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


3094种获得上市批准以及药典收录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


3501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3247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


8819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


1930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


2726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1067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


422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