Chemical Structure : GIT1 inhibitor Compound 3
CAS No.:
844464-54-6
GIT1 inhibitor Compound 3
(GIT1-IN-C3)
Catalog No.: 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.
Bulk size, bulk discount!
Welcome credit card payment!
E-mail: sales@probechem.com
Tech Support: tech@probechem.com
Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
|
M.Wt
|
424.48
|
|
Formula
|
C21H20N4O4S
|
|
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
|
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
|
References
1. Peng H, et al. Cell Death Dis. 2026 Feb 20;17(1):238.
Contact Us
sales@probechem.com
