2010年1月至今,引用Selleck产品的顶级学术期刊文献已达篇!

已有十四位诺贝尔奖得主使用Selleck产品发表文献45篇!

David Julius

2021年获得诺贝尔生理学或医学奖


Michael Houghton

2020年获得诺贝尔生理学或医学奖


James P. Allison

2018年获得诺贝尔生理学或医学奖


Michael Rosbash

2017年获得诺贝尔生理学或医学奖


Eric Richard Kandel

2000年获得诺贝尔生理学或医学奖


Brian K. Kobilka

2012年获得诺贝尔化学奖


Robert Lefkowitz

2012年获得诺贝尔化学奖


Aaron Ciechanover

2004年获得诺贝尔化学奖


化合物库

FDA 药物库


3035种获得上市批准的原料药的独特集合,可用于高通量筛选和高内涵筛选 。

临床I期后及FDA药物库


3372种已经上市或通过临床I期的药物集合,可用于高通量筛选(HTS)和高内涵筛选(HCS)。

临床前和临床药物库


提供3102种临床前和临床药物,可用于高通量筛选和高内涵筛选。

已知活性药物库-I


8270种具有生物活性的化合物的独特集合,可用于高通量筛选和高内涵筛选。

生物活性库Ⅱ


5309种具有生物活性的化合物的独特集合,可用于高通量筛选和高内涵筛选。

激酶抑制剂库


1814种激酶抑制剂的独特集合,可用于高通量筛选和高内涵筛选。

多样性化合物母核库


具有不同的核心结构的3010种化合物的独特集合,适用于高通量筛选(HTS)和高含量筛选(HCS)。

天然产物库


2661种天然产物的独特集合,可用于高通量筛选和高内涵筛选。

人内源代谢化合物库


提供1063种人类内源代谢物小分子集合,涉及多个代谢通路,可用于高通量筛选和高内涵筛选,为人类开辟肿瘤等多种疾病治疗的新途径

生物碱类化合物库


413种生物碱类化合物的独特集合,用于高通量筛选(HTS)和高内涵筛选(HCS)。

新产品

G150


G150 is a potent and highly selective human cyclic GMP-AMP synthase (h-cGAS) inhibitor with IC50 of 10.2 nM.

TH5487


TH5487 is a selective active-site inhibitor of 8-oxoguanine DNA glycosylase 1 (OGG1) with IC50 of 342 nM.

KGA-2727


KGA-2727 is a potent, selective, high-affinity inhibitor of sodium glucose cotransporter 1 (SGLT1) with Ki of 97.4 nM and 43.5 nM for human SGLT1 and rat SGLT1, respectively. The selectivity ratios (Ki for SGLT2/Ki for SGLT1) of KGA-2727 are 140 (human) and 390 (rat). KGA-2727 exhibits antidiabetic efficacy in rodent models.

Mizagliflozin


Mizagliflozin is a novel, potent, selective sodium glucose co-transporter 1 (SGLT1) inhibitor with Ki of 27 nM for human SGLT1. The selectivity ratio (Ki value for human SGLT2/Ki value for human SGLT1) of mizagliflozin is 303. Mizagliflozin shows the potential use for the amelioration of chronic constipation.

Guadecitabine (SGI-110)


Guadecitabine (SGI-110) is a next-generation hypomethylating agent whose active metabolite decitabine has a longer in-vivo exposure time than intravenous decitabine.

CM272


CM-272 is a novel first-in-class dual reversible inhibitor of G9a (GLP) and DNMTs with IC50 of 8 nM, 382 nM, 85 nM, 1200 nM, 2 nM for G9a, DNMT1, DNMT3A, DNMT3B, GLP, respectively. CM-272 prolongs survival in in vivo models of haematological malignancies by at least in part inducing immunogenic cell death.

Visomitin (SKQ1)


INT-777 (S-EMCA) is a novel potent and selective TGR5 agonist with EC50 values of 0.18 μM, 3.9 μM and 1.45 μM for WT TGR5, TGR5(N76A) and TGR5(Y89F) respectively.

BAY1125976


BAY 1125976 is a selective allosteric AKT1/2 inhibitor,exhibits high efficacy on AKT signaling-dependent tumor growth in mouse models. BAY1125976 inhibits the activity of AKT1 (IC50 = 5.2 nM at 10 µM ATP and 44 nM at 2 mM ATP) and AKT2 (IC50 = 18 nM at 10 µM ATP and 36 nM at 2 mM ATP) very potently.Whereas BAY1125976 is almost inactive on AKT3 (IC50 = 427 nM at 10 µM ATP).

Tags: kinase inhibitors, tyrosine kinase inhibitors, enzyme inhibitors, protein inhibitors, proteins kinase inhibitors, small molecules, phosphatase inhibitors