Chemical Structure : DYRK inhibitor FC-2
货号: PC-27002Not For Human Use, Lab Use Only.
DYRK inhibitor FC-2 is a potent, selective, reversible, ATP-competitive inhibitor of Dual-specificity tyrosine-regulated kinases (DYRKs) with IC50 of 19 nM (DYRK1A).
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DYRK inhibitor FC-2 is a potent, selective, reversible, ATP-competitive inhibitor of Dual-specificity tyrosine-regulated kinases (DYRKs) with IC50 of 19 nM (DYRK1A).
The gatekeeper mutants F238L and M240R demonstrated resistance to FC-2 with IC50 of 400-450 nM, F238L-M240R double mutant has IC50 of 5 uM.
FC-2 (5-20 uM) reduces neurosphere proliferation and cell invasion of GBM cell line U87MG by specifically targeting DYRK1A.
FC-2 enhances EGFR ubiquitination, leading to its lysosomal degradation in EGFR-dependent glioblastoma cell-based models.
FC-2 (2 mg/kg daily) attenuates DYRK1A-mediated tumorigenesis in U87MG subcutaneous xenograft model of Nu/J nude mice.
| 分子量 | 287.29 | |
| 分子式 | C14H9NO4S | |
| 外观性状 | Solid | |
| 储存条件 |
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| Solubility |
10 mM in DMSO |
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1. Venkataramani P, et al. Cell Chem Biol. 2026 Jun 10:S2451-9456(26)00157-1.
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