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DYRK inhibitor FC-3

Chemical Structure : DYRK inhibitor FC-3

CAS No.: 2805339-74-4

DYRK inhibitor FC-3

货号: PC-27003Not For Human Use, Lab Use Only.

DYRK inhibitor FC-3 is a potent, selective, reversible, ATP-competitive inhibitor of Dual-specificity tyrosine-regulated kinases (DYRKs) with IC50 of 53 nM (DYRK1A).

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

DYRK inhibitor FC-3 is a potent, selective, reversible, ATP-competitive inhibitor of Dual-specificity tyrosine-regulated kinases (DYRKs) with IC50 of 53 nM (DYRK1A).
The gatekeeper mutants F238L and M240R demonstrated resistance to FC-2 with IC50 of 1-2.5 uM, F238L-M240R double mutant has IC50 of 4 uM.
FC-3 (5-20 uM) reduces neurosphere proliferation and cell invasion of GBM cell line U87MG by specifically targeting DYRK1A.
FC-3 enhances EGFR ubiquitination, leading to its lysosomal degradation in EGFR-dependent glioblastoma cell-based models.
FC-3 (2 mg/kg daily) attenuates DYRK1A-mediated tumorigenesis in U87MG subcutaneous xenograft model of Nu/J nude mice.

物理化学性质&存储条件

分子量 303.29
分子式 C14H9NO5S
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

(5,6-dihydroxybenzo[d]thiazol-2-yl)(3,4-dihydroxyphenyl)methanone

参考文献

1. Venkataramani P, et al. Cell Chem Biol. 2026 Jun 10:S2451-9456(26)00157-1.

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