新製品

添加時期順序で新製品が表示されます。

PI3K/Akt/mTOR
製品コード 製品名称 製品説明 添加時期
S8738 Bimiralisib (PQR309) Bimiralisib (PQR309) is a novel brain-penetrant dual PI3K/mTOR inhibitor with in vitro and in vivo antilymphoma activity. It displays excellent selectivity versus PI3K-related lipid kinases, protein kinases and unrelated targets. Oct 24 2018
S8560 Seletalisib (UCB-5857) Seletalisib is a novel small-molecule inhibitor of PI3Kδ with an IC50 value of 12 nM and shows significant selectivity to PI3Kδ with respect to the other class I PI3K isoforms (between 24- and 303-fold). Oct 18 2018
S5313 SC66 SC66 is an allosteric inhibitor which displays a dual-inhibitory function toward AKT activity with IC50 values of 0.77, 2.85 and 0.47 μg/ml in HepG2, Huh7 and Hep3B cells after 72 h treatment, respectively. Jun 28 2018
S8680 AZD1390 AZD1390 is a first-in-class orally available and CNS penetrant ATM inhibitor with an IC50 of 0.78 nM in cells and >10,000-fold selectivity over closely related members of the PIKK family of enzymes and excellent selectivity across a broad panel of kinases. Jun 28 2018
S5284 Adenosine 5'-monophosphate monohydrate Adenosine 5'-monophosphate monohydrate (5'-AMP) is an activator of a class of protein kinases known as AMP-activated protein kinase (AMPK). Jun 24 2018
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
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
JAK/STAT
製品コード 製品名称 製品説明 添加時期
S5754 Baricitinib phosphate Baricitinib phosphate is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM, ~70 and ~10-fold selective versus JAK3 and Tyk2, no inhibition to c-Met and Chk2. Dec 12 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
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
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
Cell Cycle
製品コード 製品名称 製品説明 添加時期
S8749 MBQ-167 MBQ-167 is a potent and dual inhibitor of Rac and Cdc42 with IC50s of 103 nM and 78 nM respectively, in metastatic breast cancer cells. Nov 08 2018
S8707 ARS-1620 ARS-1620 is a potent, orally bioavailable covalent inhibitor of KRASG12C) and could achieve rapid and sustained in vivo target occupancy to induce tumor regression. Oct 18 2018
S8727 Atuveciclib (BAY-1143572) Atuveciclib (BAY-1143572) is potent and highly selective PTEFb/CDK9 inhibitor with IC50 values of 13 nM for CDK9/CycT and the ratio of IC50 values for CDK2/CDK9 is about 100. Outside the CDK family, It inhibits GSK3 kinase with IC50 values of 45 nM and 87 nM for GSK3α and GSK3β respectively. Sep 27 2018
S8526 GDC-0575 (ARRY-575, RG7741) GDC-0575 (ARRY-575, RG7741) is a potent and selective CHK1 inhibitor with an IC50 of 1.2 nM. Sep 19 2018
S5716 Abemaciclib Abemaciclib is a cell cycle inhibitor selective for CDK4/6 with IC50 of 2 nM and 10 nM in cell-free assays, respectively. Sep 11 2018
S5316 NU2058 NU2058 is an inhibitor of CDK2 with IC50 value of 17 μM in an isolated enzyme assay. It also potentiates melphalan (DMF 2.3), and monohydroxymelphalan (1.7), but not temozolomide or ionising radiation. Jun 28 2018
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 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
DNA Damage
製品コード 製品名称 製品説明 添加時期
S9451 Uridine 5'-monophosphate Uridine 5'-monophosphate is a nucleotide that is used as a monomer in RNA. Dec 12 2018
S8556 AZ31 AZ31 is a selective and novel ATM inhibitor with an IC50 of <0.0012 μM. It shows excellent selectivity over closely related enzymes (>500 fold selective over DNA-PK and PI3Kα and >1000 fold selective over mTOR, PI3Kβ and PI3Kγ). Dec 06 2018
S5627 Amsacrine hydrochloride Amsacrine hydrochloride is the hydrochloride salt form of amsacrine, which is an inhibitor of topoisomerase II with antineoplastic activity. Dec 06 2018
S9321 Topotecan Topotecan is an antineoplastic agent used to treat ovarian cancer that works by inhibiting DNA topoisomerases. Nov 16 2018
S9360 4-Hydroxyquinazoline 4-Hydroxyquinazoline is a PARP inhibitor with a high potency for PARP-1 and no effects on enzymes other than PARP. Nov 16 2018
S8729 AZ32 AZ32 is a specific inhibitor of the ATM kinase that possesses good BBB penetration in mouse with an IC50 value of <0.0062 μM for ATM enzyme. It shows adequate selectivity over ATR and also has high cell permeability. Oct 18 2018
S5374 5'-Cytidylic acid 5'-Cytidylic acid is a nucleotide that is used as a monomer in RNA. Aug 02 2018
S5384 UTP, Trisodium Salt Uridine-5'-triphosphate (UTP) is a pyrimidine nucleoside triphosphate and a substrate for the synthesis of RNA during transcription. Aug 02 2018
S5582 Cytarabine hydrochloride Cytarabine is a pyrimidine nucleoside analog that is used mainly in the treatment of leukemia. It is an antimetabolite antineoplastic agent that inhibits the synthesis of DNA. Aug 02 2018
S5552 Amenamevir Amenamevir is a potent helicase-primase inhibitor and a novel class of antiviral agent. Jul 18 2018
TGF-beta/Smad
製品コード 製品名称 製品説明 添加時期
S1292 Chelerythrine Chloride Chelerythrine is a potent, selective antagonist of PKC with IC50 of 0.66 mM. Oct 26 2018
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 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
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
製品コード 製品名称 製品説明 添加時期
S5358 Regadenoson Regadenoson is a selective A2A adenosine receptor agonist with coronary vasodilating activity. Aug 10 2018
S5413 Ertugliflozin Ertugliflozin is a potent and selective sodium-dependent glucose cotransporter 2 inhibitor with IC50 values of 0.877 nM for h-SGLT2 and 1000-fold higher for h-SGLT1. Aug 10 2018
S8694 CID16020046 (CID 16020046) CID16020046 is a selective GPR55 antagonist, inhibiting GPR55 constitutive activity with IC50 of 0.15 μM in yeast. It demonstrates weak activity against a broad spectrum of other GPCRs, ion channels, kinases, and nuclear receptor. Aug 09 2018
S5566 Dapagliflozin propanediol monohydrate Dapagliflozin propanediol belongs to the class of orally administered antidiabetic agents designated as sodiumglucose cotransporter 2 (SGLT2) inhibitors. Jul 27 2018
S5427 Alloxazine Alloxazine is an A2 receptor antagonist, which is approximately 10-fold more selective for the A2B receptor than for the A2A receptor. Jul 18 2018
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 CPI-444 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
Protein Tyrosine Kinase
製品コード 製品名称 製品説明 添加時期
S8777 Evobrutinib Evobrutinib is a highly selective BTK inhibitor with potential anti-neoplastic activity. Dec 12 2018
S5078 Osimertinib mesylate Osimertinib mesylate is the mesylate form of osimertinib, which is an oral, third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) drug. Nov 28 2018
S8757 Ripretinib (DCC-2618) DCC-2618 is an orally bioavailable switch pocket control inhibitor of wild-type and mutated forms of the tumor-associated antigens (TAA) mast/stem cell factor receptor (SCFR) KIT and PDGFR-alpha, with IC50 values of 4 nM, 8 nM, 18 nM, 5 nM and 14 nM for WT KIT, V654A KIT, T670I KIT, D816H KIT and D816V KIT, respectively. Nov 01 2018
S8609 Derazantinib(ARQ-087) Derazantinib(ARQ-087) is an orally bioavailable inhibitor of the fibroblast growth factor receptor (FGFR) with IC50 values of 1.8 nM for FGFR2, and 4.5 nM for FGFR1 and 3, showing lower potency for FGFR4 (IC50=34 nM). It also inhibits RET, DDR2, PDGFRβ, VEGFR and KIT. Sep 19 2018
S5241 Lapatinib ditosylate monohydrate Lapatinib ditosylate is a dual tyrosine kinase inhibitor which interrupts the HER2/neu and epidermal growth factor receptor (EGFR) pathways, used for treatment of solid tumours such as breast and lung cancer. Sep 19 2018
S8741 Avitinib (AC0010) Avitinib (AC0010) is a pyrrolopyrimidine-based irreversible EGFR inhibitor that is mutation-selective with IC50 value of 0.18 nM against EGFR L858R/T790M double mutations, nearly 43-fold greater potency over wild-type EGFR (IC50 value, 7.68 nM). It has comparable anti-tumor activity and tolerated toxicity. Sep 12 2018
S8724 Lazertinib (YH25448,GNS-1480) Lazertinib (YH25448,GNS-1480) is a potent, highly mutant-selective and irreversible EGFR-TKI with IC50 values of 1.7 nM, 2 nM, 5 nM, 20.6 nM and 76 nM for Del19/T790M, L858R/T790M, Del19, L85R and Wild type EGFR respectively, showing much higher IC50 values aganist ErbB2 and ErbB4. Aug 15 2018
S5272 Toceranib phosphate Toceranib phosphate, the phosphate salt of toceranib, is a selective inhibitor of the tyrosine kinase activity of several members of the split kinase RTK family, including Flk-1/KDR, PDGFR, and Kit with Ki values of 6 nM and 5 nM for Flk-1/KDR and PDGFRβ, respectively. Aug 10 2018
S5240 lenvatinib Mesylate Lenvatinib Mesylate is a synthetic, orally available inhibitor of VEGFR2 tyrosine kinase with potential antineoplastic activity. Aug 10 2018
S5234 Nintedanib Ethanesulfonate Salt Nintedanib is a small molecule tyrosine-kinase inhibitor with IC50 of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β, respectively. Aug 02 2018
Epigenetics
製品コード 製品名称 製品説明 添加時期
S8740 A-485 A-485 is a potent, selective and drug-like p300/CBP catalytic inhibitor with an IC50 of 0.06 μM for p300 HAT. It is selective over BET bromodomain proteins and >150 non-epigenetic targets. Nov 28 2018
S8723 ABBV-744 ABBV-744 is a BDII-selective BET bromodomain inhibitor that inhibits BRD2, BRD3 and BRD4. It is developed for treating AML and cancers. Nov 01 2018
S8409 KG-501 (2-naphthol-AS-E-phosphate) KG-501 is a cAMP response element-binding protein (CREB) inhibitor that disrupts CREB-dependent transcription (Ki = 10 μM) and CREB:CBP interaction (Ki = 50 μM). It also disrupts phospho (Ser-133) CREB binding to KIX with a Ki of ≈90 μM, using concentrations of CREB that were within the linear range of the binding assay. Oct 18 2018
S5438 Biphenyl-4-sulfonyl chloride Biphenyl-4-sulfonyl chloride is a HDAC inhibitor with synthetic applications in palladium-catalyzed desulfitative C-arylation. Jul 12 2018
S5445 AMI-1, free acid AMI-1 is a potent and specific Histone Methyltransferase (HMT) inhibitor with IC50 of 3.0 μM and 8.8 μM for yeast Hmt1p and human PRMT1, respectively. Jul 10 2018
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
NF-κB
製品コード 製品名称 製品説明 添加時期
S8642 GSK'963 GSK'963 is a chiral small-molecule inhibitor of RIP1 kinase with an IC50 of 29 nM in FP binding assays. It is >10 000-fold selective for RIP1 over 339 other kinases. Jul 03 2018
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
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
製品コード 製品名称 製品説明 添加時期
S5539 Olprinone Olprinone is a phosphodiesterase III (PDE3) inhibitor with IC50 values of 0.35 mM, 150 mM and 100 mM for human cardiac PDE III, PDE I and PDE II, respectively. Dec 12 2018
S5713 Pravastatin Pravastatin is a lipoprotein-lowering drug via reversibly inhibiting hydroxymethylglutaryl-CoA (HMG-CoA) reductase and the synthesis of very-low-density lipoproteins. Dec 12 2018
S5715 atorvastatin Atorvastatin is a lipid lowering agent. It is a competitive inhibitor of hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase, the rate-determining enzyme in cholesterol biosynthesis via the mevalonate pathway. Dec 12 2018
S5668 Chlorindione Chlorindione is an antagonist of vitamin K. Dec 06 2018
S5663 Minaprine dihydrochloride Minaprine dihydrochloride is hydrochloride salt form of Minaprine, which acts as a reversible inhibitor of MAO-A in rats and weakly inhibit acetylcholinesterase in rat brain (striatum) homogenates. Dec 06 2018
S5568 Tocofersolan Tocofersolan is a synthetic water-soluble version of vitamin E that is used in treatment of vitamin E deficiency. Nov 30 2018
S8689 RGX-104 RGX-104 is a orally bioavailable liver X receptor agonist that modulates innate immunity via transcriptional activation of the ApoE gene. Nov 28 2018
S5386 7-Dehydrocholesterol 7-Dehydrocholesterol is the direct precursor of free cholesterol in the cholesterol biosynthetic pathway in mammalian tissues and also a biosynthetic precursor to vitamin D3. Nov 28 2018
S8770 Lanifibranor(IVA-337) Lanifibranor (IVA-337) is a moderately potent and well balanced pan PPAR agonist with EC50 values of 1537 nM, 866 nM and 206 nM for hPPARα, hPPARδ and hPPARγ, respectively. Nov 22 2018
S5203 Sulbutiamine Sulbutiamine is a synthetic derivative of thiamine (vitamin B1), belonging to a class of supplements shown to help improve memory, learning capacity, decision-making, concentration, and focus. Sep 19 2018
Proteases
製品コード 製品名称 製品説明 添加時期
S4997 4-Butylresorcinol 4-Butylresorcinol is a potent inhibitor of tyrosinase and is used in cosmetics as a depigmenting agent. Nov 28 2018
S5720 Glecaprevir Glecaprevir is a hepatitis C virus (HCV) nonstructural (NS) protein 3/4A protease inhibitor that targets the the viral RNA replication. It displays IC50 values ranging from 3.5 to 11.3 nM for clinical isolates of HCV genotypes 1a, 1b, 2a, 2b, 3a, 4a, 5a, and 6a. Oct 18 2018
S5652 Elbasvir Elbasvir is an NS5A inhibitor, preventing hepatitis C viral RNA replication and virion assembly. Median EC50 values range from 0.2 to 3600 pmol/L, based on genotype. Sep 11 2018
S5365 Alogliptin Alogliptin is a potent, selective inhibitor of the serine protease dipeptidyl peptidase IV (DPP-4)with IC50 values of 2.63 nM and exhibits greater than 10,000 fold selectivity over the closely related serine proteases DPP-8 and DPP-9. Aug 15 2018
S5543 1, 10-Phenanthroline monohydrate 1,10-Phenanthroline is a classic chelating bidentate ligand for transition metal ions that has played an important role in the development of coordination chemistry. It is an inhibitor of metallopeptidases. Jul 27 2018
S5250 Darunavir Darunavir is a nonpeptidic HIV protease inhibitor, used to treat HIV infection. Jul 04 2018
S5402 Dasabuvir(ABT-333) Dasabuvir(ABT-333) is a non-nucleoside inhibitor of NS5B viral RNA-dependent RNA polymerase that inhibits recombinant NS5B polymerases derived from HCV genotype 1a and 1b clinical isolates with IC50 values between 2.2 and 10.7 nM. It is at least 7,000-fold selective for the inhibition of HCV genotype 1 polymerases over human/mammalian polymerases. Jun 24 2018
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
Microbiology
製品コード 製品名称 製品説明 添加時期
S5491 Lomefloxacin Lomefloxacin is a fluoroquinolone antibiotic used to treat bacterial infections. Dec 12 2018
S5700 Phthalylsulfathiazole Phthalylsulfathiazole is a broad-spectrum antimicrobial that can treat different types of infections including intestinal. Dec 12 2018
S5397 Chlorhexidine Chlorhexidine is a disinfectant and topical anti-infective agent that is active against Gram-positive and Gram-negative organisms, facultative anaerobes, aerobes, and yeasts. Dec 12 2018
S5637 Cefotiam Hexetil Hydrochloride Cefotiam Hexetil Hydrochloride is the hydrochloride salt of cefotiam hexetil. Cefotiam is a semi-synthetic, beta-lactam cephalosporin antibiotic with antibacterial activity. Dec 12 2018
S5704 Myclobutanil Myclobutanil is a widely used triazole fungicide and also a steroid demethylation inhibitor. Dec 12 2018
S5724 Dichlorophene Dichlorophen is an anticestodal agent, fungicide, germicide, and antimicrobial agent. Dec 12 2018
S9377 Eugenyl acetate Eugenyl acetate, an aromatic component of clove essential oil, exhibits various pharmacological activities, including antibacterial and anti-virulence activities against drug-resistant A. baumannii clinical isolates. Dec 12 2018
S9328 5,6,7-Trimethoxyflavone 5,6,7-Trimethoxyflavone, methylations of the hydroxyl groups of oroxylin A or baicalein, has various pharmacological activities including antiviral, anticancer and antibacterial. Dec 07 2018
S9342 1,4-Naphthoquinone 1,4-Naphthoquinone, found in diesel exhaust particles and it is an active metabolite of naphthalene, is a fumigant insecticide. Dec 07 2018
S5625 Ammonium lactate Ammonium lactate is the ammonium salt of lactic acid with mild anti-bacterial properties. Dec 06 2018
Apoptosis
製品コード 製品名称 製品説明 添加時期
S7313 Z-LEHD-FMK Z-LEHD-FMK is a specific, irreversible Caspase-9 inhibitor. Nov 30 2018
S8641 Nec-1s (7-Cl-O-Nec1) Nec-1s is a stable variant of Necrostatin-1. It is a more specific RIPK1 inhibitor lacking the IDO-targeting effect, with >1000-fold more selective for RIPK1 than for any other kinase out of 485 human kinases. Nov 22 2018
S8250 79-6 (CID5721353, BCL6 inhibitor) 79-6 (CID5721353) is a BCL6 inhibitor with Kd value of 138 μM. Jul 25 2018
S8728 PK11007 PK11007 is an anti-p53 drug that stabilizes wild type and mutant p53 via selective alkylation of two surface-exposed cysteines without compromising its DNA binding activity. It exerts antitumor functions not only via reactivating p53 but also via other cellular mechanisms, such as increase of cellular ROS to toxic levels and activation of the UPR. Jul 25 2018
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
MAPK
製品コード 製品名称 製品説明 添加時期
S7965 PLX8394 PLX8394 is a next-generation, orally available, small-molecule BRAF inhibitor with IC50 values of 3.8 nM, 14 nM and 23 nM for BRAF(V600E), WT BRAF and CRAF respectively. It has potential antineoplastic activity. Nov 22 2018
S8745 LXH254 LXH254 is a type II ATP-competitive inhibitor that inhibits both B- and CRAF kinase activities at picomolar concentrations with a high degree of selectivity against a panel of 456 human kinases and in cell-based assays. Oct 10 2018
S5069 Dabrafenib Mesylate Dabrafenib Mesylate is the mesylate salt form of dabrafenib, an orally bioavailable inhibitor of B-raf (BRAF) protein with IC50s of 0.8 nM, 3.2 nM and 5 nM for B-Raf (V600E), B-Raf (WT) and C-Raf, respectively. Jul 12 2018
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
Angiogenesis
製品コード 製品名称 製品説明 添加時期
S8679 BTK inhibitor 1 (Compound 27) BTK inhibitor 1 (compound 27) is an inhibitor of BTK with an IC50 of 0.11 nM for Btk and inhibits B cell activation in hWB with an IC50 of 2 nM. Nov 08 2018
S1711 Crotamiton Crotamiton is a drug that is used as a scabicidal (for treating scabies) and an antipruritic Oct 19 2018
S8700 TP0427736 HCl TP0427736 is a potent inhibitor of ALK5 kinase activity with an IC50 of 2.72 nM and this effect is 300-fold higher than the inhibitory effect on ALK3 (IC50 = 836 nM for ALK3). It also inhibits Smad2/3 phosphorylation in A549 cells induced by TGF-β1 with an IC50 value of 8.68 nM. Sep 27 2018
S5667 Fruquintinib (HMPL-013) Fruquintinib is a small molecule inhibitor with strong potency and high selectivity against VEGFR family. It inhibits VEGFR 1, 2, 3, with IC50 values of 33 nM, 35 nM and 0.5 nM, respectively and shows only weak inhibition of RET, FGFR-1 and c-kit kinases. Sep 27 2018
S5254 Dasatinib hydrochloride Dasatinib hydrochloride is the hydrochloride salt form of dasatinib, an inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM in cell-free assays, respectively. Sep 19 2018
S5205 Nilotinib hydrochloride Nilotinib hydrochloride is the hydrochloride salt form of nilotinib, an orally bioavailable Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity. Aug 10 2018
S8711 ARQ 531 ARQ 531 is an ATP-competitive tyrosine kinase inhibitor designed to target BTK with an IC50 of 0.85 nM. It also has a distinct kinase selectivity profile with strong inhibitory activity against several key oncogenic drivers from TEC, Trk and Src family kinases. Aug 09 2018
S5321 Y15 Y15 is a small-molecule FAK scaffolding inhibitor that directly inhibits FAK autophosphorylation in a dose- and time-dependent manner. Jun 28 2018
S8542 Zanubrutinib (BGB-3111) 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
Stem Cells & Wnt
製品コード 製品名称 製品説明 添加時期
S5439 5-Bromoindole 5-bromoindole is an important pharmaceutical chemical intermediate and a potential inhibitor of glycogen synthase kinase 3 (GSK-3). Jul 12 2018
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
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
Neuronal Signaling
製品コード 製品名称 製品説明 添加時期
S5565 Triflupromazine hydrochloride Triflupromazine hydrochloride is an antipsychotic medication of the phenothiazine class. Dec 12 2018
S5703 Carvedilol Phosphate Carvedilol Phosphate is the phosphate salt form of carvedilol, a racemic mixture and adrenergic blocking agent with antihypertensive activity and devoid of intrinsic sympathomimetic activity. Dec 12 2018
S5398 Nefazodone hydrochloride Nefazodone hydrochloride is the hydrochloride salt form of nefazodone, which is an atypical antidepressant showing antagonistic activity on serotonin reuptake. Dec 12 2018
S5693 Levomilnacipran Hydrochloride Levomilnacipran Hydrochloride is a selective serotonin and norepinephrine reuptake inhibitor with antidepressant activity. Dec 12 2018
S5723 Carvedilol EP IMpurity E Carvedilol is a nonselective beta blocker/alpha-1 blocker and used in management of congestive heart failure (CHF). Dec 12 2018
S5683 Isoproterenol sulfate dihydrate Isoproterenol Sulfate is the sulfate salt form of isoproterenol, a beta-adrenergic receptor agonist with bronchodilator activity. Dec 06 2018
S5670 Chloropyramine hydrochloride Chloropyramine hydrochloride is a histamine receptor H1 antagonist and has anti-cholinergic, antispasmodic, and antiallergic effects. Dec 06 2018
S5666 Moxisylyte hydrochloride Moxisylyte hydrochloride is an alpha-adrenergic blocking agent used for the treatment of Raynaud's disease. Dec 06 2018
S5679 Dolasetron Mesylate Dolasetron Mesylate is a serotonin 5-HT3 receptor antagonist used to treat nausea and vomiting following chemotherapy. Dec 06 2018
S5619 Betahistine Betahistine is an antivertigo drug that primarily acts as a histamine H1 agonist. Dec 06 2018
その他
製品コード 製品名称 製品説明 添加時期
S9452 10-Undecenoic acid 10-Undecenoic acid, a natural or synthetic fungistatic fatty acid, is used for the preparation of active pharmaceutical ingredients, cosmetics, perfumes, antidandruff shampoos and antimicrobial powders. Dec 12 2018
S5697 Isopropamide Iodide Isopropamide iodide is a long-acting quaternary anticholinergic drug used in the treatment of peptic ulcer and other gastrointestinal disorders. Dec 12 2018
S5371 Ajmaline Ajmaline, found in the root of Rauwolfia serpentina, is a class Ia antiarrhythmic agent. Dec 12 2018
S5372 Methyl Aminolevulinate Hydrochloride Methyl Aminolevulinate is a prodrug that is metabolised to protoporphyrin IX used in photodynamic therapy. Dec 12 2018
S5581 Olmesartan Olmesartan is an an angiotensin 2 receptor antagonist with antihypertensive activity. Dec 12 2018
S9320 Efetaal Efetaal has a fresh floral hyacinth note with a suggestion of muguet and green leaves. Dec 12 2018
S8789 SSE15206 SSE15206 is a tubulin polymerization inhibitor that has potent antiproliferative activities in cancer cell lines of different origins and overcomes resistance to microtubule-targeting agents. Dec 12 2018
S9451 Uridine 5'-monophosphate Uridine 5'-monophosphate is a nucleotide that is used as a monomer in RNA. Dec 12 2018
S9449 Urocanic acid Urocanic acid is an intermediate in the catabolism of L-histidine. Dec 12 2018
S5758 2-Methoxycinnamic acid 2-Methoxycinnamic acid is a cinnamic acid with magnetic properties. Dec 12 2018
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誠に勝手ながら、弊社では下記の期間を年末年始による休業とさせていただきます。
【休業期間】
2018年12月29日(土)から2019年1月6日(日)
休業期間中にいただきましたお問合せ等につきましては、2019年1月7日(月)以降の対応とさせていただきます。また、年内の出荷業務は2018年12月26日(水)までとさせていただきます。
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