新产品 按时间排序

PI3K/Akt/mTOR
目录号 产品名 产品描述 上架时间
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)是一种有效的、选择性的PI3Kδ/γ抑制剂,对PI3Kδ和PI3Kγ的IC50值分别为24.5 nM和33.2 nM。它对δ/γ的选择性比对α和β亚型高300倍和100倍以上。 May 11 2018
S7335 IPI-3063 IPI-3063是有效的、选择性的p110δ抑制剂,在无细胞实验中,IC50为2.5 ± 1.2 nM。其对其他I型PI3K亚型如p110α, p110β, p110γ的IC50s至少高400倍。 Mar 28 2018
S8335 PF-06409577 PF-06409577是具有口服活性的AMPK激活剂,在TR-FRET实验中,对AMPK α1β1γ1的EC50为7 nM。在patchBclamp实验中,100μM的PF-06409577对hERG没有可观测到的抑制作用,对主要的人源细胞色素P450亚型的微粒体活性也没有抑制活性(IC50 > 100 μM)。 Nov 22 2017
S8581 Serabelisib (INK-1117,MLN-1117,TAK-117) Serabelisib (INK-1117,MLN-1117,TAK-117)是一种有效的、选择性的,可用于口服的PI3Kα抑制剂,IC50为21 nM。对PI3Kα的选择性比对其他I类PI3K家族成员高100倍以上。 Sep 11 2017
S8330 IPI-549 IPI-549是PI3K-γ的有效抑制剂,选择性是对其他脂质和蛋白激酶的100倍以上。生化IC50为16 nM。 Aug 08 2017
S8589 SF2523 SF2523是一种有效的、具有高度选择性的PI3K抑制剂,对PI3Kα, PI3Kγ, DNA-PK, BRD4 和 mTOR的IC50分别为34 nM, 158 nM, 9 nM, 241 nM 和 280 nM。 Aug 01 2017
S8317 3BDO 3BDO是一种丁内酯衍生物,可靶向FKBP1A并激活mTOR信号通路,抑制HUVECs自噬。 Jul 26 2017
JAK/STAT
目录号 产品名 产品描述 上架时间
S5243 Ruxolitinib Phosphate Ruxolitinib Phosphate is the phosphate salt form of ruxolitinib, an orally bioavailable Janus-associated kinase (JAK) inhibitor with potential antineoplastic and immunomodulating activities. Jun 28 2018
S7812 Itacitinib (INCB39110) Itacitinib (INCB39110)是Janus-associated kinase 1 (JAK1)的抑制剂,具有口服生物活性和潜在的抗肿瘤活性。 Jun 01 2018
S8685 AS1517499 AS1517499是一种新型有效的STAT6抑制剂,IC50为21 nM。 May 11 2018
S8538 PF-06651600 PF-06651600是JAK3选择性的抑制剂,IC50为33.1 nM。对JAK1、JAK2和TYK2没有活性(IC50 > 10 000 nM)。 Mar 28 2018
S8605 C188-9 C188-9是一种有效的STAT3抑制剂,与STAT3以高亲和力结合,Kd=4.7±0.4 nM。C188-9在小鼠体内耐受良好,具有较好的口服生物利用度,主要富集于肿瘤组织中。 Jan 10 2018
S8541 FM-381 FM-381是JAK3的特异性抑制剂,抑制作用具有可逆性,与JAK3共价结合,IC50为127 pM。对JAK3的选择性分别是对JAK1、JAK2、TYK2的400倍、2700倍、3600倍。 Dec 27 2017
S8561 HJC0152 HJC0152是signal transducer and activator of transcription 3 (STAT3)抑制剂,其溶解度相较于niclosamide有显著的改善。 Sep 19 2017
S7985 PIM447 (LGH447) PIM447是一种新型的、泛PIM激酶抑制剂,对PIM1、PIM2、PIM3的Ki值分别为6 pM、18 pM、9 pM。它还能抑制 GSK3β, PKN1和PKCτ,但抑制效力较小,IC50在1-5 μM范围间。 May 05 2017
S7923 SH5-07 (SH-5-07) SH5-07是一种强效的异羟肟酸类STAT3抑制剂,在体内外具有抗肿瘤活性。 Mar 02 2017
S7769 BP-1-102 BP-1-102是有效的、具有口服生物活性的、选择性STAT3抑制剂,与STAT3结合亲和力Kd为504 nM.在4-6.8 μM时,抑制Stat3与pTyr肽段的相互作用和STAT3的激活。 Feb 22 2017
细胞周期(Cell Cycle)
目录号 产品名 产品描述 上架时间
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,一种含氮的二磷酸盐,是有效的破骨细胞抑制剂,可通过抑制甲戊二羟酸途径的酶、阻止小GTP结合蛋白如Ras和Rho的异戊二烯化来诱导破骨细胞凋亡。 Jun 07 2018
S8699 SNS-314 Mesylate SNS-314 Mesylate是一种有效的,选择性的Aurora AAurora BAurora C抑制剂,IC50分别为9 nM, 31 nM,和3 nM,对Trk A/B, Flt4, Fms, Axl, c-Raf和DDR2作用效果稍弱。 Apr 18 2018
S8652 Skp2 inhibitor C1 (SKPin C1) Skp2 inhibitor C1 (SKPin C1)是一种高选择性的Skp2-mediated p27 degradation小分子抑制剂。 Apr 18 2018
S8662 PTC-028 PTC-028是一种具有生物口服活性的化合物,能够通过翻译落修饰减少BMI-1水平。 Mar 15 2018
S2284 Colchicine Colchicine是一种微管聚合抑制剂, IC50为3 nM。 Dec 04 2017
S8469 CCG-203971 CCG-203971是一种新型的Rho/MRTF/SRF通路抑制剂,对SRE.L.的IC50值为0.64 μM。它可以抑制Rho介导的基因转录。 Nov 22 2017
S8632 Chk2 Inhibitor II (BML-277) Chk2 Inhibitor II (BML-277)是一种Chk2的ATP竞争性抑制剂,IC50为15 nM。它对Chk2的选择性比对Chk1和Cdk1/B激酶高1000倍以上。 Nov 02 2017
DNA损伤(DNA Damage)
目录号 产品名 产品描述 上架时间
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
S8592 Pamiparib (BGB-290) Pamiparib (BGB-290) is a potent and selective inhibitor of PARP1 and PARP2 with IC50 values of 0.83 and 0.11 nM, respectively in biochemical assays. It shows high selectivity over other PARP enzymes. Jul 17 2018
S5293 Nimustine Hydrochloride Nimustine Hydrochloride is the hydrochloride salt of nimustine, a nitrosourea with antineoplastic activity that alkylates and crosslinks DNA, thereby causing DNA fragmentation, inhibition of protein synthesis, and cell death. Jul 04 2018
S5297 Vidarabine monohydrate Vidarabine is a nucleoside antibiotic with antiviral acitivity that interferes with the synthesis of viral DNA. It is used to treat herpes simplex and varicella zoster viruses. Jul 04 2018
S5484 Rimantadine Hydrochloride Rimantadine is an RNA synthesis inhibitor that is used as an antiviral agent in the prophylaxis and treatment of influenza. It works by inhibiting a viral protein called M2, which normally mediates the transport of acid ions across the influenza virion shell. Jun 28 2018
S5059 Pixantrone Maleate Pixantrone是一种新型的aza-anthracenedione化合物,具有抗肿瘤活性。它对topoisomerase II具有弱抑制活性,通过对DNA超甲基化位点烷基化,形成DNA加合物。 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
TGF-beta/smad
目录号 产品名 产品描述 上架时间
S7959 SIS3 HCl SIS3是一种新型的特异性Smad3抑制剂,通过抑制Smad3的磷酸化抑制TGF-β和activin信号,而不影响MAPK/p38, ERK或PI3-kinase信号通路。 Oct 20 2016
S7663 Ruboxistaurin (LY333531 HCl) LY333531是特异性β-蛋白激酶C的抑制剂。能竞争性地、可逆地抑制PKCβ1和PKCβ2,IC50分别为4.7和5.9 nM。 Oct 10 2016
S7627 LDN-214117 LDN-214117是一种有效的选择性 BMP I型受体激酶 ALK2 抑制剂,IC50为 24 nM。 Apr 30 2015
S7624 SD-208 SD-208是一种选择性TGF-βRI (ALK5)抑制剂,with IC50为48 nM,选择性比TGF-βRII高100多倍。 Feb 02 2015
S7658 Kartogenin Kartogenin是一种smad4/smad5通路激活剂,促进多功能间充质干细胞选择性分化为软骨细胞。 Nov 27 2014
S7530 Vactosertib  (TEW-7197) Vactosertib  (TEW-7197) 是一种高效的,选择性的,口服生物有效的TGF-β receptor ALK4/ALK5抑制剂,IC50分别为13 nM 和 11 nM。Phase 1。 Nov 27 2014
S7119 Go6976 Go6976是一种强效的PKC抑制剂,其对PKC (老鼠大脑), PKCα, and PKCβ1的IC50分别为7.9nM,2.3 nM, 和 6.2 nM 。此外,也是JAK2Flt3的强抑制剂。 Sep 15 2014
S1421 Staurosporine Staurosporine是一种有效的PKC抑制剂,在无细胞试验中作用于PKCα,PKCγ 和PKCη,IC50分别为2 nM,5 nM 和 4 nM,对PKCδ(20 nM)和PKCε(73 nM作用较弱,对PKCζ (1086 nM)的活性很低。同时 对其他的激酶PKA, PKG, S6K, CaMKII, 等也显示抑制活性。Phase 3。 Aug 13 2014
S7146 DMH1 DMH1是选择性BMP receptor抑制剂,抑制ALK2,IC50为107.9 nM,对AMPK, ALK5, KDR (VEGFR-2)和PDGFR没有抑制效果。 May 20 2014
S7147 LDN-212854 LDN-212854 是一种强效的选择性BMP receptor抑制剂, 其作用于ALK2的IC50为1.3 nM , 分别超过作用于ALK1, ALK3, ALK4, 和 ALK5的选择性约 2-, 66-, 1641-, 和 7135倍。 May 20 2014
G蛋白偶联受体(GPCR and G P)
目录号 产品名 产品描述 上架时间
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)是一种口服的A2AR拮抗剂,可与人源A2AR结合,Ki值为1.7 nM,对A2AR的选择性是对其他腺苷受体的30倍以上。 Jun 07 2018
S4932 Proxyphylline Proxyphylline是茶碱(theophylline)的衍生物,被用作支气管扩张剂。它能够选择性地拮抗A1 adenosine receptors 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是胰高血糖素样肽-1(GLP-1)的激动剂。 Dec 19 2017
S8575 A2AR antagonist 1 A2AR antagonist 1是有效的A2AR (Adenosine A2A Receptor)拮抗剂,对A2AR和A1R的Ki值分别为4 nM和264 nM。 Nov 15 2017
酪氨酸蛋白激酶
目录号 产品名 产品描述 上架时间
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
S5242 Cediranib Maleate Cediranib Maleate is the maleate salt of Cediranib, which is a potent inhibitor of VEGFR with IC50 of <1 nM and also inhibits Flt1/4 with IC50 of 5 nM/≤3 nM. Jul 26 2018
S5248 Apatinib Apatinib is a potent inhibitor of the VEGF signaling pathway with IC50 values of 1 nM and 13 nM for VEGFR-2 and Ret, respectively. Jul 26 2018
S8721 DCC-2618 DCC-2618 is an orally bioavailable switch pocket control inhibitor of wild-type and mutated forms of KIT and PDGFR with potential antineoplastic activity. It also inhibits several other kinases, including VEGFR2, TIE2, PDGFR-beta and CSF1R, thereby further inhibiting tumor cell growth. Jul 25 2018
表观遗传学(Epigenetics)
目录号 产品名 产品描述 上架时间
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是可逆的、特异的EZH1/2抑制剂。 Apr 12 2018
S7230 UNC0642 UNC0642是一种有效的、选择性的histone methyltransferases G9a/GLP抑制剂,对G9a和GLP的IC50均小于2.5 nM。对G9a和GLP的选择性比其他激酶、GPCRs、转运体和离子通道高300倍以上。 Apr 03 2018
S8479 LLY-283 LLY-283是有效的、选择性的SAM竞争性的化学探针,靶向PRMT5。它抑制PRMT5活性,抑制其对H4R3衍生的肽段底物的甲基化,IC50为20 nM。其对PRMT5的选择性比对其他组蛋白甲基转移酶和非表观遗传靶点的选择性高100倍以上。 Mar 28 2018
S8627 OSS_128167 OSS-128167是一种特异性的SIRT6抑制剂,对SIRT6, SIRT1和SIRT2的IC50分别为89, 1578和751 μM。 Feb 28 2018
S8495 WT161 WT161是有效的、选择性的、具有口服活性的HDAC6抑制剂,对HDAC6、HDAC1和HDAC2的IC50值分别为0.4 nM、8.35 nM和15.4 nM,比对其他HDACs的选择性高100倍以上。 Feb 28 2018
S8071 UNC0638 UNC0638是一种有效的选择性的组蛋白赖氨酸甲基转移酶(HMTase)抑制剂,作用于G9aGLPIC50分别为< 15 nM和19 nM,有效且选择性地作用于多种表观遗传和非表观遗传靶点。 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)是一种具有口服活性的、有效的、选择性protein arginine methyltransferase 5 (PRMT5)抑制剂,在体内外有效地抑制肿瘤生长。 Jan 03 2018
NF-κB
目录号 产品名 产品描述 上架时间
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)是NF-κB的有效抑制剂,抑制IκB磷酸化、阻止NF-κB易位入核并减少下游细胞因子的表达。 Nov 15 2017
S8261 GSK583 GSK583是一种高度有效的、选择性的RIP2激酶抑制剂,IC50为5 nM。 Feb 09 2017
S4712 Diethylmaleate Diethylmaleate是Nrf2的激活剂,是马来酸的二乙酯形式,能消耗谷胱甘肽并抑制NFkB。 Oct 26 2016
S7948 MRT67307 HCl MRT67307是一种高效的双重的IKKϵ /TBK1抑制剂,其IC50分别为160和19 nM。 Apr 25 2016
S7691 PS-1145 PS-1145是一种特异性IKK抑制剂,IC50 为 88 nM。 Mar 09 2016
S7851 AZD3264 AZD3264是一种新型IKK2抑制剂。 Nov 27 2015
S7672 Omaveloxolone (RTA-408) Omaveloxolone (RTA-408)是一种合成的三萜类化合物,其激活细胞保护转录因子 Nrf2 并抑制 NF-κB 信号。Phase 2。 Sep 14 2015
S7697 LY2409881 LY2409881 是一种有效的选择性 IKK2 抑制剂,IC50 为 30 nM,选择性比IKK1和其他常见激酶高10倍多。 Apr 20 2015
S7441 WS3 WS3是一种β细胞增殖诱导剂,通过调节Erb3 binding protein-1 (EBP1)IκB kinase通路发挥作用。 Dec 04 2014
新陈代谢(Metabolism)
目录号 产品名 产品描述 上架时间
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
S8733 Tropifexor (LJN452) Tropifexor (LJN452) is a novel and highly potent agonist of FXR with EC50 of 0.2 nM in HTRF assay. It shows no significant off-target activity against a broad panel of enzyme, ion channel, nuclear receptor, and GPCR (>10000-fold selectivity for FXR). Sep 12 2018
S4698 Vitamin K1 Vitamin K1, made by plants, is a major type of dietary vitamin K, which is well-known for its role in blood clotting. Vitamin K1 is directly involved in photosynthesis. Sep 11 2018
S5708 Edoxaban tosylate Monohydrate Edoxaban Tosylate is the tosylate salt form of edoxaban, an orally active inhibitor of factor Xa with anticoagulant activity. Aug 30 2018
S5357 Safinamide Safinamide is an orally active, selective, reversible monoamine oxidase-B inhibitor with both dopaminergic and non-dopaminergic (glutamatergic) properties. The IC50 value of safinamide for MAO-B is 98 nM. Aug 10 2018
S5265 TBB TBB (4,5,6,7-tetrabromobenzotriazole) is a selective cell-permeable CK2 inhibitor with IC50 values of 0.9 and 1.6 μM for rat liver and human recombinant CK2 respectively. Aug 10 2018
S5388 Betrixaban   Aug 10 2018
S5389 Betrixaban maleate   Aug 10 2018
S4998 2-Aminobenzenesulfonamide 2-Aminobenzenesulfonamide is an inhibitor of carbonic anhydrase IX. Aug 10 2018
S5615 GW501516 GW501516 is a synthetic PPARδ-specific agonist that displays high affinity for PPARδ (Ki=1.1 nM) with > 1000 fold selectivity over PPARα and PPARγ. Aug 09 2018
蛋白酶体(Proteases)
目录号 产品名 产品描述 上架时间
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 (SYR-322) 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)是NS3/4A抑制剂。 Jun 13 2018
S5403 Ombitasvir (ABT-267) Ombitasvir (ABT-267)是HCV NS5A的抑制剂,具有抗病毒活性。 Jun 13 2018
S5307 PSI-6206 (RO-2433, GS-331007) PSI-6206 (RO-2433, GS-331007)是有效的HCV RNA依赖性RNA聚合酶抑制剂,靶向NS5B聚合酶 Jun 13 2018
S5079 Sitagliptin Sitagliptin是一种具有口服的、具有高度选择性的DPP-4抑制剂,IC50为18 nM。它被用于治疗2型糖尿病。 Jun 08 2018
S5063 Trelagliptin succinate Trelagliptin succinate是DPP-4抑制剂,被用作新型长效药物,用于2型糖尿病的治疗。 Jun 01 2018
微生物学(Microbiology)
目录号 产品名 产品描述 上架时间
S5657 Ertapenem sodium Ertapenem Sodium is the sodium salt of ertapenem, a long-acting, broad-spectrum antibiotic of β-lactam subclass. Sep 11 2018
S4986 Latamoxef sodium Latamoxef sodium is an antibiotic and has anti-bacterial and anti-inflammation effects. Sep 11 2018
S5394 Tizoxanide Tizoxanide, a thiazolide anti-infective, is active against anaerobic bacteria, protozoa, and a range of viruses in cell culture models, and is currently in phase II clinical development for treating chronic hepatitis C. Aug 30 2018
S5353 Cefpiramide sodium Cefpiramide sodium(SM-1652,wy-44635) is an anionic β-lactam antibiotic. It exhibits antibacterial activity against gram-positive and gram-negative bacteria, in particular, to Pseudomonas aeruginosa, which can result in achronic life-threatening infection in the lungs of cystic fibrosis patients. Aug 15 2018
S5352 Cefminox Sodium Cefminox Sodium is the sodium salt form of cefminox, a semi-synthetic, second-generation, beta-lactamase-stable cephalosporin with antibacterial activity. Aug 10 2018
S5356 Ceftiofur Ceftiofur is a semisynthetic, beta-lactamase-stable, broad-spectrum cephalosporin with antibacterial activity. Aug 10 2018
S5411 Sultamicillin Sultamicillin is a newly developed antibiotic in which ampicillin and the β-lactamase inhibitor sulbactam are linked as an ester. Aug 10 2018
S3966 Nifuratel Nifuratel is a nitrofuran derivative with local antiprotozoal and antifungal activity and a broad spectrum of antibacterial action. Aug 10 2018
S5354 Cefteram pivoxil Cefteram Pivoxil is the pivalate ester prodrug of cefteram, a semi-synthetic, broad-spectrum, third-generation cephalosporin with antibacterial activity. Aug 10 2018
S5351 Cefmetazole sodium Cefmetazole sodium is a semisynthetic cephamycin antibiotic with a broad spectrum of activity against both gram-positive and gram-negative microorganisms. Aug 10 2018
细胞凋亡(Apoptosis)
目录号 产品名 产品描述 上架时间
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是一种新型的、高效的、选择性的p53-Mdm2 interaction抑制剂,对Mdm2的亲合常数在皮摩尔范围内,对Mdm2的选择性是对Mdm4的1000倍以上。 Apr 18 2018
S8650 BTSA1 BTSA1是BAX激活剂,与其N端激活位点以高亲和力和特异性结合,诱导BAX发生构象变化,引起BAC介导的凋亡反应。BTSA1在白血病细胞系和病患样本中有效地促进凋亡,而不影响健康细胞。 Feb 28 2018
S8483 CBL0137 (CBL-0137) CBL0137(CBL-0137)激活p53并抑制NF-kB,在细胞实验中,IC50分别为0.37 μM 和 0.47 μM。它还能抑制组蛋白分子伴侣FACT,FACT促进染色质转录复合体的形成。 Jan 16 2018
S8580 COTI-2 COTI-2是一种具有口服活性的第三代胺苯硫脲,是突变型p53的激活剂,具有潜在的抗肿瘤活性。 Dec 19 2017
A2010 Adalimumab Adalimumab是靶向TNF-alpha的人源重组单克隆抗体,抑制TNF-alpha。MW: 144.19 KD。 Nov 16 2017
S8383 S63845 S63845是一种新型的、选择性的MCL-1抑制剂,Kd值为0.19 nM。对其他Bcl-2成员,如Bcl-2或Bcl-xL,没有明显结合能力。 Nov 15 2017
S8304 Azoramide Azoramide是非折叠蛋白质应答UPR的小分子调节剂,可改善内质网蛋白折叠能力,激活ER伴侣蛋白能力,保护蛋白免受内质网应激反应。 Oct 17 2017
S7100 WEHI-539 WEHI-539对BCL-XL具有高亲和力(IC50=1.1 nM)和选择性,能有效地杀伤细胞。它对Bcl-XL的亲和性是对其他BCL-2家族成员的400倍。 Sep 26 2017
MAPK
目录号 产品名 产品描述 上架时间
S5069 Dabrafenib Mesylate Dabrafenib Mesylate is the mesylate salt form of dabrafenib, an orally bioavailable inhibitor of B-raf (BRAF) protein with IC50s of 0.7 nM, 5.2 nM and 6.3 nM for B-Raf (V600E), B-Raf (WT) and C-Raf, respectively. Jul 12 2018
S8690 RAF709 RAF709是有效的B/C RAF抑制剂,对C-RAF和B-RAF的IC50值分别为0.4 nM和1.5 nM。它具有高选择性,在浓度为1 μM时,对BRAF, BRAFV600E 和 CRAF的靶向结合率大于99%,而对DDR1、DDR2、FRK和FDGFRβ的脱靶效应非常少。 May 22 2018
S8534 LY3214996 LY3214996是一种选择性、新型ERK1/2抑制剂,抑制ERK1和ERK2的IC50为5 nM。在具有BRAF和RAS突变的癌细胞系中,它能有效地抑制细胞内p-RSK1。 Nov 02 2017
S7926 Lifirafenib (BGB-283) Lifirafenib (BGB-283)有效地抑制RAF激酶家族和EGFR活性,在生化实验检测中,其对重组BRAF(V600E)激酶区域、EGFR和EGFR(T790M/L858R)突变体的IC50分别为23、29、495 nM。 Sep 19 2017
S7648 OTS964 OTS964是一种有效的TOPK抑制剂,对TOPK具有高的亲和力和选择性,IC50为28 nM。 Apr 21 2017
S8490 Tanzisertib(CC-930) CC-930对依赖于JNK的蛋白质底物c-JunJNK所有亚型的磷酸化具有ATP竞争性抑制作用(Ki(JNK1) = 44 ± 3 nM, IC50(JNK1) = 61 nM, Ki(JNK2) = 6.2 ± 0.6 nM, IC50(JNK2) = 5 nM, IC50(JNK3) = 5 nM),选择性抑制ERK1p38a的IC50分别为0.48 μM和3.4 μM。 Apr 21 2017
S7743 CCT196969 CCT196969是一种新型的、具有口服活性的pan-RAF抑制剂,同时具有抑制SRC的活性。它还能抑制LCK和p38 MAPKs。 Mar 02 2017
S8275 eFT-508 (eFT508) eFT-508 (eFT508)是一种有效的、选择性的MNK1/2的抑制剂,IC50分别为2.4 nM和1 nM。它能减少肿瘤细胞的增殖和肿瘤生长。 Mar 02 2017
S7652 OTS514 hydrochloride OTS514是一种有效的TOPK抑制剂,IC50为2.6 nM. Feb 22 2017
S8125 Pamapimod (R-1503, Ro4402257) Pamapimod (R-1503, Ro4402257)是新型的、选择性的p38 MAPK抑制剂。它能抑制p38α和p38β, IC50分别为0.014±0.002和0.48± 0.04 μM。对p38delta和p38gamma没有活性。 Dec 01 2016
血管生成(Angiogenesis)
目录号 产品名 产品描述 上架时间
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 Btk inhibitor 2 Btk inhibitor 2是BTK抑制剂。 Jun 07 2018
S8555 Asciminib (ABL001) Asciminib(ABL001)是一种有效的、选择性的ABL1变构抑制剂,Kd值为0.5-0.8 nM,与ABL1的十四酰口袋结合。 May 11 2018
S8348 BMS-935177 BMS-935177是一种有效的、可逆的BTK抑制剂,IC50为2.8 nM,具有良好的激酶选择性。它对BTK比对其他激酶如TEC, BMX, ITK, and TXK更有效力,选择性是其5-67倍。 Apr 25 2018
A2006 Bevacizumab Bevacizumab是一种人源化的anti-VEGF单克隆抗体,是VEGF的抑制剂。可与所有人源VEGF-A亚型(和具有生物活性的蛋白水解片段)结合、中和。MW:149 KD。 Nov 16 2017
A2007 Trastuzumab Trastuzumab是人源重组的抗体抑制剂,与HER2的胞外区域相结合。 MW:145.53 KD。 Nov 16 2017
A2008 Pertuzumab Pertuzumab是一种人源单价克隆抗体,抑制HER2二聚化、破坏HER2与其他HER家族成员结合的能力。MW: 148 KD。 Nov 16 2017
Stem Cell & Wnt
目录号 产品名 产品描述 上架时间
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是porcn抑制剂,在培养细胞中进行的Wnt信号报告基因实验中,EC50为80 pM。它能有效地抑制Hela细胞中Dvl2/3的磷酸化。 Jun 01 2018
S8661 CA3 CA3对YAP1/Tead转录活性具有有效的抑制作用,主要靶向高表达YAP1、具有癌症干细胞属性的、难治疗的食管腺癌细胞。 Mar 15 2018
S7160 Glasdegib (PF-04449913) Glasdegib(PF-04449913)是一种强效且口服生物有效的Smoothened (Smo)抑制剂,其IC50为5 nM。Phase 2。 Mar 07 2018
S8647 iCRT3 iCRT3是Wnt/β-catenin信号的拮抗剂,在Wnt responsive STF16-luc reporter assays中IC50为8.2 nM。 Jan 10 2018
S8597 LYN-1604 LYN-1604是一种潜在的ULK1激动剂,在MDA-MB-231细胞中IC50为1.66 μM。它能与野生型ULK1结合,Kd=291.4 nM。与突变型ULK1蛋白ULK1(Y89A)的结合亲和力急剧减小,其Kd值比ULK1、ULK1 (K50A)和ULK1 (L53A)大。 Dec 05 2017
S8644 GNF-6231 GNF-6231是一种有效的、具有口服活性的、选择性的Porcupine抑制剂,其IC50为0.8 nM。 Dec 05 2017
S8554 Super-TDU Super-TDU是靶向YAP-TEADs interaction的抑制性多肽。 Sep 19 2017
S8572 Amcasertib (BBI503) Amcasertib (BBI503)是一种cancer stemness kinase抑制剂,抑制Nanog和其他癌症干细胞通路,具有潜在的抗癌活性。 Aug 01 2017
S8474 LF3 LF3是一种特异的、对经典Wnt信号通路抑制剂,通过破坏β-catenin和Tcf4的相互作用发挥抑制作用,IC50<2 μM。 Apr 21 2017
Ubiquitin
目录号 产品名 产品描述 上架时间
S5315 PRT4165 PRT4165 is a Bmi1/Ring1A inhibitor with an IC50 of 3.9 µM in the cell-free assay and also inhibits PRC1-mediated H2A ubiquitylation in vivo and in vitro. Jun 24 2018
S8696 2-D08 2-D08是一种具有细胞透性的蛋白类泛素化(protein sumoylation)抑制剂。它还能抑制Axl, IRAK4, ROS1, MLK4, GSK3β, RET, KDR和PI3Kα,IC50分别为0.49, 3.9, 5.3, 9.8, 11, 11, 17和35 nM。 May 24 2018
S7109 Pevonedistat (MLN4924) Pevonedistat (MLN4924)是Nedd8激活酶(NAE)的小分子抑制剂,IC50为4 nM。 Aug 31 2017
S8288 VLX1570 VLX1570是蛋白酶DUB的竞争性抑制剂,在体外IC50值约为10μM。 May 19 2017
S7892 Avadomide(CC-122) CC-122,一种新型的多效性修饰剂化合物,在弥漫性大B细胞淋巴瘤(DLBCL)中具有抗肿瘤、免疫调节活性。其分子靶标为cereblon (CRBN),CRBN是E3泛素化连接酶复合体CRL4CRBN的底物受体。 Mar 31 2017
S4920 b-AP15 b-AP15是一种deubiquitinases(去泛素化酶)抑制剂,识别19S蛋白酶体的,抑制Ub-AMC分解, IC50为2.1 μM。 Mar 30 2015
S7529 ML323 ML323 是强效的选择性的USP1-UAF1抑制剂,其IC50为76 nM。 Jun 30 2014
S7142 NSC697923 NSC697923 是一种细胞选择透过性Ub-conjugating enzyme (E2)复合Ubc13-Uev1A 抑制剂. Apr 09 2014
S7285 NMS-873 NMS-873是特异性p97的变构抑制剂,IC50=30nM,对VCP/p97的选择性相对于对其他AAA ATPase、Hsp90和其他所检测激酶较高。 Jan 29 2014
S7199 DBeQ DBeQ是一种选择性的,有效的,可逆的,ATP竞争性的p97抑制剂,IC50为1.5 μM。 Jul 19 2013
Neuronal Signaling
目录号 产品名 产品描述 上架时间
S4281 Tasimelteon Tasimelteon is a selective dual melatonin receptor (MT1/MT2) agonist with 2.1-4.4 times greater affinity for the MT2 receptor believed to mediate circadian rhythm phase-shifting (Ki = 0.0692 nM and Ki = 0.17 nM in NIH-3T3 and CHOeK1 cells, respectively), than for the MT1 receptor (Ki = 0.304 nM and Ki = 0.35 nM, respectively). Sep 19 2018
S5217 Arformoterol Tartrate Arformoterol Tartrate is the tartrate salt of arformoterol, a long-acting beta-2 adrenergic agonist with bronchodilator activity. Sep 19 2018
S5659 Emedastine Emedastine is a potent, high affinity histamine H1-receptor-selective antagonist with Ki of 1.3 ±0.1 nM for H1-receptors while considerably weaker at H2- (K1 = 49,067 ± 11,113 nM) and H3-receptors (Ki = 12,430 ± 1,282 nM). Sep 11 2018
S5654 Indacaterol Indacaterol is an ultra-long-acting β-adrenoceptor agonist with pKi of 7.36 for β1-adrenoceptor and pKi of 5.48 for β2-adrenoceptor. Sep 11 2018
S5655 Venlafaxine Venlafaxine is an arylalkanolamine serotonin-norepinephrine reuptake inhibitor (SNRI), used to treat major depressive disorder (MDD), generalised anxiety disorder (GAD), panic disorder and social phobia. Sep 11 2018
S5714 lurasidone Lurasidone is a second-generation antipsychotic agent that exhibits full antagonism at dopamine D2 and serotonin 5-HT2A receptors with binding affinities Ki = 1 nM and Ki = 0.5 nM, respectively. It also has high affinity for serotonin 5-HT7 receptors (Ki = 0.5 nM), partial agonist activity at 5-HT1A receptors (Ki = 6.4 nM) and lacks affinity for histamine H1 and muscarinic M1 receptors. Sep 11 2018
S5647 Emedastine Difumarate Emedastine Difumarate is the difumarate salt form of emedastine, a second generation, selective histamine H1 receptor antagonist with anti-allergic activity. Aug 30 2018
S5326 Dolasetron Dolasetron is a highly specific and selective serotonin 5-HT3 receptor antagonist. It has minimal activity at other known serotonin receptors, and has low affinity for dopamine receptors. Aug 10 2018
S5239 Paroxetine mesylate Paroxetine Mesylate is the mesylate salt form of paroxetine, a phenylpiperidine derivative and a selective serotonin reuptake inhibitor (SSRI) with antidepressant and anxiolytic properties. Aug 10 2018
S5267 Nylidrin Hydrochloride Nylidrin Hydrochloride, a β-adrenergic agonist, is used therapeutically for its vasodilating effect on the peripheral circulation and possibly on the cerebral circulation as well. Aug 10 2018
其他
目录号 产品名 产品描述 上架时间
S5726 Triiodothyronine Triiodothyronine is a thyroid hormone that affects various physiological process in the body, including growth and development, metabolism, body temperature, and heart rate. Sep 19 2018
S5685 Desoximetasone Desoximetasone is a synthetic glucocorticoid receptor agonist with metabolic, anti-inflammatory and immunosuppressive activity. Sep 19 2018
S5681 Vinburnine Vinburnine is a vasodilator. It is a vinca alkaloid and a metabolite of vincamine. Sep 19 2018
S5067 Losartan Losartan is a selective, orally administered, nonpeptide blocker of angiotensin II type 1 (AT1) receptor used to treat high blood pressure, diabetic kidney disease, heart failure, and left ventricular enlargement. Sep 19 2018
S2071 Prulifloxacin (NM441, AF 3013) Prulifloxacin是ulifloxacin的前体药物,是一种广谱喹诺酮类抗菌药。 Sep 19 2018
S5728 Delapril Hydrochloride Delapril Hydrochloride is the hydrochloride salt form of delapril, which is a lipophilic, non-sulfhydryl angiotensin-converting enzyme (ACE) inhibitor with antihypertensive activity. Sep 12 2018
S5730 Alimemazine Tartrate Alimemazine is a phenothiazine derivative that is used as an antipruritic. Sep 12 2018
S5672 Hydroxyhexamide Hydroxyhexamide is a pharmacologically active metabolite of acetohexamide, which is a sulfonylurea hypoglycemic agent. Sep 12 2018
S5709 Norgestrel Norgestrel is synthetic steroidal progestin that is used in combination with ethinyl estradiol for oral contraception. It also has strong neuroprotective activity. Sep 11 2018
S8736 Verinurad (RDEA3170) Verinurad (RDEA3170) is a high-affinity inhibitor of the URAT1 transporter with an IC50 of 25 nM for inhibiting transport activity of human URAT1. It inhibits the related URAT1 homologs OAT4 and OAT1 with approximately 200-fold lower affinity compared to URAT1 with IC50 values of 5.9 µM and 4.6 µM, respectively. Sep 11 2018