LDN-192960,184582-62-5

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LDN-192960

CAS No. : 184582-62-5

MCE 国际站：LDN-192960

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

研究领域：Cell Cycle/DNA Damage  |  Protein Tyrosine Kinase/RTK

作用靶点：Haspin Kinase  |  DYRK

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).
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.
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.

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