C3TD879 | Citron kinase inhibitor | Probechem Biochemicals

Chemical Structure : C3TD879

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C3TD879 (CITK inhibitor)

货号: PC-21755Not For Human Use, Lab Use Only.

C3TD879 is a potent, selective first-in-class Citron kinase (CITK) chemical inhibitor with biochemical IC50 of 12 nM.

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生物&药学活性

C3TD879 is a potent, selective first-in-class Citron kinase (CITK) chemical inhibitor with biochemical IC50 of 12 nM.
C3TD879 is highly selective for CITK in the Eurofins KinaseProfiler assay against 373 human kinases, with exception of NEK family kinases AAK1 and BIKE (>17-fold selective).
C3TD879 directly binds to and stabilizes CITK kinase domain (Met1-Ala449) in target engagement assays, binds to NL-CITK KD with Kd = 0.3 nM and to full-length NL-CITK with Kd = 9.5 nM.
C3TD879 shows no on-target antiproliferative phenotype in HeLa cells.
C3TD879 does not significantly affect cell cycle progression or induce multinucleation in HeLa cells.
C3TD879 is the first chemical probe suitable for interrogating the complex biology of CITK.
CITK is an AGC-family serine/threonine kinase closely related to the Rho-associated (ROCK) and Aurora (AURK) protein kinases, has been reported to play both catalytic and structural roles during cytokinesis.

物理化学性质&存储条件

分子量	364.49
分子式	C22H28N4O
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	(R)-2-Amino-4,4-dimethyl-N-(3-methyl-4-(2-methyl-1H-pyrrolo[2,3-b]pyridin-4-yl)phenyl)pentanamide

参考文献

1. Maw JJ, et al. J Med Chem. 2024 Feb 8. doi: 10.1021/acs.jmedchem.3c01807.

C3TD879 (CITK inhibitor)

生物&药学活性

物理化学性质&存储条件

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C3TD879 (CITK inhibitor)

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