Chemical Structure : GIT1 inhibitor Compound 3
CAS No.:
844464-54-6
GIT1 inhibitor Compound 3
(GIT1-IN-C3)
货号: PC-26306Not For Human Use, Lab Use Only.
GIT1 inhibitor Compound 3 (GIT1-IN-C3) is a selective small molecule inhibitor of ARF GTPase protein 1 (GIT1) with MST KD of 6.2 uM, effectively disrupts GIT1 from interacting with MAT2B and RAF/MEK/ERK to halt cancer cell growth in vitro and in vivo.
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纯度 & COA & 质检文件 纯度:
>98% (HPLC)
生物&药学活性
GIT1 inhibitor Compound 3 (GIT1-IN-C3) is a selective small molecule inhibitor of ARF GTPase protein 1 (GIT1) with MST KD of 6.2 uM, effectively disrupts GIT1 from interacting with MAT2B and RAF/MEK/ERK to halt cancer cell growth in vitro and in vivo.
C3 binds selectively to GIT1 with KD of 6.2 µM but not to GIT2.
C3 inhibits growth of multiple cancer cell lines (HepG2, Hep3B, MzChA-1, RKO, HT-29) with inhibition occurring at 10 µM but not in non-malignant AML12 or HEK293 cells.
C3 arrests cell cycle progression at G2/M phases and induces cell death only in liver and colon cancer cells.
C3 inhibits the clonogenic potential of RKO and HepG2 cells at 1 uM.
C3 disrupts GIT1-MAT2B scaffold and RAF/MEK/ERK recruitment.
C3 induces cyclin B1 stabilization and activates cyclin B1/CDK1.
C3 (25 mg/kg daily, i.p.) inhibits CRC growth in multiple in vivo models.
物理化学性质&存储条件
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分子量
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424.48
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分子式
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C21H20N4O4S
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外观性状
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Solid
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CAS No.
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储存条件
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- 固体粉末
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-20°C 12 个月; 4°C 6 个月
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- 配置液
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-80°C 6 个月; -20°C 6 个月
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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2-(8,8-dimethyl-4-oxo-7,10-dihydro-8H-pyrano[3'',4'':5',6']pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-3(4H)-yl)-N-(furan-2-ylmethyl)acetamide
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参考文献
1. Peng H, et al. Cell Death Dis. 2026 Feb 20;17(1):238.
