905978-63-4
Chemical Structure
IG-105
- CAS No.: 905978-63-4
- Formula:C20H19N3O4S
- Molecular Weight:397.45
IUPAC Name: N-(2,6-dimethoxypyridin-3-yl)-9-methyl-9H-carbazole-3-sulfonamide
InChIKey: JTPDYODKXJLRLA-UHFFFAOYSA-N
SMILES: O=S(C1=CC2=C(C=C1)N(C)C3=C2C=CC=C3)(NC4=CC=C(OC)N=C4OC)=O
Biological Activity: IG-105 is a potent tubulin inhibitor, with an IC50 of 0.6 μM for competitive inhibition of [3H] colchicine binding to tubulin, and an IC50 of 3 μM for inhibition of tubulin polymerization. IG-105 inhibits microtubule polymerization by binding to the colchicine pocket of tubulin, induces cell cycle arrest at the G2-M phase, and subsequently activates the caspase cascade through Bcl-2 inactivation and p53 upregulation to induce apoptosis. As a non-Pgp substrate, IG-105 effectively overcomes multidrug resistance. IG-105 can be used in the research of leukemia, breast cancer, liver cancer, prostate cancer, lung cancer, melanoma, pancreatic cancer and colon cancer[1].
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IG-105 | IG-105 is a potent tubulin inhibitor, with an IC50 of 0.6 μM for competitive inhibition of [3H] colchicine binding to tubulin, and an IC50 of 3 μM for inhibition of tubulin polymerization. IG-105 inhibits microtubule polymerization by binding to the colchicine pocket of tubulin, induces cell cycle arrest at the G2-M phase, and subsequently activates the caspase cascade through Bcl-2 inactivation and p53 upregulation to induce apoptosis. As a non-Pgp substrate, IG-105 effectively overcomes multidrug resistance. IG-105 can be used in the research of leukemia, breast cancer, liver cancer, prostate cancer, lung cancer, melanoma, pancreatic cancer and colon cancer. | |||||||||||||||||||||
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Keywords
