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

Chemical Structure : LDN192960

CAS No.: 184582-62-5

LDN192960 (LDN-192960, LDN 192960)

货号: PC-21469Not For Human Use, Lab Use Only.

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

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

LDN192960 (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 328.43
分子式 C18H20N2O2S
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

参考文献

1. Banerjee S, et al. Proc Natl Acad Sci U S A. 2019 Dec 3;116(49):24881-24891.
2. Cuny GD, et al. Bioorg Med Chem Lett. 2010 Jun 15;20(12):3491-4.

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