CHR-6494

Short Summary : Haspin inhibitor,potent ands selective

Category : Cell Cycle/Checkpoint|Haspin

Purity : 0.98

CAS Number : 1333377-65-3

Formula : C16H16N6

Molecular Weight : 292.34

SMILE : CCCNC1=NN2C(=NC=C2C3=CC4=C(C=C3)NN=C4)C=C1

Solubility : Soluble in DMSO

Storage : Store at -20°C

Description : Haspin is a serine/threonine kinase that phosphorylates Thr-3 of histone H3 in mitosis that has emerged as a possible cancer therapeutic target. CHR-6494 is a first-in-class Haspin inhibitor with a wide spectrum of anticancer effects. Recent research showed that CHR-6494 reduces H3T3ph levels in a dose-dependent manner and causes a mitotic catastrophe characterized by metaphase misalignment, spindle abnormalities and centrosome amplification. From the cellular standpoint, the identified small-molecule Haspin inhibitor causes arrest in G2/M and subsequently apoptosis. Importantly, ex vivo assays also demonstrate its anti-angiogenetic features; in vivo, it shows antitumor potential in xenografted nude mice without any observed toxicity.

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