin is a potent adenosine kinase inhibitor with IC50 of 26 nM. It inhibits nucleoside transporter, CK1, insulin receptor tyrosine kinase, phosphorylase kinase, PKA, CK2 and PKC. Sep 08 2016
S4649 Atipamezole hydrochloride Atipamezole is a synthetic α2 adrenergic receptor antagonist. It has also been researched in humans as a potential anti-Parkinsonian drug. Atipamezole hydrochloride is hydrochloride form of atipamezole. Sep 08 2016
S4650 Atipamezole Atipamezole is a synthetic α2 adrenergic receptor antagonist. It has also been researched in humans as a potential anti-Parkinsonian drug. Sep 08 2016
PTK
Catalog No. Product Name Information Added
S8404 S49076 S49076 is a novel, potent inhibitor of MET, AXL/MER, and FGFR1/2/3 with IC50 values below 20 nmol/L. Feb 09 2017
S4736 Trapidil Trapidil is a PDGF antagonist that can inhibit the proliferation of the PDGF-producing glioma cells. Jan 19 2017
S8272 XMD8-87 XMD8-87 is a novel tyrosine kinase nonreceptor 2(TNK2) inhibitor with IC50s of 38 nmol/L and 113 nmol/L for the D163E and R806Q mutations. Jan 16 2017
S8273 XMD16-5 XMD16-5 is a novel tyrosine kinase nonreceptor 2(TNK2) inhibitor with IC50s of 16 nmol/L and 77 nmol/L for the D163E and R806Q mutations. Jan 16 2017
S7014 LY2801653 (Merestinib) LY2801653 is a type-II ATP competitive, slow-off inhibitor of MET tyrosine kinase with a dissociation constant (Ki) of 2 nM, a pharmacodynamic residence time (Koff) of 0.00132 min(-1) and t1/2 of 525 min. Jan 09 2017
S8362 ARRY-380 (ONT-380, Irbinitinib) ARRY-380 (ONT-380) is an orally bioavailable inhibitor of the human epidermal growth factor receptor tyrosine kinase ErbB-2 (also called HER2) with potential antineoplastic activity. Dec 29 2016
S8228 NT157 NT157, a selective inhibitor of IRS-1/2(insulin receptor substrate), has the potential to inhibit IGF-1R and STAT3 signaling pathways in cancer cells and stroma cells of TME leading to a decrease in cancer cell survival. Dec 15 2016
S8189 BAW2881 (NVP-BAW2881) BAW2881 (NVP-BAW2881) is a novel vascular endothelial growth factor (VEGF) receptor tyrosine-kinase inhibitor that potently inhibits VEGFR1-3 at 1.0-4.3 nanomolar (nM) concentrations and inhibits PDGFRβ, c-Kit, and RET at 45-72 nM concentrations. Dec 01 2016
S7960 LOXO-101 LOXO-101 is an oral potent and selective ATP-competitive inhibitor of tropomyosin receptor kinases (TRK). Nov 03 2016
S8242 EAI045 EAI045 is an allosteric inhibitor that targets selected drug-resistant EGFR mutants but spares the wild-type receptor. Oct 26 2016
Epigenetics
Catalog No. Product Name Information Added
S7816 MI-463 MI-463 is a potent inhibitor of Menin-MLL interaction with an IC50 value of 15.3 nM. Mar 02 2017
S7820 EPZ020411 EPZ020411 is a potent and selective small molecule PRMT6 inhibitor with an IC50 of 10 nM. Feb 09 2017
S8071 UNC0638 UNC0638 is a potent, selective and cell-penetrant chemical probe for G9a and GLP with IC50 of <15 nM and 19 nM, respectively, shows selectivity over a wide range of epigenetic and non-epigenetic targets. Jan 24 2017
S8147 MS049 MS049 is a potent and selective inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively. Jan 19 2017
S8359 UNC3866 UNC3866 is a potent antagonist of the methyllysine (Kme) reading function of the Polycomb CBX and CDY families of chromodomains. UNC3866 binds the chromodomains of CBX4 and CBX7 most potently, with a K(d) of ∼100 nM for each, and is 6- to 18-fold selective as compared to seven other CBX and CDY chromodomains. Jan 09 2017
S8287 CPI-455 CPI-455 is a specific KDM5 inhibitor, elevating global levels of H3K4 trimethylation (H3K4me3) and decreased the number of DTPs in multiple cancer cell line models treated with standard chemotherapy or targeted agents. Dec 29 2016
S8353 CPI-1205 CPI-1205 is an orally available selective inhibitor of the histone lysine methyltransferase EZH2, with potential antineoplastic activity. Dec 08 2016
S8190 CPI-637 CPI-637 is a selective and cell-active benzodiazepinone CBP/EP300 bromodomain inhibitor. Dec 01 2016
S7853 CPI-0610 CPI-0610 is a potent and selective benzoisoxazoloazepine BET bromodomain inhibitor and currently undergoing human clinical trials for hematological malignancies. Dec 01 2016
S7833 OICR-9429 OICR-9429 is a potent antagonist of the interaction of WDR5 with peptide regions of MLL and Histone 3 and reduces viability of acute myeloid leukemia cells in vitro. Dec 01 2016
NF-κB
Catalog No. Product Name Information Added
S8261 GSK583 GSK583 is a highly potent and selective inhibitor of RIP2 kinase with an IC50 of 5 nM. Feb 09 2017
S4712 Diethylmaleate Diethylmaleate is the diethyl ester of maleic acid and a glutathione-depleting compound that inhibits NFkB. Oct 26 2016
S7948 MRT67307 MRT67307 is a potent and dual IKKϵ and TBK1 inhibitor with IC50 of 160 and 19 nM, respectively. Apr 25 2016
S7691 PS-1145 PS-1145 is a specific IKK inhibitor with IC50 of 88 nM. Mar 09 2016
S7851 AZD3264 AZD3264 is a novel IKK2 inhibitor. Nov 27 2015
S7672 Omaveloxolone (RTA-408) Omaveloxolone (RTA-408) is a synthetic triterpenoid that activates the cytoprotective transcription factor Nrf2 and inhibits NF-κB signaling. Phase 2. Sep 14 2015
S7697 LY2409881 LY2409881 is a potent and selective IKK2 inhibitor with IC50 of 30 nM, >10-fold selectivity over IKK1 and other common kinases. Apr 20 2015
S7441 WS3 WS3 is a β cell proliferation inducer via modulation of Erb3 binding protein-1 (EBP1) and the IκB kinase pathway. Dec 04 2014
S7442 WS6 WS6 is a β cell proliferation inducer via modulation of Erb3 binding protein-1 (EBP1) and the IκB kinase pathway. Nov 12 2014
S7273 SC75741 SC75741 is a potent NF-κB inhibitor with EC50 of 200 nM. Jun 30 2014
Metabolism
Catalog No. Product Name Information Added
S8405 RRx-001 RRx-001 is a novel epigenetic modulator with potential radiosensitizing activity. It inhibits glucose 6-phosphate dehydrogenase(G6PD) in human tumor cells, binds hemoglobin and drives RBC-mediated redox reactions under hypoxia. Mar 02 2017
S7456 LCI699 LCI699(Osilodrostat) is a potent inhibitor of 11β-hydroxylase, an enzyme catalyzing the final step of cortisol synthesis. Feb 09 2017
S8459 TAK-063 TAK-063 is a novel and selective phosphodiesterase 10A(PDE10A) inhibitor with an IC50 of 0.30 nM. Feb 09 2017
S4741 Danshensu Danshensu, a herbal preparation used in traditional Chinese medicine, possesses potential antitumor and anti‑angiogenesis effects. Feb 09 2017
S8244 Etomoxir (Na salt) Etomoxir is an irreversible inhibitor of carnitine palmitoyltransferase-1 (CPT-1) on the outer face of the inner mitochondrial membrane. Jan 09 2017
S8382 ML390 ML390 is a human DHODH inhibitor that induces differentiation in acute myeloid leukemia. Dec 01 2016
S7466 GGTI 298 GGTI 298 is a geranylgeranyltransferase I inhibitor with ability to arrest human tumor cells in the G1 phase of the cell cycle and induce apoptosis. Dec 01 2016
S4699 Etretinate Etretinate is an oral aromatic retinoid acid which is effective in psoriasis and other dermatological syndromes. It activates retinoid receptors, causing an induction of cell differentiation, inhibition of cell proliferation, and inhibition of tissue infiltration by inflammatory cells. Nov 03 2016
S4725 Benzenesulfonamide Benzenesulfonamide ia an inhibitor of carbonic anhydrases. Nov 03 2016
S4717 Isatin Isatin is an endogenous MAO inhibitor. Oct 26 2016
Proteases
Catalog No. Product Name Information Added
S8457 UK-371804 HCl UK-371804 is a potent and selective urokinase-type plasmogen activator (uPA) inhibitor with excellent enzyme potency (Ki=10 nM) and selectivity profile (4000-fold versus tPA and 2700-fold versus plasmin). Mar 02 2017
S7420 CA-074 methyl ester (CA-074 Me) CA-074 Me is a membrane-permeable derivative of CA-074 and acts as an irreversible cathepsin B inhibitor. Jan 09 2017
S4697 Saxagliptin hydrate Saxagliptin H2O is a selective and reversible DPP4 inhibitor with IC50 of 26 nM. Sep 21 2016
S4636 Teneligliptin hydrobromide Teneligliptin is a novel, potent, and long-lasting dipeptidyl peptidase-4 inhibitor; competitively inhibited human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50 values of approximately 1 nM. Sep 21 2016
S4662 Atazanavir Atazanavir is an azapeptide and HIV-protease inhibitor that is used in the treatment of HIV infections and AIDS in combination with other anti-HIV agents. Sep 21 2016
S4666 Sivelestat sodium Sivelestat sodium is a competitive inhibitor of human neutrophil elastase, also inhibits leukocyte elastase obtained from rabbit, rat, hamster and mouse. Sep 20 2016
S4571 Hexylresorcinol Hexylresorcinol is an organic compound with local anaesthetic, antiseptic and anthelmintic properties, is a potent inhibitor of mushroom tyrosinase. The IC50 values of hexylresorcinol for monophenolase is 1.24 μM and for diphenolase is 0.85 μM. Aug 17 2016
S8136 Sivelestat (ONO-5046) Sivelestat is a potent and selective inhibitor of neutrophil elastase with IC50 of 44nM. It almost shows no activity at a range of other proteases. Aug 05 2016
S7377 Aprotinin Aprotinin is a small protein serine protease inhibitor, used to reduce perioperative blood loss and transfusion. Jun 28 2016
S7038 Epoxomicin Epoxomicin is a selective proteasome inhibitor with anti-inflammatory activity, inhibits primarily the CH-L activity of the 20S proteasome, while T-L and PGPH catalytic activities are also inhibited at 100- and 1000-fold reduced rate. Feb 01 2016
Microbiology
Catalog No. Product Name Information Added
S4678 Povidone iodine Povidone iodine is a stable chemical complex of polyvinylpyrrolidone (povidone, PVP) and elemental iodine. It is used as topical antiseptic in surgery and for skin and mucous membrane infections, also as aerosol. Oct 10 2016
S1395 Polymyxin B sulphate Polymyxin B is an antibiotic primarily used for resistant gram-negative infections. Sep 21 2016
S2315 Kanamycin sulfate Kanamycin sulfate(Kanamycin monosulfate) is an aminoglycoside antibiotic, available in oral, intravenous, and intramuscular forms, and used to treat a wide variety of infections. Sep 21 2016
S4685 Efavirenz Efavirenz is a synthetic non-nucleoside reverse transcriptase (RT) inhibitor with antiviral activity. Sep 21 2016
S4671 Cefradine Cephradine is a semi-synthetic cephalosporin antibiotic. Sep 21 2016
S4663 Fusidate Sodium Fusidate Sodium is a sodium salt form of fusidic acid, a bacteriostatic antibiotic derived from the fungus Fusidium coccineum and used as a topical medication to treat skin infections. Sep 20 2016
S4601 Clioquinol Clioquinol is an orally bioavailable, lipophilic, copper-binding, halogenated 8-hydroxyquinoline with antifungal, antiparasitic and potential antitumor activities. Sep 20 2016
S4550 Azelaic acid Azelaic acid is an organic compound produced by the ozonolysis of oleic acid and possesses antibacterial, keratolytic, comedolytic, and anti-oxidant activity. Sep 20 2016
S4647 Cefmenoxime hydrochloride Cefmenoxime, a potent inhibitor of Enterobacteriaceae, is a cephalosporin antibiotic that is administered intravenously or intramuscularly. Sep 08 2016
S4602 Acetohydroxamic acid Acetohydroxamic acid is an Urease Inhibitor. In the urine, it acts as an antagonist of the bacterial enzyme urease. Sep 08 2016
Apoptosis
Catalog No. Product Name Information Added
S7724 APR-246 (PRIMA-1MET) APR-246, also known as PRIMA-1MET, is a small organic molecule that has been shown to restore tumour-suppressor function primarily to mutant p53 and also to induce cell death in various cancer types. Jan 19 2017
S8403 MX69 MX69 is a MDM2/XIAP inhibitor, used for cancer treatment. Jan 09 2017
S8158 PD-1/PD-L1 Inhibitor 3 PD-1/PD-L1 Inhibitor 3(Programmed Death-1/Programmed Death-Ligand 1 Inhibitor 3)is a Macrocyclic inhibitor of PD-1/PD-L1 interaction with IC50 of 5.6 nM Dec 29 2016
S7875 NVP-CGM097 NVP-CGM097 is a highly potent and selective MDM2 inhibitor. It binds to the p53 binding-site of the Mdm2 protein, disrupting the interaction between both proteins, leading to an activation of the p53 pathway. Dec 08 2016
S7849 BDA-366 BDA-366 is a small-molecule Bcl2-BH4 domain antagonist and binds BH4 with high affinity and selectivity. Dec 01 2016
S7801 A-1331852 A-1331852 is a potent and selectiveBCL-XL inhibitor and may be useful in the treatment of cancer, immune and autoimmune diseases. Oct 26 2016
S7800 A-1155463 A-1155463, a highly potent and selective BCL-XL inhibitor, shows picomolar binding affinity to BCL-XL, and >1000-fold weaker binding to BCL-2 and related proteins BCL-W(Ki=19 nM) and MCL-1(Ki>440 nM). Oct 20 2016
S7723 PRIMA-1 PRIMA-1 is a mutant p53 reactivator. It induces apoptosis and inhibits growth of human tumors with mutant p53. Oct 10 2016
S7314 Z-IETD-FMK Z-IETD-FMK is a specific Caspase-8 inhibitor. Sep 21 2016
S7312 Z-DEVD-FMK Z-DEVD-FMK is a specific, irreversible Caspase-3 inhibitor, and also shows potent inhibition on caspase-6, caspase-7, caspase-8, and caspase-10. Sep 21 2016
MAPK
Catalog No. Product Name Information Added
S7743 CCT196969 CCT196969 is a novel orally available, pan-RAF inhibitor with anti-SRC activity. It also inhibits SRC, LCK, and the p38 MAPKs. Mar 02 2017
S8275 eFT-508 (eFT508) eFT-508 (eFT508) is a potent and selective MNK1/2 inhibitor with IC50s of 2.4 nM and 1 nM, respectively. It potentially results in decreased tumor cell proliferation and tumor growth. Mar 02 2017
S8125 Pamapimod (R-1503, Ro4402257) Pamapimod (R-1503, Ro4402257) is a novel, selective inhibitor of p38 mitogen-activated protein kinase. It inhibits p38α and p38β enzymatic activity with IC50 values of 0.014±0.002 and 0.48± 0.04 microM, respectively with no activity against p38delta or p38gamma isoforms. Dec 01 2016
S8355 APS-2-79 APS-2-79 is a MAPK antagonist that modulating KSR-dependent MAPK signalling by antagonizing RAF heterodimerization as well as the conformational changes required for phosphorylation and activation of KSR-bound MEK. Nov 21 2016
S8201 BI-78D3 BI-78D3 is a competitive JNK inhibitor with IC50 of 280nM that displays > 100 fold selectivity over p38α and no activity at mTOR and PI-3K. Aug 05 2016
S7964 PLX7904 PLX7904, also known as PB04, is a potent and selective paradox-breaker RAF inhibitor. It is able to efficiently inhibit activation of ERK1/2 in mutant BRAF melanoma cells but does not hyperactivate ERK1/2 in mutant RAS-expressing cells. Jul 14 2016
S7752 SC1 Pluripotin (SC1) is a dual inhibitor of extracellular signal-regulated kinase 1 (ERK1, MAPK3) and RasGAP. Maintains embryonic stem cell (ESC) self-renewal. Jul 14 2016
S8124 BMS-582949 BMS-582949 is a potent and selective p38 mitogen-activated protein kinase (p38 MAPK) inhibitor with IC50 of 13nM,inhibiting both p38 kinase activity and activation of p38. Jul 05 2016
S7121 MLN2480 MLN2480 is an oral, selective pan-Raf kinase inhibitor in chinical trials. Jun 13 2016
S7544 Vacquinol-1 Vacquinol-1 is an MKK4 activator, which rapidly and selectively induces glioma cell death. Apr 29 2016
Angiogenesis
Catalog No. Product Name Information Added
S7940 NSC12 NSC12 is an orally available pan-FGF trap able to inhibit FGF2/FGFR interaction and endowed with promising antitumor activity. Jan 24 2017
S8401 JNJ-42756493 (Erdafitinib) JNJ-42756493 (Erdafitinib) is a potent and selective orally bioavailable, pan fibroblast growth factor receptor (FGFR) inhibitor with potential antineoplastic activity. Jan 16 2017
S7286 RO9021 RO9021 potently inhibits SYK kinase activity with an average IC50 of 5.6 nM and suppresses B-cell receptor signaling. Dec 29 2016
S8188 BFH772 BFH772 is a novel potent oral VEGFR2 inhibitor, targeting VEGFR2 kinase with IC50 of 3 nM. Dec 08 2016
S8312 NSC228155 NSC228155 is an activator of EGFR, binding to the sEGFR dimerization domain II and modulate EGFR tyrosine phosphorylation. Nov 21 2016
S7006 BAY-61-3606 BAY-61-3606 is a potent and selective inhibitor of Syk kinase (Ki = 7.5 nM). Nov 03 2016
S1717 Fomepizole Fomepizole is a competitive inhibitor of alcohol dehydrogenase, the enzyme that catalyzes the initial steps in the metabolism of ethylene glycol and methanol to their toxic metabolites. Sep 08 2016
S7939 Chetomin Chetomin is an inhibitor of HIF-1 by weaken transcription of HIF-1,disrupting the binding of HIF-1α and HIF-2α to p300 at low nanomolar concentrations. Jul 05 2016
S7738 PRT-060318 PRT-060318 (PRT318) is a novel selective inhibitor of the Syk tyrosine kinase, as an approach to HIT treatment. Jun 30 2016
S8116 ACP-196 Acalabrutinib(ACP-196) is a selective second-generation Bruton's tyrosine kinase (BTK) inhibitor, which prevents the activation of the B-cell antigen receptor (BCR) signaling pathway. ACP-196 has improved target specificity over ibrutinib with 323-, 94-, 19- and 9-fold selectivity over the other TEC kinase family members (ITK, TXK, BMX, and TEC, respectively) and no activity against EGFR. Jun 12 2016
Stem Cell & Wnt
Catalog No. Product Name Information Added
S8429 PNU-74654 PNU-75654 disrupts the Wnt signaling pathway via inhibition of the interaction (KD50=450 nM) between β-catenin and Tcf4. Mar 02 2017
S7169 LY3039478 LY3039478 is a novel and orally bioavailable inhibitor of Notch-1 intracellular domain (N1ICD) cleavage with IC50 of ~1 nM. Phase 1. Feb 10 2017
S4747 Jervine Jervine is an inhibitor of Hedgehog signaling (IC50=500-700 nM) that inhibits the sonic hedgehog (shh) pathway by interacting with smoothened. Jan 24 2017
S8129 Salinomycin (from Streptomyces albus) Salinomycin, traditionally used as an anti-coccidial drug, has recently been shown to possess anti-cancer and anti-cancer stem cell (CSC) effects. Jan 24 2017
S8334 XMU-MP-1 XMU-MP-1 is an inhibitor of MST1/2 with IC50 values of 71.1±12.9 nM and 38.1±6.9 nM against MST1 and MST2, respectively. Jan 16 2017
S8249 HPI-4 (Ciliobrevin A) HPI-4 (Ciliobrevin A) is a hedgehog (Hh) pathway antagonist. It blocks Sonic hedgehog (Shh)-induced Hh pathway activation (IC50 = 7 μM) downstream of Smo. Dec 29 2016
S8320 SKL2001 SKL2001 is a novel agonist of the Wnt/β-catenin pathway that disrupts the Axin/β-catenin interaction. Dec 01 2016
S8327 KYA1797K KYA1797K is a highly potent and selective Wnt/β-catenin inhibitor with IC50 of 0.75 µM (TOPflash assay). Nov 03 2016
S8200 MK-4101 MK-4101, a potent inhibitor of the Hedgehog pathway, shows anti-tumor activity through the inhibition of proliferation and induction of extensive apoptosis in tumor cells. Oct 20 2016
S8280 IMR-1 IMR-1 is a novel class of Notch inhibitors targeting the transcriptional activation with IC50 of 6 μmol/L. Sep 08 2016
Ubiquitin
Catalog No. Product Name Information Added
S4920 b-AP15 b-AP15 is a deubiquitinases inhibitor for 19S proteasomes activity of Ub-AMC cleavage with IC50 of 2.1 μM. Mar 30 2015
S7529 ML323 ML323 displays reversible, nanomolar inhibitory activity and excellent selectivity toward USP1/UAF1 with IC50 of 76 nM. Jun 30 2014
S7142 NSC697923 NSC697923 is a cell-permeable and selective inhibitor of the Ub-conjugating enzyme (E2) complex Ubc13-Uev1A. Apr 09 2014
S7285 NMS-873 NMS-873 is an allosteric and specific p97 inhibitor with IC50 of 30 nM that demonstrates potent selectivity for VCP/p97 compared to a panel of other AAA ATPases, Hsp90, and 53 additional analyzed kinases (IC50s >10 μM). Jan 29 2014
S7199 DBeQ DBeQ is a selective, potent, reversible, and ATP-competitive p97 inhibitor with IC50 of 1.5 μM. Jul 19 2013
S4921 MNS (3,4-Methylenedioxy-β-nitrostyrene, MDBN) MNS is a tyrosine kinase inhibitor, inhibits Syk, Src, p97 with IC50 of 2.5 μM, 29.3 μM and 1.7 μM, respectively. Jul 19 2013
S7129 PYR-41 PYR-41 is the first cell-permeable inhibitor of ubiquitin-activating enzyme E1, with no activity at E2. Jul 19 2013
S7130 PR-619 PR-619 is a non-selective, reversible inhibitor of the deubiquitinylating enzymes (DUBs) with EC50 of 1-20 μM in a cell-free assay. Jul 17 2013
S7132 P5091 (P005091) P5091(P005091) is a selective and potent inhibitor of ubiquitin-specific protease 7 (USP7) with EC50 of 4.2 μM and the closely related USP47. Jul 17 2013
S7133 P22077 P22077 is an inhibitor of ubiquitin-specific protease USP7 with EC50 of 8.6 μM, also inhibits the closely related USP47. Jul 17 2013
Neuronal Signaling
Catalog No. Product Name Information Added
S8193 AZD3293 (LY3314814) AZD3293, also known as LY3314814 is an oral beta-secretase 1 cleaving enzyme (BACE) inhibitor. Jan 24 2017
S8274 STO-609 STO-609 is a specific inhibitor of the Ca2+/Calmodulin-dependent protein kinase kinase(CaM-KK) that inhibits the activities of recombinant CaM-KKα and CaM-KKβ isoforms, with Ki values of 80 and 15 ng/ml, respectively, and also inhibits their autophosphorylation activities. Jan 19 2017
S8433 NS-398 (NS398) NS-398 is a selective inhibitor of cyclooxygenase-2 (COX-2). The IC50 values for human recombinant COX-1 and -2 are 75 and 1.77 μM, respectively. Jan 09 2017
S4729 Tamsulosin hydrochloride Tamsulosin is a potent and selective α1a adrenergic receptor antagonist. Dec 29 2016
S4732 MPTP hydrochloride MPTP hydrochloride is a dopaminergic neurotoxin and cause selective destruction of dopaminergic neurons in animal models of parkinsonism. Dec 01 2016
S4731 Perphenazine Perphenazine is a phenothiazine derivative and a dopamine antagonist with antiemetic and antipsychotic properties. Nov 23 2016
S4631 Prochlorperazine dimaleate salt Prochlorperazine dimaleate is a dopamine (D2) receptor antagonist. Nov 23 2016
S4702 Sarcosine Sarcosine is a competitive inhibitor of the type I glycine transporter (GlyT1) and an N-methyl-D-aspartate receptor (NMDAR) co-agonist. Nov 21 2016
S4700 4-Aminobutyric acid Gamma-Aminobutyric Acid is a naturally occurring neurotransmitter with central nervous system (CNS) inhibitory activity. Nov 21 2016
S4719 Kynurenic acid Kynurenic acid, a natural metabolite of tryptophan via the kynurenine pathway, is a broad-spectrum excitatory amino acid antagonist; It proved to be an antagonist at NMDA, kainate and AMPA receptors. Oct 26 2016
Others
Catalog No. Product Name Information Added
S4742 Rebaudioside C Rebaudioside C belongs to the family of Steviol Glycosides. It is a natural constituent of the plant Stevia rebaudiana Bertoni and used as natural sweeteners to diabetics and others on carbohydrate-controlled diets. Mar 02 2017
S8446 Importazole Importazole is a small molecule inhibitor of the transport receptor importin-β specifically blocking importin-β-mediated nuclear import. Mar 02 2017
S8402 KRIBB11 KRIBB11 abolishes the heat shock-induced luciferase activity with an IC50 of 1.2 μM. It is an inhibitor of the transcription factor Heat Shock Factor 1 (HSF1). Feb 22 2017
S7652 OTS514 OTS514 is a highly potent TOPK(T-LAK cell-originated protein kinase) inhibitor with an IC50 value of 2.6 nM. Feb 22 2017
S8137 Capsazepine Capsazepine acts as a competitive antagonist of capsaicin and a transient receptor potential vanilloid type 1(TRPV1) antagonist. Feb 09 2017
S8337 1400W 1400W is a slow, tight binding, and highly selective inhibitor of inducible nitric-oxide synthase(iNOS). Feb 09 2017
S8270 SRT2183 SRT2183 is a small-molecule activator of the sirtuin subtype SIRT1, currently being developed by Sirtris Pharmaceuticals. Jan 24 2017
S8439 Monastrol Monastrol is a cell-permeable small molecule inhibitor of kinesin-5(KIF11) which is essential for maintaining separation of the half-spindles. Jan 24 2017
S4737 Psoralen Psoralen is a naturally occurring furocoumarin that intercalates with DNA, inhibiting DNA synthesis and cell division. Jan 24 2017
S4738 Arctiin Arctiin acts on an agonists of the adiponectin receptor 1 with anti-cancer effects. Jan 24 2017