1. Cell Cycle/DNA Damage Cytoskeleton Apoptosis Epigenetics
  2. Microtubule/Tubulin Apoptosis PARP Caspase
  3. Tubulin polymerization-IN-68

Tubulin polymerization-IN-68 (compound 32) is a tubulin inhibitor that can inhibit tubulin polymerization and destroy the cellular microtubule network. Tubulin polymerization-IN-68 can upregulate the expression of PARP-1 and caspase-3 and induce cell apoptosis, and has anticancer activity. Tubulin polymerization-IN-68 can effectively inhibit HepG2 (IC50=93 nM) and significantly inhibit the growth of HepG2 xenograft tumors in nude mice by oral administration.

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Tubulin polymerization-IN-68

Tubulin polymerization-IN-68 Chemical Structure

CAS No. : 2924156-96-5

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Description

Tubulin polymerization-IN-68 (compound 32) is a tubulin inhibitor that can inhibit tubulin polymerization and destroy the cellular microtubule network. Tubulin polymerization-IN-68 can upregulate the expression of PARP-1 and caspase-3 and induce cell apoptosis, and has anticancer activity. Tubulin polymerization-IN-68 can effectively inhibit HepG2 (IC50=93 nM) and significantly inhibit the growth of HepG2 xenograft tumors in nude mice by oral administration[1].

IC50 & Target

PARP-1[1]

Cellular Effect
Cell Line Type Value Description References
A-375 IC50
3.568 μM
Compound: 32
Antiproliferative activity against human A-375 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human A-375 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 39163776]
A549 IC50
1.502 μM
Compound: 32
Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 39163776]
HepG2 IC50
0.093 μM
Compound: 32
Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 39163776]
PANC-1 IC50
6.951 μM
Compound: 32
Antiproliferative activity against human PANC-1 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human PANC-1 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 39163776]
U-251 IC50
11.814 μM
Compound: 32
Antiproliferative activity against human U-251 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human U-251 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 39163776]
Molecular Weight

263.29

Formula

C16H13N3O

CAS No.
SMILES

O=C1NC(C2=CC3=C(NC=C3)C=C2)NC4=C1C=CC=C4

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Purity & Documentation
References
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Tubulin polymerization-IN-68
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