New Products

PI3K/Akt/mTOR
Catalog No. Product Name Information Added
S8672 Tenalisib (RP6530) Tenalisib (RP6530) is a potent and selective dual PI3Kδ/γ inhibitor with IC50 values of 24.5 nM and 33.2 nM for PI3Kδ and PI3Kγ, respectively. Its selectivity over α and β isoforms are more than 300-fold and 100-fold, respectively. May 11 2018
S7335 IPI-3063 IPI-3063 is a potent and selective p110δ inhibitor with biochemical IC50 of 2.5 ± 1.2 nM and IC50 values for the other class I PI3K isoforms (p110α, p110β, p110γ) are at least 400-fold higher. Mar 28 2018
S8335 PF-06409577 PF-06409577 is orally bioavailable AMPK activator with EC50 of 7 nM for α1β1γ1 in the TR-FRET assay and it shows no detectable inhibition of hERG in a patch-clamp assay (100 μM) and was not an inhibitor (IC50 > 100 μM) of the microsomal activities of major human cytochrome P450 isoforms. Nov 22 2017
S8581 Serabelisib (INK-1117,MLN-1117,TAK-117) Serabelisib (INK-1117,MLN-1117,TAK-117) is a potent and selective oral PI3Kα isoform inhibitor (IC50 of 21 nmol/L against PI3Kα) that has demonstrated > 100-fold selectivity relative to other class I PI3K family members (PI3Kβ/γ/δ) and mTOR, and a high degree of selectivity against many other kinase. Sep 11 2017
S8330 IPI-549 IPI-549 is a potent inhibitor of PI3K-γ with >100-fold selectivity over other lipid and protein kinases. The biochemical IC50 for PI3K-γ is 16 nM. Aug 08 2017
S8589 SF2523 SF2523 is a highly selective and potent inhibitor of PI3K with IC50 values of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively. Aug 01 2017
S8317 3BDO 3BDO, a butyrolactone derivative, could target FKBP1A and activate the mTOR signaling pathway. It inhibits autophagy in HUVECs. Jul 26 2017
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 umbralisib (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
JAK/STAT
Catalog No. Product Name Information Added
S7812 Itacitinib (INCB39110) Itacitinib(INCB39110) is an orally bioavailable inhibitor of Janus-associated kinase 1 (JAK1) with potential antineoplastic activity. Jun 01 2018
S8685 AS1517499 AS1517499 is a novel and potent STAT6 inhibitor with an IC50 value of 21 nM. May 11 2018
S8538 PF-06651600 PF-06651600 is a potent and irreversible JAK3-selective inhibitor with an IC50 of 33.1 nM but without activity (IC50 > 10 000 nM) against JAK1, JAK2, and TYK2. Mar 28 2018
S8605 C188-9 C188-9 is a potent inhibitor of STAT3 that binds to STAT3 with high affinity (KD=4.7±0.4 nM). C188-9 is well tolerated in mice, shows good oral bioavailability, and is concentrated in tumors. Jan 10 2018
S8541 FM-381 FM-381 is a JAK3 specific reversible covalent inhibitor with IC50 of 127 pM for JAK3 and demonstrates 400-, 2,700- and 3,600-fold selectivity over JAK1, JAK2, and TYK2, respectively. Dec 27 2017
S8561 HJC0152 HJC0152 is a signal transducer and activator of transcription 3 (STAT3) inhibitor with remarkably improved aqueous solubility. Sep 19 2017
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
Cell Cycle
Catalog No. Product Name Information Added
S5244 Zoledronic acid monohydrate Zoledronic acid, a nitrogen-containing bisphosphonate, is a potent osteoclast inhibitor which induces apoptosis in osteoclasts by inhibiting enzymes of the mevalonate pathway and preventing the isoprenylation of small GTP-binding proteins such as Ras and Rho. Jun 07 2018
S8699 SNS-314 Mesylate SNS-314 Mesylate is a potent and selective inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 9 nM, 31 nM, and 3 nM, respectively and less potent to Trk A/B, Flt4, Fms, Axl, c-Raf and DDR2. Apr 18 2018
S8652 Skp2 inhibitor C1 (SKPin C1) Skp2 inhibitor C1 (SKPin C1) is a specific and selective small-molecule inhibitor of Skp2-mediated p27 degradation by reducing p27 binding through key compound-receptor contacts. Apr 18 2018
S8662 PTC-028 PTC-028 is an orally bioavailable compound that decreases BMI-1 levels by posttranslational modification. Mar 15 2018
S2284 Colchicine Colchicine is a microtubule polymerization inhibitor with an IC50 of 3 nM. Dec 04 2017
S8469 CCG-203971 CCG-203971 is a novel small-molecule inhibitor of the Rho/MRTF/SRF pathway with the IC50 value of 0.64 μM for SRE.L. It inhibits Rho-mediated gene transcription. Nov 22 2017
S8632 Chk2 Inhibitor II (BML-277) Chk2 Inhibitor II (BML-277) is an ATP-competitive inhibitor of Chk2 with IC50 of 15 nM. It is 1000-fold more selective toward Chk2 serine/threonine kinase than for Chk1 and Cdk1/B kinases. Nov 02 2017
S8499 KRpep-2d KRpep-2d is a K-Ras(G12D) selective inhibitory cyclic peptide with selectivity against wild-type (WT) K-Ras and the K-Ras(G12C) mutant. The IC50 value is 1.6 nM. Sep 11 2017
S8387 MSC2530818 MSC2530818, a CDK8 inhibitor with the IC50 of 2.6 nM, displays excellent kinase selectivity, biochemical and cellular potency, microsomal stability, and is orally bioavailable. Jul 26 2017
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
DNA Damage
Catalog No. Product Name Information Added
S5059 Pixantrone Maleate Pixantrone is a novel aza-anthracenedione compound with antitumor activity. It is a weak topoisomerase II inhibitor and forms stable DNA adducts through alkylation with specificity for DNA hypermethylated sites. Jun 01 2018
S5111 7-Ethylcamptothecin 7-Ethyl Camptothecin is an anti-cancer chemical that exhibits a strong activity against various murine tumors through Topo I (topoisomerase) inhibition. Apr 02 2018
S4782 5-methoxyflavone 5-methoxyflavone is a novel DNA polymerase-beta inhibitor and neuroprotective agent against beta-amyloid toxicity. Mar 30 2018
S3898 Hydroxy Camptothecine 10-Hydroxycamptothecin is a cell-permeable powerful DNA topoisomerase I inhibitor. It has selective inhibitory effect on the phosphorylation of histone H1 and H3, but less effect on other histones. Mar 12 2018
S8666 BAY 1895344 (BAY-1895344) BAY 1895344 is a potent, highly selective and orally available ATR inhibitor with an IC50 of 7 nM. Jan 16 2018
S3669 Carmustine Carmustine is a cell-cycle phase nonspecific alkylating antineoplastic agent and used in the treatment of brain tumors and various other malignant neoplasms. Nov 29 2017
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
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 Ruboxistaurin (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 Vactosertib  (TEW-7197) Vactosertib  (TEW-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
S8720 AZD-4635 (HTL1071) AZD-4635 (HTL1071) is an oral A2AR antagonist that binds to human A2AR with a Ki of 1.7 nM and with > 30-fold selectivity over other adenosine receptors. Jun 07 2018
S4932 Proxyphylline Proxyphylline is a derivative of theophylline which is used as a bronchodilator and for its cardiovascular properties. It selectively antagonizes A1 adenosine receptors (Ki = 82 nM for bovine brain) versus A2 adenosine receptors (Ki = 850 µM for platelets). Apr 18 2018
S3988 Theophylline-7-acetic acid Theophylline-7-acetic acid (Acefylline), acting as an adenosine receptor antagonist, is a stimulant drug of the xanthine chemical class. Apr 12 2018
S3734 Albiglutide Albiglutide is a glucagon-like peptide-1 agonist (GLP-1 agonist). Dec 19 2017
S8575 A2AR antagonist 1 A2AR antagonist 1 is a potent A2AR (Adenosine A2A Receptor) antagonist with Ki values of 4 nM and 264 nM for A2AR and A1R, respectively. Nov 15 2017
S8637 Ipragliflozin (ASP1941) Ipragliflozin (ASP1941) is a highly selective sodium-glucose cotransporter 2 (SGLT2) inhibitor with an IC50 value of 7.4 nM for hSGLT2 and a 254-fold selectivity versus SGLT1. Oct 24 2017
S2879 AMD3465 hexahydrobromide AMD3465 is a monomacrocyclic CXCR4 antagonist. Sep 06 2017
S8558 Tofogliflozin(CSG 452) Tofogliflozin is a novel sodium-glucose co-transporter 2(SGLT2) inhibitor with IC50 values of 2.9 nM and 8444 nM for hSGLT2 and hSGLT1, respectively. Aug 29 2017
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
PTK
Catalog No. Product Name Information Added
S5232 Alectinib hydrochloride Alectinib is a second generation oral drug that selectively inhibits the activity of anaplastic lymphoma kinase (ALK) tyrosine kinase. Jun 13 2018
S5077 Regorafenib Monohydrate Regorafenib is a novel oral multikinase inhibitor with IC50 values of 13, 4.2, 46, 22, 7, 1.5, 2.5, 28, 19 nM for VEGFR1, murine VEGFR2, murine VEGFR3, PDGFR-β, KIT, RET, RAF-1, B-RAF and B-RAF(V600E) respectively. Jun 08 2018
S8675 H3B-6527 H3B-6527 is a highly selective covalent FGFR4 inhibitor with an IC50 value of <1.2 nM and at least 250-fold selectivity over FGFR1-3 (IC50 values of 320, 1,290 and 1,060 nM respectively). Feb 28 2018
S7674 Savolitinib(AZD6094, HMPL-504) Savolitinib (volitinib, AZD6094, HMPL-504) is a novel, potent, and selective MET inhibitor currently in clinical development in various indications, including PRCC. The IC50 values of this compound for c-Met and p-Met are 5 nM and 3 nM, respectively. It shows exquisite selectivity for c-Met over 274 kinase. Feb 28 2018
S3759 Norcantharidin Norcantharidin is a synthetic anticancer compound which is a dual inhibitor for c-Met and EGFR in human colon cancers. Feb 07 2018
S8553 Avapritinib (BLU-285) Avapritinib (BLU-285) is a small molecule kinase inhibitor that potently inhibits PDGFRα D842V mutant activity in vitro (IC50 = 0.5 nM) and PDGFRα D842V autophosphorylation in the cellular setting (IC50 = 30 nM); also a potent inhibitor of the analogous KIT mutation, D816V in KIT Exon 17 (IC50 = 0.5 nM). Oct 24 2017
S7754 Gilteritinib (ASP2215) Gilteritinib(ASP2215) is a small-molecule FLT3/AXL inhibitor with IC50 values of 0.29 nM and 0.73 nM for FLT3 and AXL, respectively. It inhibits FLT3 at an IC50 value that was approximately 800-fold more potent than the concentration required to inhibit c-KIT (230 nM). Oct 17 2017
S8511 Belizatinib (TSR-011) "Belizatinib (TSR-011) is a potent inhibitor of ALK (IC50=0.7 nM) and tropomyosin receptor kinase (TRK) (IC50 values less than 3 nM for TRK A, B, and C). " Sep 19 2017
S8407 PF-06273340 PF-06273340 is a highly potent, kinases elective, well-tolerated pan-Trk inhibitor with IC50 values of 6, 4, 3 nM for TrkA, TrkB, Trk C, respectively. Aug 29 2017
S8583 TPX-0005 TPX-0005 is a novel ALK/ROS1/TRK inhibitor with the IC50 values of 1.01 nM for WT ALK, 1.26 nM for ALK(G1202R), and 1.08 nM for ALK(L1196M); also a potent SRC inhibitor (IC50 5.3 nM). Aug 01 2017
Epigenetics
Catalog No. Product Name Information Added
S8607 JQ-EZ-05 (JQEZ5) JQ-EZ-05 is a specific and reversible EZH1/2 inhibitor. Apr 12 2018
S7230 UNC0642 UNC0642 is a potent, selective inhibitor of histone methyltransferases G9a/GLP with IC50s less than 2.5 nM for G9a and GLP and shows more than 300-fold selective for G9a and GLP over a broad range of kinases, GPCRs, transporters, and ion channels. Apr 03 2018
S8479 LLY-283 LLY-283 is the potent and selective SAM-competitive chemical probe for PRMT5. It inhibits PRMT5 enzyme activity with IC50 of 20 nM for methylation of an H4R3 derived peptide substrate, and shows greater than 100-fold selectivity over other histone methyltransferases and non-epigenetic targets. Mar 28 2018
S8627 OSS_128167 OSS_128167 is a specific SIRT6 inhibitor with IC50 values of 89, 1578 and 751 μM for SIRT6, SIRT1 and SIRT2, respectively. Feb 28 2018
S8495 WT161 WT161 is a potent, selective, and bioavailable HDAC6 inhibitor with IC50 values of 0.4 nM, 8.35 nM and 15.4 nM for HDAC6, HDAC1 and HDAC2, respectively; shown to have >100-fold selectivity over other HDACs. Feb 28 2018
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. Feb 08 2018
S3944 Valproic acid Valproic acid is a fatty acid with anticonvulsant properties used in the treatment of epilepsy. It is also a histone deacetylase inhibitor and is under investigation for treatment of HIV and various cancers. Jan 25 2018
S8664 GSK3326595 (EPZ015938) GSK3326595 (EPZ015938) is an orally active, potent and selective inhibitor of protein arginine methyltransferase 5 (PRMT5) and potently inhibits tumor growth in vitro and in vivo in animal models. Jan 03 2018
S8648 ACY-738 ACY-738 inhibits HDAC6 with low nanomolar potency (IC50=1.7 nM) and a selectivity of 60- to 1500-fold over class I HDACs. Dec 05 2017
S8601 CP2 CP2 is a cyclic peptide that inhibits the JmjC histone demethylases KDM4 with IC50 values of 42 nM and 29 nM for KDM4A and KDM4C, respectively. Nov 07 2017
NF-κB
Catalog No. Product Name Information Added
S3633 Pyrrolidinedithiocarbamate ammonium Ammonium pyrrolidine dithiocarbamate (PDTC) is a potent nuclear factor-κB (NF-κB) inhibitor that inhibits IκB phosphorylation, blocks NF-κB translocation to the nucleus and reduces the expression of downstream cytokines. Nov 15 2017
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 NF-kB. 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
Metabolism
Catalog No. Product Name Information Added
S5097 Methotrexate disodium Methotrexate sodium, an inhibitor of tetrahydrofolate dehydrogenase, is an antineoplastic antimetabolite with immunosuppressant properties. Jun 13 2018
S5082 Vitamin K2 Vitamin K2 is an important fat-soluble vitamin that plays critical roles in protecting heart and brain, and building strong bones. It also plays an important role in cancer protection. Jun 13 2018
S4994 Methylcobalamin Methylcobalamin is one active form of vitamin B12 which can directly participate in homocysteine metabolism. It is used to treat some nutritional diseases and other diseases in clinic, such as Alzheimer's disease and rheumatoid arthritis. Jun 08 2018
S4987 Inositol niacinate   Jun 08 2018
S4989 AOA hemihydrochloride Aminooxyacetic acid is an inhibitor of aminobutyrate aminotransferase involved in amino acid and polyamine metabolism. Jun 01 2018
S5200 Diaveridine Diaveridine is coccidiostat with anti-parasitic activity and also a dihydrofolate reductase (DHFR) inhibitor preventing folic acid synthesis in species of Pneumocystis. Jun 01 2018
S4825 Pancreatin Pancreatic enzymes also known as pancrelipase and pancreatin, are commercial mixtures of amylase, lipase, and protease. They are used to treat malabsorption syndrome due to pancreatic problems. May 16 2018
S4871 Pyridoxal 5-phosphate monohydrate Pyridoxal 5-phosphate monohydrate is an active vitamin B6 metabolite, which is a cofactor in many reactions of amino acid metabolism. May 16 2018
S8444 KPT-9274 KPT-9274 is an orally bioavailable small molecule that is a non-competitive dual inhibitor of PAK4 and NAMPT. It shows an IC50 of ~120 nM for NAMPT in a cell-free enzymatic assay. Apr 25 2018
S4837 Ibudilast Ibudilast is a relatively non-selective phosphodiesterase inhibitor with anti-inflammatory and neuroprotective activities. Apr 18 2018
Proteases
Catalog No. Product Name Information Added
S5404 Paritaprevir (ABT-450) Paritaprevir (ABT-450) is a nonstructural (NS) protein 3/4A protease inhibitor. Jun 13 2018
S5403 Ombitasvir (ABT-267) Ombitasvir (ABT-267) is an inhibitor of the HCV non-structural protein 5A with antiviral activity. Jun 13 2018
S5307 PSI-6206 (RO-2433, GS-331007) PSI-6206 (RO-2433, GS-331007) is a potent inhibitor of the hepatitis C virus RNA-dependent RNA polymerase, targeting NS5B polymerase. Jun 13 2018
S5079 Sitagliptin Sitagliptin is an oral and highly selective DPP-4 inhibitor with an IC50 of 18 nM. It is used for the treatment of type 2 diabetes. Jun 08 2018
S5063 Trelagliptin succinate Trelagliptin succinate is a dipeptidyl peptidase IV (DPP-4) inhibitor which is used as a new long-acting drug for once-weekly treatment of type 2 diabetes mellitus (DM). Jun 01 2018
S4935 Asunaprevir Asunaprevir is an orally bioavailable inhibitor of the hepatitis C virus enzyme serine protease NS3 that is necessary for protein processing required for viral replication. Apr 12 2018
S5015 Simeprevir Simeprevir is a competitive, reversible, macrocyclic, noncovalent hepatitis C virus (HCV) NS3/4A protease inhibitor that acts directly against the hepatitis C virus. It has a medium inhibitory concentration (IC50) <13 nM for all HCV NS3/4A enzymes(genotypes 1a, 1b, 2, 4, 5, and 6), but has an IC50 value of 37 nM for genotype 3. Apr 12 2018
S3733 Boceprevir Boceprevir is an oral, direct acting hepatitis C virus (HCV) protease inhibitor with Ki value of 14 nM for NS3. It is used in combination with other antiviral agents in the treatment of chronic hepatitis C, genotype 1. Dec 05 2017
S3724 Velpatasvir Velpatasvir is a second-generation NS5A inhibitor that inhibits hepatitis C viral replication through acting on the crucial "membranous web" that facilitates RNA replication. Nov 29 2017
S3728 Grazoprevir Grazoprevir anhydrous is a Hepatitis C Virus NS3/4A Protease inhibitor with IC50 values of 7pM, 4pM, and 62pM for HCV genotype 1a, 1B, and 4 respectively. Nov 23 2017
Microbiology
Catalog No. Product Name Information Added
S5048 Fosfomycin Disodium Fosfomycin is a bactericidal, low-molecular weight, broad-spectrum antibiotic, with putative activity against several bacteria, including multidrug-resistant Gram-negative bacteria, by irreversibly inhibiting an early stage in cell wall synthesis. Jun 13 2018
S5051 Pipemidic acid Pipemidic acid is a pyridopyrimidine antibiotic derivative of piromidic acid with activity against gram-negative and some gram-positive bacteria. Jun 13 2018
S5081 Ceforanide Ceforanide is a new cephalosporin with antibacterial activity and has a longer elimination half-life than any currently available cephalosporin. Jun 13 2018
S5035 6-Aminopenicillanic acid 6-Aminopenicillanic acid (6-APA) is the central component of penicillin β-lactam antibiotics which are generated by Penicillium. It is used as precursor for antibiotic compounds ampicillin and amoxicillin. Jun 13 2018
S5053 Imazalil Imazalil is a fungicide widely used in agriculture, also used in veterinary medicine as a topical antimycotic. Jun 13 2018
S5245 Raltegravir potassium Raltegravir Potassium is the orally bioavailable potassium salt of raltegravir, the first approved human immunodeficiency virus type 1 (HIV-1) integrase inhibitor. Jun 13 2018
S5062 Daclatasvir Digydrochloride Daclatasvir is an orally available antiviral agent that inhibits the NS5A region of the hepatitis C virus (HCV) used for the treatment of chronic HCV genotype 1 and 3 infection. Jun 08 2018
S5092 Febantel Febantel is a prodrug that is metabolized to fenbendazole and oxfendazole, which are undoubtedly the active parasiticides. Jun 08 2018
S4878 Neticonazole Hydrochloride Neticonazole is an imidazole antifungal for the treatment of fungal skin infections. Jun 08 2018
S5093 Rafoxanide Rafoxanide is a salicylanilide used as an anthelmintic, being effective treatment for the control of fluke infections in animals. Jun 07 2018
Apoptosis
Catalog No. Product Name Information Added
S8606 HDM201 HDM201 is a novel, highly potent and selective inhibitor of the p53-Mdm2 interaction with affinity constant for Mdm2 in the picomolar range and a selectivity ratio greater than 10000-fold vs Mdm4. Apr 18 2018
S8650 BTSA1 BTSA1 is a pharmacologically optimized BAX activator that binds with high affinity and specificity to the N-terminal activation site and induces conformational changes to BAX leading to BAX-mediated apoptosis. It effectively promotes apoptosis in leukemia cell lines and patient samples while sparing healthy cells. Feb 28 2018
S8483 CBL0137 (CBL-0137) CBL0137(CBL-0137) activates p53 and inhibits NF-kB with EC50s of 0.37 μM and 0.47 μM in the cell-based p53 and NF-kB reporter assays, respectively. It also inhibits histone chaperone FACT (facilitates chromatin transcription complex). Jan 16 2018
S8580 COTI-2 COTI-2 is an orally available third generation thiosemicarbazone and activator of mutant forms of the p53 protein, with potential antineoplastic activity. Dec 19 2017
A2010 Adalimumab Adalimumab is the first fully human, recombinant IgG1 monoclonal antibody that specifically targets human TNF-alpha, MW: 144.19 KD. Nov 16 2017
S8383 S63845 S63845 is a new, selective MCL-1 inhibitor with the Kd value of 0.19 nM and has no discernible binding to the other BCL-2 members, BCL-2 or BCL-XL. Nov 15 2017
S8304 Azoramide Azoramide is a small-molecule modulator of the unfolded protein response (UPR). It improves ER protein-folding ability and activates ER chaperone capacity to protect cells against ER stress. Oct 17 2017
S7100 WEHI-539 WEHI-539 has high affinity (IC50=1.1 nM) and selectivity for BCL-XL and potently kills cells by selectively antagonizing its prosurvival activity. It has more than a 400-fold higher affinity for BCL-XL versus other prosurvival BCL-2 family members. Sep 26 2017
S8465 GSK'872 (GSK2399872A) GSK'872 (GSK2399872A) is a potent and selective RIP3 kinase inhibitor which binds RIP3 kinase domain with high affinity (IC50=1.8 nM) and inhibits kinase activity with IC50 of 1.3 nM. It has minimal cross-reactivity. Sep 05 2017
S8591 FX1 FX1 is a selective BCL6 BTB inhibitor with an IC50 value of 35 μM in reporter assays. FX1 shows great selectivity against a panel of 50 different kinases. 10 μM FX1 fails to significantly inhibit of any of these kinases. Aug 29 2017
MAPK
Catalog No. Product Name Information Added
S8690 RAF709 RAF709 is a potent inhibitor of B/C RAF kinase with almost equivalent IC50 values of 0.4 nM for B-RAF and C-RAF, showing a high level of selectivity, demonstrating greater than 99% on-target binding to BRAF, BRAFV600E, and CRAF at 1 μM and very few off-targets with DDR1 (>99%), DDR2 (86%), FRK (92%), and PDGFRb (96%), the only kinases with binding >80% at 1 μM. May 22 2018
S8534 LY3214996 LY3214996 is a selective and novel ERK1/2 inhibitor with IC50 of 5 nM for both enzymes in biochemical assays. It potently inhibits cellular phospho-RSK1 in BRAF and RAS mutant cancer cell lines. Nov 02 2017
S7926 Lifirafenib (BGB-283) Lifirafenib (BGB-283) potently inhibits RAF family kinases and EGFR activities in biochemical assays with IC50 values of 23, 29 and 495 nM for the recombinant BRAFV600E kinase domain, EGFR and EGFR T790M/L858R mutant. Sep 19 2017
S7648 OTS964 OTS964 is a potent TOPK inhibitor with high affinity and selectivity and IC50 value is 28 nM. Apr 21 2017
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
S7652 OTS514 hydrochloride OTS514 is a highly potent TOPK(T-LAK cell-originated protein kinase) inhibitor with an IC50 value of 2.6 nM. Feb 22 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. IC50=120 ± 23 nM. Nov 21 2016
Angiogenesis
Catalog No. Product Name Information Added
S8542 Btk inhibitor 2 Btk inhibitor 2 is a BTK inhibitor. Jun 07 2018
S8555 Asciminib (ABL001) Asciminib(ABL001) is a potent and selective allosteric ABL1 inhibitor with dissociation constant (Kd) of 0.5-0.8 nM and selectivity to the myristoyl pocket of ABL1. May 11 2018
S8348 BMS-935177 BMS-935177 is a potent, reversible Bruton's Tyrosine Kinase (BTK) inhibitor with an IC50 value of 2.8 nM and demonstrates good kinase selectivity. It is more potent against BTK than other kinase, including the other Tec family kinases (TEC, BMX, ITK, and TXK) over which the compound is between 5- and 67-fold selective. Apr 25 2018
A2006 Bevacizumab Bevacizumab is a humanized anti-VEGF monoclonal antibody which binds to and neutralizes all human VEGF-A isoforms and bioactive proteolytic fragments, MW:149 KD. Nov 16 2017
A2007 Trastuzumab Trastuzumab is a humanized, recombinant monoclonal antibody that binds to the extracellular domain of HER2, MW:145.53 KD. Nov 16 2017
A2008 Pertuzumab Pertuzumab, a humanized monoclonal antibody and the first in the class of agents called the HER2 dimerization inhibitors, impairs the ability of HER2 to bind to other members of the HER family, MW: 148 KD. Nov 16 2017
S8230 Ensartinib (X-396) Ensartinib (X-396) is a novel, potent and specific ALK TKI with the IC50 less than 4 nM in Ambit assays. Oct 09 2017
S8578 PRN1371 PRN1371 is an irreversible covalent FGFR1-4 kinase inhibitor, with IC50s of 0.6, 1.3, 4.1, 19.3 and 8.1 nM for FGFR1, 2, 3, 4 and CSF1R, respectively. Sep 26 2017
S8441 LW 6 LW6 is a hypoxia-inducible factor 1(HIF) inhibitor which potently inhibits HIF-1α accumulation by degrading HIF-1α without affecting the HIF-1a mRNA levels during hypoxia. It inhibits hypoxia-induced HIF-1α transcription activity with IC50 of 2.64 μM in cell-based HRE-reporter gene assays. Sep 19 2017
S8442 TAK-659 TAK-659 is a potent and selective inhibitor of spleen tyrosine kinase (SYK) with an IC50 value of 3.2 nM. It is selective against most other kinases, but potent toward both SYK and FLT3. Aug 08 2017
Stem Cell & Wnt
Catalog No. Product Name Information Added
S8645 IWP-O1 IWP-O1 is a porcn inhibitor with an EC50 value of 80 pM in a cultured cell reporter assay of Wnt signaling and effectively suppresses the phosphorylation of Dvl2/3 in HeLa cells. Jun 01 2018
S8661 CA3 CA3 has potent inhibitory effects on YAP1/Tead transcriptional activity and primarily targets YAP1 high and therapy-resistant esophageal adenocarcinoma cells endowed with CSC properties. Mar 15 2018
S7160 Glasdegib (PF-04449913) Glasdegib (PF-04449913) is a potent, and orally bioavailable Smoothened (Smo) inhibitor with IC50 of 5 nM. Phase 2. Mar 07 2018
S8647 iCRT3 iCRT3 is an antagonist of Wnt/β-catenin signaling with an IC50 of 8.2 nM in the Wnt responsive STF16-luc reporter assays. Jan 10 2018
S8597 LYN-1604 LYN-1604 is a potential ULK1 agonist with IC50 of 1.66 μM against MDA-MB-231 cells and it binds to wild-type ULK1 with a binding affinity in the nanomole range (Kd=291.4 nM). The ULK1 (Y89A) mutant protein caused a sharp decrease in binding affinity with lower response and Kd than wild-type ULK1, ULK1 (K50A) and ULK1 (L53A) mutants. Dec 05 2017
S8644 GNF-6231 GNF-6231 is a potent, orally active and selective Porcupine inhibitor with IC50 of 0.8 nM. Dec 05 2017
S8554 Super-TDU Super-TDU is an inhibitory peptide targeting YAP-TEADs interaction. Sep 19 2017
S8572 Amcasertib (BBI503) Amcasertib (BBI503), a first-in-class cancer stemness kinase inhibitor, is claimed to inhibit Nanog and other CSC pathways by targeting kinases with potential anticancer activity. Aug 01 2017
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
Ubiquitin
Catalog No. Product Name Information Added
S8696 2-D08 2-D08 is a cell permeable, mechanistically unique inhibitor of protein sumoylation. It is also inhibits Axl, IRAK4, ROS1, MLK4, GSK3β, RET, KDR and PI3Kα with IC50 values of 0.49, 3.9, 5.3, 9.8, 11, 11, 17 and 35 nM respectively in biochemical assays. May 24 2018
S7109 Pevonedistat (MLN4924) MLN4924 is a small molecule inhibitor of Nedd8 activating enzyme (NAE) with IC50 of 4 nM. Aug 31 2017
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
Neuronal Signaling
Catalog No. Product Name Information Added
S5073 Donepezil Donepezil is a piperidine based, potent, specific, non-competitive and reversible inhibitor of acetylcholinesterase (AChE) used for the treatment of mild to moderate dementia of the Alzheimer's type. Jun 13 2018
S5088 Labetalone hydrochloride Labetalone hydrochloride is hydrochloride form of labetalone, a blocker of both alpha- and beta-adrenergic receptors that is used as an antihypertensive. Jun 13 2018
S5302 6-Methoxy-2-naphthoic acid 6-Methoxy-2-naphthoic acid is an modulator of NMDAR. Jun 13 2018
S5075 Acotiamide Acotiamide is a novel acetylcholinesterase inhibitor with fundus-relaxing and gastroprokinetic properties. Jun 08 2018
S4834 Propantheline bromide   Jun 08 2018
S5052 Granisetron Granisetron is a serotonin receptor (5HT-3 selective) antagonist that is used as an antiemetic and antinauseant for cancer chemotherapy. Jun 08 2018
S5066 Pramipexole dihydrochloride Pramipexole dihydrochloride is a dopamine agonist of the non-ergoline class indicated for treating Parkinson's disease (PD) and restless legs syndrome (RLS) with Ki values of 3.9 nM, 2.2 nM, 0.5 nM and 5.1 nM for D2S receptor, D2L receptor, D3 receptor and D4 receptor. Jun 08 2018
S5100 Pralidoxime Iodide Pralidoxime Iodide (2-PAM) is an antidote approved for reactivation of inhibited acetylcholinesterase (AChE) in organophosphate poisoning. Jun 07 2018
S5034 Melitracen hydrochloride Melitracen hydrochloride is a potential dopamine D1/2 receptor antagonist which has antidepressant properties. May 22 2018
S5042 Bevantolol hydrochloride Bevantolol hydrochloride is a cardioselective, beta adrenoceptor antagonist, devoid of intrinsic β sympathomimetic activity and with weak membrane-stabilizing and local anesthetic properties. May 22 2018
Others
Catalog No. Product Name Information Added
S5306 Forchlorfenuron (KT-30, CPPU) Forchlorfenuron is a synthetic cytokinin that inhibits septins and exhibits anti-parasitic, anticancer, and anti-angiogenic activities. Jun 13 2018
S5037 Phenazine methosulfate Phenazine methosulfate is widely used as an intermediate electron carrier for coupling the production of NADH or NADPH to the reduction of tetrazolium salts to coloured formazans. Jun 13 2018
S5056 Dinoprost tromethamine Dinoprost Tromethamine is a synthetic analogue of the naturally occurring prostaglandin F2 alpha, which stimulates myometrial activity, relaxes the cervix, inhibits corpus luteal steroidogenesis, and induces luteolysis by direct action on the corpus luteum. Jun 13 2018
S5222 Coluracetam Coluracetam (BCI-540, MKC-231) is a nootropic belonging to the racetam family of drugs with cognitive enhancing and neuroprotective effects. Jun 13 2018
S5024 Miriplatin Miriplatin is a derivative of cisplatin containing myristates as a carrier ligand. It is a novel lipophilic platinum complex developed to treat hepatocellular carcinoma. Jun 13 2018
S5045 Nomilin Nomilin is a triterpenoid present in common edible citrus fruits with putative anticancer properties. Jun 08 2018
S5074 Argatroban Monohydrate Argatroban is a direct, selective thrombin inhibitor with anticoagulant effects. Jun 08 2018
S4991 Valpromide Valpromide is an antiepileptic drug, derivative of Valproic acid (VPA), used as a mood-stabilizer in bipolar disorder. Jun 08 2018
S4877 Eperisone hydrochloride Eperisone hydrochloride is muscle relaxant agent with antispasmodic effects. It is widely used in the treatment of patients with muscular contractures, low back pain or spasticity. Jun 08 2018
S5058 Revaprazan Hydrochloride Revaprazan Hydrochloride is a new reversible proton pump inhibitor with long-lasting acid-suppressive effects. Jun 08 2018