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WC36

Chemical Structure : WC36

CAS No.:

WC36 (Syk-cSH2 inhibitor WC36)

Catalog No.: 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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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

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.

Physicochemical Properties

M.Wt 390.447
Formula C21H22N6O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

cyclohexyl 2-diazo-3-(1H-indol-3-yl)-3-(pyrimidin-2-ylamino)propanoate

References

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

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