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
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
A5047 PI3 Kinase p85 alpha Rabbit Recombinant mAb   Nov 13 2017
A5048 PI3 Kinase p55 gamma Rabbit Recombinant mAb   Oct 10 2017
A5008 AMPK alpha 1 Rabbit Recombinant mAb   Oct 09 2017
A5012 PRAS40 Rabbit Recombinant mAb   Oct 09 2017
A5023 AKT1 Rabbit Recombinant mAb   Oct 09 2017
A5025 AMPK gamma 1 Rabbit Recombinant mAb   Oct 09 2017
A5030 Phospho-Akt(Ser473) Rabbit Recombinant mAb   Oct 09 2017
A5031 AKT1/2/3 Rabbit Recombinant mAb   Oct 09 2017
A5033 Phospho-S6K1(T421/S424) Rabbit Recombinant mAb   Oct 09 2017
JAK/STAT
目录号 产品名 产品描述 上架时间
A5042 STAT5a Rabbit Recombinant mAb   Oct 10 2017
A5044 STAT2 Rabbit Recombinant mAb   Oct 10 2017
A5045 STAT4 Rabbit Recombinant mAb   Oct 10 2017
A5003 STAT5b Rabbit Recombinant mAb   Oct 09 2017
A5020 STAT5A/B Rabbit Recombinant mAb   Oct 09 2017
A5024 JAK2 Rabbit Recombinant mAb   Oct 09 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
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 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)是一种Chk2的ATP竞争性抑制剂,IC50为15 nM。 Nov 02 2017
A5035 Cyclin D1 Rabbit Recombinant mAb   Oct 10 2017
A5004 Chk1 Rabbit Recombinant mAb   Oct 09 2017
A5011 c-Myc Rabbit Recombinant mAb   Oct 09 2017
A5016 Cyclin B1 Rabbit Recombinant mAb   Oct 09 2017
S8499 KRpep-2d KRpep-2d是选择性的K-Ras(G12D)抑制性环肽,相较于WT K-Ras和K-Ras(G12C),对K-Ras(G12D)选择性更高,IC50为1.6 nM。 Sep 11 2017
S8387 MSC2530818 MSC2530818是一种CDK8抑制剂,IC50为2.6 nM。具有良好的激酶选择性、生化和细胞效力、微粒体稳定性,并具有生物口服活性。 Jul 26 2017
S8520 Senexin A Senexin A是有效的、选择性的CDK8抑制剂,还抑制CDK19Kd值分别为0.83 μM和0.31 μM。 Jul 11 2017
DNA损伤(DNA Damage)
目录号 产品名 产品描述 上架时间
S3669 Carmustine Carmustine是一种细胞周期非特异性烷基化抗肿瘤剂,用于治疗脑瘤及多种其他恶性肿瘤。 Nov 29 2017
A5037 PARP Rabbit Recombinant mAb   Oct 10 2017
A5039 SIRT6 Rabbit Recombinant mAb   Oct 10 2017
A5049 SIRT1 Rabbit Recombinant mAb   Oct 10 2017
A5034 Cleaved PARP Rabbit Recombinant mAb   Oct 09 2017
S8427 LTURM34 LTURM34是特异性的DNA-PK抑制剂,对DNA-PK活性的抑制选择性比对PI3K活性的抑制高170倍,IC50为0.034 μM。 Jun 13 2017
S8539 TAS-102 TAS-102是一种用于口服的、由胸苷核酸类似物trifluridine和胸苷磷酸酶抑制剂tipiracil hydrochloride组合的组合药。 Jun 01 2017
S8379 YU238259 YU238259是一种新型的homology-dependent DNA repair(HDR)抑制剂,在细胞GFP报告基因实验中,发现其不抑制非同源性末端接合NHEJ。 May 10 2017
S8481 SRT3025 HCl SRT3025是一种具有口服活性的SIRT1小分子激活剂。 Apr 27 2017
S8434 B02 B02是一种人源RAD51小分子抑制剂,IC50为27.4 μM,对大肠杆菌中的同系物RecA没有抑制作用(IC50>250 μM)。 Apr 21 2017
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 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 EW-7197 EW-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
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
S8637 Ipragliflozin (ASP1941) Ipragliflozin (ASP1941)是一种高度选择性的sodium-glucose cotransporter 2 (SGLT2)抑制剂,对hSGLT2的IC50值为7.4 nM,对SGLT2的选择性是对SGLT1的选择性的254倍。 Oct 24 2017
S2879 AMD3465 hexahydrobromide AMD3465是一种单一大环类CXCR4的拮抗剂。 Sep 06 2017
S8558 Tofogliflozin(CSG 452) Tofogliflozin是一种新型的sodium-glucose co-transporter 2(SGLT2)抑制剂,对hSGLT2和hSGLT1的IC50值分别为2.9 nM和8444 nM。 Aug 29 2017
S8517 Lixisenatide Lixisenatide是一种短效的(一天一次给药)的glucagon-like peptide-1 (GLP-1) receptor激动剂(GLP-1RA),在受体结合研究中,其对人源GLP-1受体的IC50值为1.4 nM。 Jul 11 2017
S8415 PACAP 1-38 PACAP 1-38是高度有效的PACAP受体激动剂(Kd=100 pM),能够刺激腺苷酸环化酶和吞噬作用。 Mar 31 2017
S8416 PACAP 6-38 PACAP 6-38 是PACAP (pituitary adenylate cyclase-activating polypeptide)的非刺激性竞争性拮抗剂,IC50为2 nM。在体内,它还能作为功能性的CARTp拮抗剂。 Mar 31 2017
S7182 JTE 013 JTE-013是sphingosine 1-phosphate receptor 2(S1P2)拮抗剂(IC50=17.6 nM)。在超过10 μM的浓度下,对S1P1或S1P3没有作用。在HTC4细胞中,JTE-013拮抗S1P4的Ki值为237 nM。 Mar 31 2017
S8414 PACAP 1-27 垂体腺苷环化酶激活肽(PACAP 1-27)是有效的PACAP受体拮抗剂。 Feb 22 2017
S8345 ONO-7300243 ONO-7300243是一种新型的、有效的溶血磷脂酸受体LPA1的拮抗剂,IC50为160 nM。 Dec 08 2016
酪氨酸蛋白激酶
目录号 产品名 产品描述 上架时间
S8553 Avapritinib (BLU-285) Avapritinib (BLU-285)是一种小分子激酶抑制剂,可有效抑制PDGFRα D842V突变体的活性、在细胞背景下抑制PDGFRα D842V自我磷酸化(IC50=30 nM);同时也是KIT突变(KIT D816V)的抑制剂(IC50=0.5 nM)。 Oct 24 2017
S7754 Gilteritinib (ASP2215) Gilteritinib(ASP2215)是小分子FLT3/AXL抑制剂,对FLT3和AXL的IC50值为0.29 nM和0.73 nM。其抑制c-KIT的IC50值约为抑制FLT3的800倍。 Oct 17 2017
A5006 Met (c-Met) Rabbit Recombinant mAb   Oct 09 2017
S8511 Belizatinib (TSR-011) Belizatinib (TSR-011)是一种有效的ALK(IC50=0.7 nM)和tropomyosin receptor kinase (TRK) (IC50<3 nM)抑制剂。 Sep 19 2017
S8407 PF-06273340 PF-06273340是一种高度有效的、具有激酶选择性的、耐受良好的泛Trk抑制剂,对TrkA、TrkB、TrkC的IC50值分别为6 nM、4 nM、3 nM。 Aug 29 2017
S8583 TPX-0005 TPX-0005是一种新型的ALK/ROS1/TRK抑制剂,对WT ALKALK(G1202R)ALK(L1196M)的IC50分别为1.01 nM、1.26 nM、1.08 nM;同时也是一种有效的SRC抑制剂,IC50为5.3 nM。 Aug 01 2017
S8573 Sitravatinib (MGCD516) Sitravatinib (MGCD516)是一种新型的、靶向多种参与调节S180肉瘤细胞生长的RTKs的小分子抑制剂,包括c-Kit, PDGFRβ, PDGFRα, c-Met和Axl。 Jul 26 2017
S2752 HER2-Inhibitor-1 HER2-Inhibitor-1是一种有效的,选择性的HER2抑制剂,IC50为8 nM,等效作用于截短的p95-HER2,作用于HER2比作用于EGFR选择性高500倍。Phase 1。 Jul 13 2017
S8570 RXDX-106 (CEP-40783) RXDX-106 (CEP-40783)是一种可口服的、有效的、选择性的TAM(TYRO3, AXL, MER)/MET抑制剂,在肽段磷酸化实验中具有较低的纳摩尔级别生化活性;在体外激酶结合试验中具有慢速的解离率(T1/2 >120 min)。 Jul 11 2017
S8518 AD80 AD80,一种多激酶抑制剂,对人源RETBRAFS6KSRC活性较强,但对mTOR的活性比AD57或AD58弱。其对RET的IC50值为4 nM。 Jul 03 2017
表观遗传学(Epigenetics)
目录号 产品名 产品描述 上架时间
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是一种环肽,能够抑制JmjC histone demethylases KDM4,对KDM4AKDM4C的IC50分别为42 nM和29 nM。 Nov 07 2017
S8624 JNJ-64619178 JNJ-64619178是PRMT5抑制剂,具有较高的选择性和效力(PRMT5-MEP-50, IC50=0.14 nM)、良好的药代动力学特性以及安全性。 Nov 02 2017
S8494 PF-06726304 PF-06726304是选择性EZH2抑制剂,对WT EZH2和EZH2(Y641N)的Ki值分别为0.7 nM和3 nM。抑制H3K27me3的IC50为15 nM。 Oct 24 2017
S8567 Tucidinostat (Chidamide) Chidamide是HDAC1, 2, 3, 10的低摩尔浓度抑制剂,IC50分别为95、160、67、78 nM。 Oct 17 2017
A5041 ATF2 Rabbit Recombinant mAb   Oct 10 2017
A5000 HDAC2 Rabbit Recombinant mAb   Oct 09 2017
A5014 CREB Rabbit Recombinant mAb   Oct 09 2017
A5021 HDAC6 Rabbit Recombinant mAb   Oct 09 2017
S8502 TMP195 TMP195是一种选择性的class IIa HDAC抑制剂,在基于细胞的实验中,IC50为300 nM。 Jul 19 2017
NF-κB
目录号 产品名 产品描述 上架时间
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
S7442 WS6 WS6通过调节Erb3 binding protein-1 (EBP1)IκB kinase通路诱导β细胞增殖。 Nov 12 2014
新陈代谢(Metabolism)
目录号 产品名 产品描述 上架时间
S3720 Elafibranor Elafibranor is an agonist of the peroxisome proliferator-activated receptor-α(PPAR-alpha) and peroxisome proliferator-activated receptor-δ(PPAR-δ). It improves insulin sensitivity, glucose homeostasis, and lipid metabolism and reduces inflammation. Nov 29 2017
S3740 Selegiline HCl Selegiline (L-deprenyl) is a selective, irreversible inhibitor of monoamine oxidase B (MAO-B) with selectivity for MAO-B vs MAO-A and used in the treatment of Parkinson's disease. Nov 29 2017
S3647 Mafenide Acetate Mafenide Acetate is a sulfonamide that inhibits the enzyme carbonic anhydrase and is used as topical anti-infective, especially in burn therapy. Nov 27 2017
S3658 O6-Benzylguanine O6-Benzylguanine (O6-BG) is a potent O6-alkylguanine DNA alkyltransferase (AGT) inactivator. Nov 27 2017
S3673 Sulfaphenazole Sulfaphenazole is an inhibitor of CYP2C9 with Ki value of 0.3 μM and demonstrates at least 100-fold selectivity over other CYP450 isoforms (Ki values of 63 and 29 μM for CYP2C8 and CYP2C18, respectively, and no activity at CYP1A1, CYP1A2, CYP3A4, CYP2C19). Nov 27 2017
S3690 Pargyline hydrochloride Pargyline is an irreversible inhibitor of monoamine oxidase (MAO)-B with Ki values of 13 and 0.5 μM for time-dependent inhibition of the activity of MAO-A and -B, respectivey. Nov 23 2017
S3665 Trolox   Nov 23 2017
S3660 Uniconazole Uniconazole is a plant growth regulator that functions by inhibiting cytochrome P450 707As (Ki = 68 nM), a family of enzymes that catabolize ABA. It suppress gibberellin and sterol biosynthesis. Nov 23 2017
S8616 PKM2 inhibitor(compound 3k) PKM2 inhibitor(Compound 3K) displays PKM2 inhibitory activity with the IC50 value of 2.95 μM. The IC50 value for PKM1 is 4-5-fold higher than that for PKM2. Nov 22 2017
S8588 ACSS2 inhibitor ACSS2 inhibitor是有效的、特异性的乙酰辅酶A合成酶2 (ACSS2)抑制剂。 Nov 15 2017
蛋白酶体(Proteases)
目录号 产品名 产品描述 上架时间
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
S3692 N-Ethylmaleimide (NEM) N-Ethylmaleimide (NEM)是一种来源于马来酸的有机化合物。它是cysteine peptidases的不可逆转性抑制剂,在活性位点硫醇基发生烷化。 Nov 15 2017
S8565 Omarigliptin (MK-3102) Omarigliptin (MK-3102)是一种竞争性的、可逆的DPP-4抑制剂(IC50 = 1.6 nM, Ki = 0.8 nM)。在所有检测的蛋白酶中,包括QPP, FAP, PEP, DPP8和DPP9等,对DPP-4具有高选择性,具有微弱的离子通道活性(IC50 > 30 μM at IKr, Caγ1.2, and Naγ1.5)。 Jul 11 2017
S8457 UK-371804 HCl UK-371804是一种有效的urokinase-type plasmogen activator (uPA)抑制剂,Ki为10 nM,其选择性良好,对uPA的选择性比对tPA高4000倍,比对plasmin高2700倍。 Mar 02 2017
S7420 CA-074 methyl ester (CA-074 Me) CA-074 Me是可透过膜的CA-074的衍生物,是一种不可逆的cathepsin B抑制剂。 Jan 09 2017
S4697 Saxagliptin hydrate Saxagliptin H2O是一种选择性的、可逆的DPP4抑制剂,其IC50为26 nM。 Sep 21 2016
S4636 Teneligliptin hydrobromide Teneligliptin是一种新型的、有效的、长效的dipeptidyl peptidase-4(DPP4)抑制剂。在体外,teneligliptin竞争性地抑制人血浆、大鼠血浆以及人源重组DPP4,IC50约为1 nM。 Sep 21 2016
S4662 Atazanavir Atazanavir是一种氮杂肽及HIV-蛋白酶抑制剂,常与其他抗HIV药物结合,用于治疗HIV感染以及获得性免疫缺乏综合征。 Sep 21 2016
微生物学(Microbiology)
目录号 产品名 产品描述 上架时间
S3707 Ethopabate Ethopabate (ETP) is a coccidiostat that is frequently used to prevent and treat coccidiosis in chickens. Nov 30 2017
S3708 Sulfachloropyridazine Sulfachloropyridazine is an antibiotic used to treat a variety of bacterial infections. Nov 30 2017
S3709 Furagin Furagin is 2-substituted 5-nitrofuran, chemically and structurally similar to well-known antibacterial compound nitrofurantoin with antimicrobial activities. Nov 30 2017
S3746 Lumefantrine Lumefantrine is an antimalarial agent used to treat acute uncomplicated malaria. Nov 30 2017
S3705 Chlorobutanol Chlorobutanol (trichloro-2-methyl-2-propanol)是一种防腐剂、镇静剂、催眠剂和弱的局部麻醉剂,具有抗菌抑菌作用。 Nov 29 2017
S3710 Fosfomycin calcium Fosfomycin是一种杀菌剂,可通过使UDP-N-acetylglucosamine-3-enolpyruvyltransferase失活而一直细菌细胞壁形成。Fosfomycin可通过甘油磷酸盐转运蛋白进入细胞壁。 Nov 29 2017
S3722 Isavuconazole Isavuconazole is a new extended-spectrum triazole with activity against yeasts, molds, and dimorphic fungi that inhibits cytochrome P450 (CYP)-dependent 14α-lanosterol demethylation, which is essential for fungal cell membrane ergosterol synthesis. Nov 29 2017
S3695 Cystamine dihydrochloride Cystamine dihydrochloride acts as an anti-infective agent, which is used in the treatment of urinary tract infections and also as a radiation-protective agent that interferes with sulfhydryl enzymes. Nov 27 2017
S3644 Sulfamonomethoxine   Nov 27 2017
S3649 Ceftazidime Ceftazidime is a third-generation cephalosporin that has activity against Gram-negative bacilli, including Pseudomonas aeruginosa. Nov 27 2017
细胞凋亡(Apoptosis)
目录号 产品名 产品描述 上架时间
A2010 Adalimumab Adalimumab是靶向TNF的人源重组单克隆抗体,抑制TNF。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
A5046 TNF Receptor II Rabbit Recombinant mAb   Oct 10 2017
A5010 Bcl-2 Rabbit Recombinant mAb   Oct 09 2017
A5013 Caspase-3 Rabbit Recombinant mAb   Oct 09 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
S8465 GSK'872 (GSK2399872A) GSK'872 (GSK2399872A)是一种有效的、特异性的RIP3 kinase抑制剂,与RIP3激酶区域以高亲和力结合(IC50为1.8 nM),抑制酶活性的IC50为1.3 nM。仅具微弱交叉反应。 Sep 05 2017
S8591 FX1 FX1是一种选择性的BCL6 BTB抑制剂,IC50为35 μM。在所检测的50多种激酶中,FX1具有高选择性,10 μM的FX1不能显著地抑制这些激酶。 Aug 29 2017
S7126 Marinopyrrole A (Maritoclax) Marinopyrrole A (Maritoclax)是一种选择性的Mcl-1拮抗剂。它能够结合Mcl-1,而不是Bcl-XL,引起其发生蛋白酶体降解。Maritoclax能够破坏Bim和Mcl-1的相互作用,IC50为10.1 μM。 Aug 23 2017
MAPK
目录号 产品名 产品描述 上架时间
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
A5036 Phospho-Erk1(T202/Y204)+Erk2 (T185/Y187) Rabbit Recombinant mAb   Oct 10 2017
A5043 Raf1 Rabbit Recombinant mAb   Oct 10 2017
A5050 MEK3/MEK6 Rabbit Recombinant mAb   Oct 10 2017
A5005 JNK1/2/3 Rabbit Recombinant mAb   Oct 09 2017
A5009 MEK2 Rabbit Recombinant mAb   Oct 09 2017
A5017 p38 MAPK Rabbit Recombinant mAb   Oct 09 2017
A5018 ERK2 Rabbit Recombinant mAb   Oct 09 2017
A5019 MEK1 Rabbit Recombinant mAb   Oct 09 2017
A5026 JNK1/JNK3 Rabbit Recombinant mAb   Oct 09 2017
血管生成(Angiogenesis)
目录号 产品名 产品描述 上架时间
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
S8230 Ensartinib (X-396) Ensartinib (X-396)是一种新型的、有效的、特异的ALK酪氨酸激酶抑制剂,在Ambit assay中对ALK的IC50小于4 nM。 Oct 09 2017
S8578 PRN1371 PRN1371是FGFR1-4的不可逆性共价抑制剂,对于FGFR1, 2, 3, 4和CSF1R的IC50分别为0.6、1.3、4.1、19.3、和8.1 nM。 Sep 26 2017
S8441 LW 6 LW6是hypoxia-inducible factor 1(HIF)抑制剂。在缺氧环境下,LW6能通过降解HIF-1α,从而有效地抑制HIF-1α的积累,不影响HIF-1α mRNA水平。在cell-based HRE-reporter gene assays中,LW6抑制缺氧诱导的HIF-1α转录活性的IC50为2.64 μM。 Sep 19 2017
S8442 TAK-659 TAK-659是一种有效的、选择性的SYK抑制剂。IC50为3.2 nM。对其他激酶具有选择性,对FLT3也能有效抑制,IC50为4.6 nM。 Aug 08 2017
A2000 Cetuximab Cetuximab是一种新型的分子靶向药物,是EGFR的抑制剂,同时也是人源EGFR单克隆抗体,与EGFR的胞外结合区域相互作用并抑制其受配体刺激;MW:145.781 KD。 Jun 02 2017
S8229 Brigatinib (AP26113) Brigatinib (AP26113)是一种有效的、选择性的ALK抑制剂,IC50=0.6 nM;也是ROS1抑制剂,IC50=0.9 nM。它还能以相对较低的效力抑制FLT3、FLT3(D835Y)、EGFR。 May 10 2017
S8523 GSK2256098 GSK2256098是一种有效的、选择性的、可逆的、ATP竞争性的FAK kinase抑制剂,apparent Ki为0.4 nM。 Apr 27 2017
Stem Cell & Wnt
目录号 产品名 产品描述 上架时间
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
A5038 Beta Catenin Rabbit Recombinant mAb   Oct 10 2017
A5007 GSK3 beta Rabbit Recombinant mAb   Oct 09 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
S7954 CP21R7 (CP21) CP21R7(CP21)是一种有效的、选择性的GSK-3β抑制剂,能有效激活经典Wnt信号通路。 Mar 31 2017
S8392 NCB-0846 NCB-0846是一种新型的、口服的Wnt小分子化合物抑制剂,抑制TNIK (TRAF2 and NCK-Interacting Kinase)的IC50为21 nM。 Mar 31 2017
S8429 PNU-74654 PNU-75654通过抑制β-catenin和Tcf4的相互作用(Kd=450 nM),破坏Wnt signaling pathway Mar 02 2017
Ubiquitin
目录号 产品名 产品描述 上架时间
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
S4921 MNS (3,4-Methylenedioxy-β-nitrostyrene, MDBN) MNS (3,4-Methylenedioxy-β-nitrostyrene, MDBN)是一种酪氨酸激酶抑制剂,抑制SykSrcp97IC50分别为2.5 μM, 29.3 μM和1.7 μM。 Jul 19 2013
S7129 PYR-41 PYR-41是第一个泛素激活酶E1的细胞渗透性抑制剂,对E2没有活性。 Jul 19 2013
Neuronal Signaling
目录号 产品名 产品描述 上架时间
S3706 Sarpogrelate hydrochloride Sarpogrelate is a selective 5-HT2A antagonist with pKi values of 8.52, 7.43 and 6.57 for 5-HT2A, 5-HT2C and 5-HT2B receptors respectively. Nov 30 2017
S3716 Flibanserin Flibanserin is a nonhormonal, centrally acting molecule that acts as an agonist at postsynaptic 5-HT1A receptors and as an antagonist at 5-HT2A receptors. Nov 30 2017
S3721 Bilastine Bilastine is a new, well-tolerated, nonsedating H1 receptor antihistamine and has a rapid onset and prolonged duration of action. Nov 29 2017
S3723 Ramosetron Hydrochloride Ramosetron Hydrochloride is the hydrochloride salt of ramosetron, a selective serotonin (5-HT) receptor antagonist with potential antiemetic activity. Nov 29 2017
S3735 Umeclidinium bromide Umeclidinium bromide is a long-acting muscarinic antagonist approved for the maintenance treatment of chronic obstructive pulmonary disease (COPD). Nov 29 2017
S3737 Cangrelor Tetrasodium Cangrelor是一种有效的、竞争性的P2Y12 receptor抑制剂,可通过静脉注射、抑制ADP诱导的血小板凝集。 Nov 29 2017
S3640 Methoxyphenamine Hydrochloride Methoxyphenamine Hydrochloride is a β-adrenergic receptor agonist of the amphetamine class used as a bronchodilator. Nov 27 2017
S3727 Vilanterol Trifenate Vilanterol trifenatate is a novel inhaled long-acting beta2 adrenoceptor agonist with inherent 24-hour activity for once daily treatment of COPD and asthma. Nov 27 2017
S3656 Piribedil Piribedil is a relatively selective dopamine (D2/D3) agonist with moderate antidepressant activity. It also has α2-adrenergic (α2A/α2C) antagonist properties. Nov 27 2017
S3662 Pirenzepine dihydrochloride Pirenzepine is an antimuscarinic agent which inhibits gastric acid secretion at lower doses than are required to affect gastrointestinal motility, salivary, central nervous system, cardiovascular, ocular and urinary functions. Nov 27 2017
其他
目录号 产品名 产品描述 上架时间
S3694 Glucosamine hydrochloride Glucosamine is a natural constituent of glycosaminoglycans in the cartilage matrix and synovial fluid, also presents in the shells of shellfish, animal bones, bone marrow, and fungi. Glucosamine is commonly used as a treatment for osteoarthritis, although its acceptance as a medical therapy varies. Dec 05 2017
S3712 Tulathromycin A Tulathromycin A is a novel long-acting semi-synthetic tribasic macyocyclic antibiotic of the triamilide group and used for the treatment of pulmonary diseases of swine and cattle. Dec 05 2017
S3738 Travoprost Travoprost is a PGF2a analog that was launched as an ophthalmic solution administered topically for the treatment of elevated intraocular hypertension as a result of open-angle glaucoma, a common optic neuropathy, and a leading cause of blindness. Dec 05 2017
S3739 Calcipotriene Calcipotriene is a synthetic derivative of calcitriol, a form of vitamin D. It can induce differentiation and suppresses proliferation of keratinocytes, reversing abnormal keratinocyte changes in psoriasis, and lead to normalization of epidermal growth. Dec 05 2017
S3628 BHQ BHQ is a potent and selective inhibitor of the sarco-endoplasmic reticulum Ca2+-ATPase (SERCA). Dec 05 2017
S3715 Boldenone Undecylenate Boldenone is an agonist of the androgen receptor (AR). Boldenone Undecylenate is a derivative of testosterone, which has strong anabolic effect and only moderately androgenic. Dec 05 2017
S3730 Metaxalone Metaxalone is a muscle relaxant used to relax muscles and relieve pain caused by strains, sprains, and other musculoskeletal conditions. Dec 05 2017
S3750 Sodium benzoate Sodium benzoate is a preservative and uesd as a food additive which is bacteriostatic and fungistatic under acidic conditions. Dec 05 2017
S3642 Cesium chloride Cesium chloride is the inorganic compound. It is widely used medicine structure in isopycnic centrifugation for separating various types of DNA and is a reagent in analytical chemistry. Dec 05 2017
S2378 Butylscopolamine Bromide Butylscopolamine Bromide是一种外周性的抗毒蕈碱,抗胆碱的药剂,用作腹部特定的解痉药。 Dec 04 2017