New Products

PI3K/Akt/mTOR
Catalog No. Product Name Information Added
S8157 GDC-0326 GDC-0326 is a potent and selective inhibitor of PI3Kα with Ki value of 0.2 nM; remarkably selective over the other class I isoforms in enzymatic assays. Jul 11 2017
S7682 SAR405 SAR405 is a low-molecular-mass kinase inhibitor of Vps34 (KD 1.5 nM) showing high selectivity and not be active up to 10 μM on class I and class II PI3Ks as well as on mTOR. Jun 01 2017
S8194 TGR-1202 TGR-1202, a novel, next generation PI3Kδ inhibitor, inhibits PI3Kδ activity in enzyme and cell based assays with IC50 and EC50 values of 22.2 & 24.3 nM, respectively. Apr 12 2017
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) HCl 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
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
JAK/STAT
Catalog No. Product Name Information Added
S7985 PIM447 (LGH447) PIM447 is a novel pan-PIM kinase inhibitor with Ki values of 6 pM, 18 pM, 9 pM for PIM1, PIM2, PIM3 respectively. It also inhibits GSK3β, PKN1, and PKCτ, but at a significantly lower potency with IC50 between 1 and 5 μM (>105-fold differential relative to the Ki on PIMs). May 05 2017
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 maleate 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
Cell Cycle
Catalog No. Product Name Information Added
S8520 Senexin A Senexin A is a potent and selective inhibitor of CDK8 and its nearest relative, CDK19 with Kd values of 0.83 μM and 0.31 μM for CDK8 and CDK19 ATP site binding, respectively. Jul 11 2017
S7178 Prexasertib (LY2606368) Prexasertib (LY2606368) is an ATP-competitive CHK1 inhibitor with a Ki value of 0.9 nmol/L. For CHK2 and RSK, its IC50 values are 8 nM and 9 nM respectively in cell-free assay. Jun 29 2017
S8156 ARS-853 (ARS853) ARS-853 is a selective, covalent inhibitor of KRAS(G12C) that inhibits mutant KRAS-driven signaling by binding to the GDP-bound oncoprotein and preventing activation. Jun 05 2017
S7552 CFI-400945 CFI-400945 is an orally active, potent and selective polo-like kinase 4(PLK4) inhibitor with Ki value of 0.26 nM. May 05 2017
S8489 GSK180736A (GSK180736) GSK180736A, developed as a Rho-associated, coiled-coil-containing protein kinase inhibitor, binds to GRK2(G protein-coupled receptor kinase 2) with logIC50 pf -6.6 (logIC50 -4.0 for GRK5 and >-3 for GRK1); ≥400-fold selective for GRK2 over both GRK1 and GRK5. Apr 27 2017
S8426 10074-G5 10074-G5 is a c-Myc inhibitor that binds to and distorts the bHLH-ZIP domain of c-Myc (Kd = 2.8 µM), thereby inhibiting c-Myc/Max heterodimer formation and inhibiting its transcriptional activity (IC50 = 146 µM). Apr 21 2017
S7992 LDC4297 (LDC044297) LDC4297 is a novel CDK7 inhibitor (IC50=0.13±0.06 nM for CDK7 versus IC50s between 10 nM and 10,000 nM for all other analyzed CDKs). Mar 31 2017
S8253 CCT245737 CCT245737 is an orally active CHK1 inhibitor with The IC50 of 1.4 nM. It exhibits >1,000-fold selectivity against CHK2 and CDK1. Mar 31 2017
S8208 Hydroxyfasudil (HA-1100) HCl Hydroxyfasudil (HA-1100), an active metabolite of fasudil hydrochloride, is a specific Rho-kinase(ROCK) inhibitor with IC50 values of 0.73 μM and 0.72 μM for ROCK1 and ROCK2, respectively. Mar 31 2017
S7511 LY2857785 LY2857785 is a type I reversible and competitive ATP kinase inhibitor against CDK9(IC50=0.011 μM) and also inhibits other transcription kinases CDK8(IC50=0.016 μM) and CDK7 (IC50=0.246 μM). Mar 30 2017
DNA Damage
Catalog No. Product Name Information Added
S8427 LTURM34 LTURM34 is a specific DNA-PK inhibitor, 170-fold more selective for DNA-PK activity compared to PI3K activity, with IC50 value of 0.034 μM. Jun 13 2017
S8539 TAS-102 TAS-102 is an orally administered combination of a thymidine-based nucleic acid analogue, trifluridine, and a thymidine phosphorylase inhibitor, tipiracil hydrochloride. Jun 01 2017
S8379 YU238259 YU238259 is a novel inhibitor of homology-dependent DNA repair(HDR), but does not inhibit non-homologous end-joining (NHEJ), in cell-based GFP reporter assays. May 10 2017
S8481 SRT3025 HCl SRT3025 is an orally available small molecule activator of the SIRT1 enzyme. Apr 27 2017
S8434 B02 B02 is a small-molecule inhibitor of human RAD51 with an IC50 of 27.4 μM, but does not inhibit its E. coli homologue RecA (IC50 > 250 μM). Apr 21 2017
S8363 NMS-P118 NMS-P118 is a potent, orally available, and highly selective PARP-1 inhibitor endowed with excellent ADME and pharmacokinetic profiles, showing 150-fold selectivity for PARP-1 over PARP-2 (Kd 0.009 μM vs 1.39 μM, respectively). Apr 21 2017
S8245 Thiomyristoyl Thiomyristoyl is a potent and specific SIRT2 inhibitor with an IC50 of 28 nM. It inhibits SIRT1 with an IC50 value of 98 μM and does not inhibit SIRT3 even at 200 μM. Mar 31 2017
S8460 Salermide Salermide is a reverse amide with a strong in vitro inhibitory effect on Sirt1 and Sirt2. Compared with Sirt1, Salermide is even more efficient at inhibiting Sirt2. Mar 31 2017
S8419 E7449 E7449 is an orally bioavailable, brain penetrable, small molecule dual inhibitor of PARP1/2 that also inhibits PARP5a/5b, otherwise known as tankyrase1 and 2 (TNKS1/2), important regulators of canonical Wnt/β-catenin signaling. It has IC50 values of 1.0 and 1.2 nM for PARP1 and 2, respectively. Mar 31 2017
S8270 SRT2183 SRT2183 is a small-molecule activator of the sirtuin subtype SIRT1, currently being developed by Sirtris Pharmaceuticals. Jan 24 2017
TGF-beta/smad
Catalog No. Product Name Information Added
S7959 SIS3 HCl 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 HCl 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
S8517 Lixisenatide Lixisenatide is a once-daily short-acting glucagon-like peptide-1 (GLP-1) receptor agonist (GLP-1RA) with an IC50 of 1.4 nM for the human GLP-1 receptor in receptor binding studies. Jul 11 2017
S8415 PACAP 1-38 PACAP 1-38 is a highly potent PACAP receptor agonist (Kd = 100 pM). It stimulates adenylate cyclase and phagocytosis. Mar 31 2017
S8416 PACAP 6-38 PACAP 6-38 is a PACAP (pituitary adenylate cyclase-activating polypeptide) non-stimulating competitive antagonist with an IC50 value of 2 nM. It also acts as a functional CARTp antagonist in vivo. Mar 31 2017
S7182 JTE 013 JTE 013 is a potent and selective S1P2 antagonist with IC50 of 17.6 nM. Mar 31 2017
S2879 AMD3465 hexahydrobromide 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
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
S8256 Liraglutide Liraglutide is a long-acting glucagon-like peptide-1(GLP-1) receptor agonist. Oct 10 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
PTK
Catalog No. Product Name Information Added
S8570 RXDX-106 (CEP-40783) RXDX-106 (CEP-40783) is an orally-available, potent and selective TAM(TYRO3, AXL, MER)/MET inhibitor displaying low nanomolar biochemical activity and slow (T1/2 >120 min) inhibitor off-rate in peptide phosphorylation assays and in vitro kinase binding assays, respectively. Jul 11 2017
S8518 AD80 AD80, a multikinase inhibitor, shows strong activity against human RET, BRAF, S6K, and SRC but were much less active than either AD57 or AD58 against mTOR. The IC50 value for RET is 4 nM. Jul 03 2017
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 Merestinib (LY2801653) 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 Irbinitinib (ARRY-380, ONT-380) 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
Epigenetics
Catalog No. Product Name Information Added
S8340 SGC2085 SGC2085 is a potent and selective Coactivator Associated Arginine Methyltransferase 1 (CARM1) inhibitor with an IC50 value of 50 nM and >100-fold selective over other PRMTs. Jul 03 2017
S7983 A-196 A-196 is a potent and selective inhibitor of SUV420H1 and SUV420H2 with IC50 values of 0.025 and 0.144 μM, respectively; more than 100-fold selective over other histone methyltransferases and non-epigenetic targets. Jul 03 2017
S8344 AZD5153 AZD5153 is a potent, selective, and orally available BET/BRD4 bromodomain inhibitor with pKi of 8.3 for BRD4. May 10 2017
S8265 GSK6853 GSK6853 is a selective benzimidazolone BRPF1 inhibitor with pIC50 of 8.1(TR-FRET) showing greater than 1600-fold selectivity over all other bromodomains tested. Apr 27 2017
S8496 EED226 EED226 is a potent, selective, and orally bioavailable a novel allosteric Polycomb repressive complex 2 (PRC2) inhibitor with an IC50 of 23.4 nM when the H3K27me0 peptide was used as substrate and an IC50 of 53.5 nM when the mononucleosome was used as the substrate. It directly binds to the H3K27me3 binding pocket of EED. Apr 27 2017
S8464 Citarinostat (ACY-241) Citarinostat (ACY-241) is an orally available selective HDAC6 inhibitor with IC50 of 2.6 nM and 46 nM for HDAC6 and HDAC3, respectively. It has 13 to 18-fold selectivity towards HDAC6 in comparison to HDAC1-3. Mar 31 2017
S7817 MI-503 MI-503 is a potent and selective Menin-MLL inhibitor with IC50 of 14.7 nM. It shows pronounced growth suppressive activity in a panel of human MLL leukemia cell lines(GI50 at 250 nM-570 nM range), but only a minimal effect in human leukemia cell lines without MLL translocations. Mar 31 2017
S8400 Mivebresib(ABBV-075) Mivebresib(ABBV-075) is a novel BET family bromodomain inhibitor. It binds bromodomains of BRD2/4/T with similar affinities (Ki of 1-2.2 nM) and highly selective for 18 bromodomain proteins tested (Kd > 1 μM; more than 600-fold selectivity vs. BRD4), but exhibits roughly 10-fold weaker potency towards BRD3 (Ki of 12.2 nM) and has moderate activity towards CREBBP (Kd = 87 μM; 54-fold selectivity vs. BRD4). Mar 31 2017
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 2HCl EPZ020411 is a potent and selective small molecule PRMT6 inhibitor with an IC50 of 10 nM. Feb 09 2017
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 HCl 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
S8452 BAY-876 BAY-876 is a potent and selective GLUT1 inhibitor (IC50=0.002 μM) with a selectivity factor of >100 against GLUT2, GLUT3, and GLUT4. May 10 2017
S8432 Troglitazone (CS-045) Troglitazone is a potent agonist for the peroxisome proliferator-activated receptor-(PPAR) that is a ligand activated transcription factor regulating cell differentiation and growth. Apr 27 2017
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
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 TFA salt 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
Proteases
Catalog No. Product Name Information Added
S8565 Omarigliptin (MK-3102) Omarigliptin (MK-3102) is a competitive, reversible inhibitor of DPP-4 (IC50 = 1.6 nM, Ki = 0.8 nM). It is highly selective over all proteases tested (IC50 > 67 μM), including QPP, FAP, PEP, DPP8, and DPP9 and has weak ion channel activity (IC50 > 30 μM at IKr, Caγ1.2, and Naγ1.5). Jul 11 2017
S8410 MG-132(R) MG-132(R) is a potent, reversible, and cell permeable proteasome inhibitor with IC50 of 0.22 μM. Apr 12 2017
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 tetrahydrate Sivelestat sodium tetrahydrate 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
Microbiology
Catalog No. Product Name Information Added
S8324 ZK756326 2HCl 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
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
Apoptosis
Catalog No. Product Name Information Added
S7901 Ac-DEVD-CHO Ac-DEVD-CHO is a potent aldehyde inhibitor of Group II caspases with Ki values of 0.2 nM and 0.3 nM for for caspase-3 and caspase-7, respectively. Weak inhibition for caspase-2. Jun 29 2017
S7609 GW4869 GW4869 is a neutral, noncompetitive inhibitor of sphingomyelinase (SMase) with an IC50 of 1 μM. It is selective for N-SMase, and does not inhibit acid SMase at up to at least 150 μM. Jun 21 2017
S7362 AZD5582 AZD5582, a novel small-molecule IAP inhibitor, binds potently to the BIR3 domains of cIAP1, cIAP2, and XIAP with IC50 values of 15, 21, and 15 Jun 13 2017
S8366 CRT0066101 CRT0066101 is a small molecule PKD family specific inhibitor which specifically blocks PKD1/2 activity and does not suppress PKCα/PKCβ/PKCε activity in multiple. Jun 13 2017
S7942 Bioymifi Bioymifi, a small-molecule death receptor 5 (DR5) agonist, binds to the extracellular domain(ECD) of DR5 with a Kd of 1.2 μM but showed little binding affinity to the DR4 ECD. It induces DR5 clustering and aggregation, leading to apoptosis. Apr 12 2017
S8177 BH3I-1 BH3I-1 is a Bcl-XL-BH3 domain interaction inhibitor with Ki of 2.4 μM (by fluorescence polarization ).It is a selective inhibitor of Bcl-2 family proteins. Mar 30 2017
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
MAPK
Catalog No. Product Name Information Added
S8490 Tanzisertib(CC-930) CC-930 is kinetically competitive with ATP in the JNK-dependent phosphorylation of the protein substrate c-Jun and potent against all isoforms of JNK (Ki(JNK1) = 44 ± 3 nM, IC50(JNK1) = 61 nM, Ki(JNK2) = 6.2 ± 0.6 nM, IC50(JNK2) = 5 nM, IC50(JNK3) = 5 nM) and selective against MAP kinases ERK1 and p38a with IC50 of 0.48 and 3.4 μM respectively. Apr 21 2017
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 HCl 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
Angiogenesis
Catalog No. Product Name Information Added
A2000 Cetuximab Cetuximab, a novel molecular-targeted agent,is an inhibitor of EGFR monoclonal humanized antibody interacting with the extracellular binding site of EGFR to block ligand stimulation. MW : 145.781 KD. Jun 02 2017
S8229 Brigatinib (AP26113) Brigatinib (AP26113) is a potent and selective ALK (IC50, 0.6 nM) and ROS1 (IC50, 0.9 nM) inhibitor. It also inhibits ROS1, FLT3, and mutant variants of FLT3 (D835Y) and EGFR with lower potentcy. May 10 2017
S8523 GSK2256098 GSK2256098 is a potent, selective, reversible, and ATP competitive FAK kinase inhibitor with apparent Ki of 0.4 nM. Apr 27 2017
S7824 Nazartinib (EGF816, NVS-816) Nazartinib (EGF816, NVS-816) is a covalent, irreversible, mutant-selective EGFR inhibitor that has nanomolar inhibitory potency against activating mt (L858R, ex19del) and T790M mt, with up to 60-fold selectivity over wild type (wt) EGFR in vitro. Apr 21 2017
S8503 BLU-554 (BLU554) BLU-554 is a potent, highly-selective, oral FGFR4 inhibitor with an IC50 value of 5 nM. The IC50s for FGFR1-3 is 624-2203 nM. Apr 21 2017
S8493 PD-166866 (PD166866) PD-166866 is a synthetic molecule inhibiting the tyrosin kinase action of FGFR1, shows a very high selectivity towards FGFR1 and inhibits the auto-phosphorylation activity of FGRF1. Apr 21 2017
S8192 SUN11602 SUN11602 is a small synthetic compound that mimics the neuroprotective activities of bFGF and activates key molecules in the FGF receptor-1-mitogen-activated protein kinase/extracellular signal-regulated kinase-1/2 kinase (FGFR-1-MEK/ERK) signaling pathway. Apr 12 2017
S8443 MK-8617 MK-8617 is an orally active pan-inhibitor of Hypoxia-inducible factor prolyl hydroxylase 1−3 (HIF PHD1−3), inhibiting PHD1, 2, 3 with IC50s of 1.0, 1.0 and 14 nM, respectively. Apr 12 2017
S7958 Lificiguat(YC-1) YC-1 is an nitric oxide (NO)-independent activator of soluble guanylyl cyclase(sGC) and an inhibitor of Hypoxia-inducible factor-1alpha (HIF-1alpha). Mar 31 2017
S8412 Naquotinib(ASP8273) Naquotinib(ASP8273) is an orally available, irreversible, mutant-selective, epidermal growth factor receptor (EGFR) inhibitor, with potential antineoplastic activity. Mar 31 2017
Stem Cell & Wnt
Catalog No. Product Name Information Added
S8474 LF3 LF3 is a specific inhibitor of canonical Wnt signaling by disrupting the interaction between β-catenin and TCF4 with an IC50 less than 2 μM. Apr 21 2017
S7954 CP21R7 (CP21) CP21R7, also known CP21, is a potent and selective GSK-3β inhibitor that can potently activate canonical Wnt signalling. Mar 31 2017
S8392 NCB-0846 NCB-0846 is a novel, orally small-molecule Wnt inhibitor that inhibits TNIK (TRAF2 and NCK-Interacting Kinase) with an IC50 value of 21 nM. Mar 31 2017
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 an oral Notch inhibitor with an IC50 of 0.41 nM. 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
Ubiquitin
Catalog No. Product Name Information Added
S8288 VLX1570 VLX1570 is a competitive inhibitor of proteasome DUB activity, with an IC50 of ~10 μM in vitro. May 19 2017
S7892 Avadomide(CC-122) Avadomide(CC-122), a new chemical entity termed pleiotropic pathway modifier, is a novel agent for Diffuse large B-cell lymphoma(DLBCL) with antitumor and immunomodulatory activity. Its molecular target is the protein cereblon (CRBN), a substrate receptor of the cullin ring E3 ubiquitin ligase complex CRL4CRBN. Mar 31 2017
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
Neuronal Signaling
Catalog No. Product Name Information Added
S8564 Verubecestat (MK-8931) Verubecestat (MK-8931) is a potent and selective beta-secretase inhibitor and BACE1 protein inhibitor or Beta-site APP-cleaving enzyme 1 inhibitor. Jun 29 2017
S4748 Ondansetron Hydrochloride Dihydrate Ondansetron is a highly specific and selective serotonin 5-HT3 receptor antagonist (Ki=6.16 nM), with low affinity for dopamine receptors. Mar 31 2017
S4749 Citalopram HBr Citalopram HBr, an antidepressant, is an orally administered selective serotonin reuptake inhibitor (SSRI) with IC50 of 1.8 nM. Mar 31 2017
S4751 Cisapride hydrate Cisapride acts directly as a selective serotonin 5-HT4 receptor agonist with IC50 of 0.483 μM. And It also acts indirectly as a parasympathomimetic. Mar 31 2017
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
Others
Catalog No. Product Name Information Added
S8427 LTURM34 LTURM34 is a specific DNA-PK inhibitor, 170-fold more selective for DNA-PK activity compared to PI3K activity, with IC50 value of 0.034 μM. Jun 13 2017
S8539 TAS-102 TAS-102 is an orally administered combination of a thymidine-based nucleic acid analogue, trifluridine, and a thymidine phosphorylase inhibitor, tipiracil hydrochloride. Jun 01 2017
S8397 Eltanexor (KPT-8602) Eltanexor(KPT-8602) is a second-generation, orally bioavailable XPO1 inhibitor with IC50 values of 20−211 nM in 10 AML lines after 3 days exposure. Jun 01 2017
S8278 SHP099 dihydrochloride SHP099 is a highly potent, selective and orally bioavailable small-molecule SHP2 inhibitor with an IC50 value of 0.071 μM and shows no activity against SHP1. May 19 2017
S8367 GSK2193874 GSK2193874 is an orally active, potent, and selective blocker of transient receptor potential vanilloid 4 (TRPV4) with IC50 values of 0.04 and 0.002 μM for hTRPV4 and rTRPV4, respectively. May 10 2017
S8379 YU238259 YU238259 is a novel inhibitor of homology-dependent DNA repair(HDR), but does not inhibit non-homologous end-joining (NHEJ), in cell-based GFP reporter assays. May 10 2017
S8481 SRT3025 HCl SRT3025 is an orally available small molecule activator of the SIRT1 enzyme. Apr 27 2017
S7648 OTS964 OTS964 is a potent TOPK inhibitor with high affinity and selectivity and IC50 value is 28 nM. Apr 21 2017
S8434 B02 B02 is a small-molecule inhibitor of human RAD51 with an IC50 of 27.4 μM, but does not inhibit its E. coli homologue RecA (IC50 > 250 μM). Apr 21 2017
S8363 NMS-P118 NMS-P118 is a potent, orally available, and highly selective PARP-1 inhibitor endowed with excellent ADME and pharmacokinetic profiles, showing 150-fold selectivity for PARP-1 over PARP-2 (Kd 0.009 μM vs 1.39 μM, respectively). Apr 21 2017