LDN-192960

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

LDN-192960  纯度: 99.56%

LDN-192960 是 Haspin 和 DYRK2 的双重抑制剂，IC50 值分别为 10 nM 和 48 nM。

LDN-192960

LDN-192960 Chemical Structure

CAS No. : 184582-62-5

规格 价格 是否有货
5 mg ￥3500 询问价格 & 货期
10 mg ￥5500 询问价格 & 货期

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LDN-192960 的其他形式现货产品:

LDN-192960 hydrochloride

生物活性

LDN-192960 is an inhibitor of Haspin and Dual-specificity Tyrosine-regulated Kinase 2 (DYRK2) with IC50s of 10 nM and 48 nM, respectively[1].

IC50 & Target

IC50: 10 nM (Haspin); 48 nM (DYRK2)[1]
体外研究
(In Vitro)

LDN-192960 (10 μM) is selective and inhibits ten of the other kinases by ≥90%, with only five being potently inhibited (IC50<1 μm), including clk1 (ic50=0.21 μM), DYRK1A (IC50= 0.10 μM), DYRK2 (IC50=2 nM), DYRK3 (IC50=19 nM) and PIM1 (IC50=0.72 μM)[1].
LDN-0192960 (0-5 μM; 2 hours) demonstrates that the classical Haspin inhibition phenotype by reducing levels of p-Thr3H3 in HeLa cells overexpressing Haspin with an EC50 of 1.17 μM[2].
LDN-0192960 (0-1 μM; 1 hour incubation in the presence of nocodazole and MG132) demonstrates the classical Haspin inhibition phenotype by reducing levels of p-Thr3H3 in HeLa cells synchronized in mitosis with an EC50 of 0.02 μM[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

328.43

Formula

C18H20N2O2S
CAS 号

184582-62-5
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
参考文献

  • [1]. Cuny GD, et al. Structure-activity relationship study of acridine analogs as haspin and DYRK2 kinase inhibitors. Bioorg Med Chem Lett. 2010 Jun 15;20(12):3491-4.

    [2]. Katrin Kestav, et al. Structure, Roles and Inhibitors of a Mitotic Protein Kinase Haspin. Curr Med Chem. 2017;24(21):2276-2293.

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