1. Cell Cycle/DNA Damage Cytoskeleton Apoptosis
  2. Microtubule/Tubulin Apoptosis
  3. Tubulin polymerization-IN-9

Tubulin polymerization-IN-9 是一种有效的微管蛋白 (tubulin) 抑制剂,IC50 为 1.82 μM。Tubulin polymerization-IN-9 能引起细胞周期阻滞在 G2/M 期,诱导 K562 细胞凋亡 (apoptosis) 和线粒体去极化。Tubulin polymerization-IN-9 具有强效的抗血管和抗肿瘤活性。

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Tubulin polymerization-IN-9 Chemical Structure

Tubulin polymerization-IN-9 Chemical Structure

CAS No. : 2485020-93-5

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Tubulin polymerization-IN-9 is a potent tubulin inhibitor with IC50 of 1.82 μM. Tubulin polymerization-IN-9 causes cell cycle arrest at G2/M phase, and induces cell apoptosis and depolarized mitochondria of K562 cells. Tubulin polymerization-IN-9 has potent anti-vascular and antitumor activities[1].

IC50 & Target

IC50: 1.82 μM (tubulin)[1]

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HCT-8 IC50
0.621 μM
Compound: 11k
Antiproliferative activity against human HCT8 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human HCT8 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 32853870]
HepG2 IC50
0.525 μM
Compound: 11k
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: 32853870]
K562 IC50
0.287 μM
Compound: 11k
Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 32853870]
体外研究
(In Vitro)

Tubulin polymerization-IN-9 (compound 11k) (0.1, 1, 10 μM; 72 hours) has potent activity against these three cancer cell lines with IC50 values ranging from 0.287 to 0.621 μM[1].
Tubulin polymerization-IN-9 (0.15, 0.3 and 0.6 μM; 24 hours) induces a dose-dependent collapse of the microtubule networks[1].
Tubulin polymerization-IN-9 (0.15, 0.3 and 0.6 μM; 48 hours) observes a gradual accumulation of cells at G2/M phase in K562 cells[1].
Tubulin polymerization-IN-9 (0.15, 0.3 and 0.6 μM; 72 hours) effectively induces cell apoptosis in K562 cells in a concentration-dependent manner[1].
Tubulin polymerization-IN-9 (0.15, 0.3 and 0.6 μM; 24 hours) causes mitochondrial depolarization of K562 cells in the process of apoptosis[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

Cell Line: K562 HepG2 and HCT-8 cells[1]
Concentration: 0.1, 1, 10 μM
Incubation Time: 72 hours
Result: Showed potent activity against these three cancer cell lines with IC50 values ranging from 0.287 to 0.621 μM.

Immunofluorescence

Cell Line: K562 cells[1]
Concentration: 0.15, 0.3 and 0.6 μM
Incubation Time: 24 hours
Result: Induced a dose-dependent collapse of the microtubule networks.

Cell Cycle Analysis

Cell Line: K562 cells[1]
Concentration: 0.15, 0.3 and 0.6 μM
Incubation Time: 48 hours
Result: Observed a gradual accumulation of cells at G2/M phase in K562 cells.

Apoptosis Analysis

Cell Line: K562 cells[1]
Concentration: 0.15, 0.3 and 0.6 μM
Incubation Time: 72 hours
Result: Effectively induced cell apoptosis in K562 cells in a concentration-dependent manner.
体内研究
(In Vivo)

Tubulin polymerization-IN-9 (15 and 30 mg/kg; IV; once a day, for 21 days) effectively suppresses the tumor volume and reduces tumor weight by 71.1% at a dose of 30 mg/kg[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male ICR mice (5 weeks; injected with H22 cells; n=6)[1]
Dosage: 15 and 30 mg/kg
Administration: IV; once a day, for 21 days
Result: Effectively suppressed the tumor volume and reduced tumor weight by 71.1% at a dose of 30 mg/kg.
分子量

420.32

Formula

C19H19NO5Se

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

纯度 & 产品资料
参考文献
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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