PeptideDB

Tubulin/HDAC-IN-1

CAS: 2413587-26-3 F: C21H18N4O3 W: 374.39

Tubulin/HDAC-IN-1 is a dual tubulin and HDAC-IN-1 inhibitor through CH/π interaction with tubulin and hydrogen bond int
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Bioactivity Tubulin/HDAC-IN-1 is a dual tubulin and HDAC-IN-1 inhibitor through CH/π interaction with tubulin and hydrogen bond interaction with HDAC8. Tubulin/HDAC-IN-1 inhibits tubulin polymerization and selectively inhibits HDAC8 (IC50: 150 nM). Tubulin/HDAC-IN-1 has cytotoxicity against various human cancer cells, also arrests cell cycle in the G2/M phase and induces cell apoptosis. Tubulin/HDAC-IN-1 can be used in the research of hematologic and solid tumors such as neuroblastoma, leukemia[1].
Invitro Tubulin/HDAC-IN-1 (Compound 12a, 72 h) shows cytotoxicity against various human cancer cell lines with an averaged IC50 value of 0.6 nM[1].Tubulin/HDAC-IN-1 (2 nM, 24 h) induces HT29 cell cycle arrest in the G2/M phase and produces caspase-induced apoptosis of HT29 cells through mitochondrial dysfunction[1].Tubulin/HDAC-IN-1 selectively inhibits HDAC8 (IC50: 150 nM), inhibits HDAC6 and HDAC11 with IC 50 values of 1 μM and 1.9 μM respectively[1].Tubulin/HDAC-IN-1 (0.5-100 nM, 24 h/30 min) dose-dependently increases γH2AX level and acetylated SMC3 in HT-29 cells[1].Tubulin/HDAC-IN-1 (5-15 μΜ, 0-40 min) inhibits tubulin polymerization in a dose-dependent manner, with a maximal effect achieved at 10 μM[1].Tubulin/HDAC-IN-1 (250 nM, 30 min) depolymerizes the cell microtubule network, and the effect is not specific[1].Tubulin/HDAC-IN-1 shows good in vitro metabolic stability expressed by the intrinsic clearance CLint (given in μL/min/mg protein) using rat liver microsomes (RLM) and human liver microsomes (HLM)[1].Compound
Name Tubulin/HDAC-IN-1
CAS 2413587-26-3
Formula C21H18N4O3
Molar Mass 374.39
Transport Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.