WC36 | Syk-cSH2 inhibitor | Probechem Biochemicals

Chemical Structure : WC36

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WC36 (Syk-cSH2 inhibitor WC36)

货号: PC-49383Not For Human Use, Lab Use Only.

WC36 is a potent, specific inhibitor of Syk-cSH2 with IC50 of 40 nM, inhibits Syk-cSH2-PIP3 binding, specifically and potently suppresses oncogenic activities of Syk in AML cells.

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生物&药学活性

WC36 is a potent, specific inhibitor of Syk-cSH2 with IC50 of 40 nM, inhibits Syk-cSH2-PIP3 binding, specifically and potently suppresses oncogenic activities of Syk in AML cells.
WC36 potently blocks BCR-mediated activation of Syk in B cells, effectively suppresses phosphorylation of all BCR signaling proteins.
WC36 does not inhibit binding of ZAP-70-cSH2 to PIP3-containing vesicles, showing selectivity for Syk-cSH2 over ZAP-70-cSH2.
WC36 (5 uM) potently suppressed the phosphorylation and activation of Syk, ERK1/2 and STAT3/5 in entospletinib-resistant MV4-11 cells, but not 5 μM entospletinib.
WC36 potently inhibited proliferation of entospletinib-resistant MV4-11 cells.
WC36 suppressed HL-60 and patient-derived AML cells, while entospletinib was ineffective, WC36 potently inhibited phosphorylation of Syk, ERK1/2 and STAT3/5 in AML cells.
WC36 blocks not only the Syk kinase activity, but also its noncatalytic scaffolding function that is linked to drug resistance.

物理化学性质&存储条件

分子量	390.447
分子式	C21H22N6O2
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	cyclohexyl 2-diazo-3-(1H-indol-3-yl)-3-(pyrimidin-2-ylamino)propanoate

参考文献

1. Indira Singaram, et al. Nat Chem Biol. 2022 Oct 13. doi: 10.1038/s41589-022-01150-z.

WC36 (Syk-cSH2 inhibitor WC36)

生物&药学活性

物理化学性质&存储条件

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WC36 (Syk-cSH2 inhibitor WC36)

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物理化学性质&存储条件

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