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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Haspin Kinase-LDN192960 hydrochloride
LDN192960 hydrochloride

Chemical Structure : LDN192960 hydrochloride

CAS No.: 2309172-48-1

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LDN192960 hydrochloride (LDN-192960)

货号: PC-73113Not For Human Use, Lab Use Only.

LDN192960 hydrochloride (LDN-192960) is a highly potent and selective, dual Haspin and DYRK2 inhibitor with IC50 of 10 nM and 48 nM respectively.

规格 价格 库存 数量
5 mg ￥1580 In stock
10 mg ￥2480 In stock
25 mg ￥4280 In stock
50 mg Get quote
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

LDN192960 hydrochloride (LDN-192960) is a highly potent and selective, dual Haspin and DYRK2 inhibitor with IC50 of 10 nM and 48 nM respectively.
LDN192960 suppresses Thr25 RPT3 phosphorylation in a dose-dependent manner in HEK293T cells transiently overexpressing DYRK2-FLAG, with maximal effects at 1-10 uM.
LDN192960 does not inhibit any of the 130+ kinases including other CMGC kinase family members that are closely related to the DYRKs.
LDN192960 binds to the ATP-binding pocket of DYRK2, also potently inhibits DYRK1A, DYRK3 and Pim with IC50 of <3, 122 and 10 nM, respectively.
LDN192960 perturbs proteasome activity, induces cell death, and impedes proliferation and invasion on MDA-MB-468 cells.
LDN192960 impedes MM progression and delays myeloma-mediated bone degeneration.
LDN192960 induces cytotoxicity in bortezomib-resistant MM, both in cells and in vivo. significantly alleviates tumor burden in standard and PDX TNBC models.

物理化学性质&存储条件

分子量 401.35
分子式 C18H22Cl2N2O2S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

3-((2,7-Dimethoxyacridin-9-yl)thio)propan-1-amine dihydrochloride

参考文献

1. Banerjee S, et al. Proc Natl Acad Sci U S A. 2019 Dec 3;116(49):24881-24891.

2. Correa-Sáez A, et al. Cell Mol Life Sci. 2020 Dec;77(23):4747-4763.

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