2. Cell Cycle/DNA Damage Cytoskeleton Epigenetics Apoptosis Metabolic Enzyme/Protease
  3. Microtubule/Tubulin HDAC Apoptosis Mitochondrial Metabolism
  4. Tubulin/HDAC-IN-1

Tubulin/HDAC-IN-1 是一种双重的 tubulin 和 HDAC-IN-1 抑制剂，其通过与 tubulin 的 CH/π 相互作用以及与 HDAC8 的氢键相互作用而发挥功能。Tubulin/HDAC-IN-1 可抑制 tubulin 聚合并选择性抑制 HDAC8 (IC50: 150 nM)。Tubulin/HDAC-IN-1 对各种人类癌细胞具有细胞毒性，还可将细胞周期阻滞在 G2/M 期并诱导细胞凋亡 (apoptosis)。Tubulin/HDAC-IN-1 可用于神经母细胞瘤、白血病等血液肿瘤和实体肿瘤的研究。

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Tubulin/HDAC-IN-1 Chemical Structure

Tubulin/HDAC-IN-1 Chemical Structure

CAS No. : 2413587-26-3

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Tubulin/HDAC-IN-1 相关抗体

Top Publications Citing Use of Products

查看 HDAC 亚型特异性产品:

查看所有亚型
HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

IC50 & Target[1]

HDAC8

150 nM (IC50)

HDAC6

1 μM (IC50)

HDAC11

1.9 μM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
0.84 nM
Compound: 12a
Antiproliferative activity against human A549 cells after 72 hrs by CellTiter Glo assay
Antiproliferative activity against human A549 cells after 72 hrs by CellTiter Glo assay
[PMID: 35797900]
HCT-116 GI50
0.5 nM
Compound: 12a
Antiproliferative activity against human HCT-116 cells after 72 hrs by CellTiter Glo assay
Antiproliferative activity against human HCT-116 cells after 72 hrs by CellTiter Glo assay
[PMID: 35797900]
HT-29 IC50
0.62 nM
Compound: 12a
Antiproliferative activity against human HT-29 cells after 72 hrs by CellTiter Glo assay
Antiproliferative activity against human HT-29 cells after 72 hrs by CellTiter Glo assay
[PMID: 35797900]
K562 IC50
0.35 nM
Compound: 12a
Antiproliferative activity against human K562 cells after 72 hrs by CellTiter Glo assay
Antiproliferative activity against human K562 cells after 72 hrs by CellTiter Glo assay
[PMID: 35797900]
K562 IC50
0.56 nM
Compound: 12a
Antiproliferative activity against imatinib-resistant human K562 cells over expressing MDR1 after 72 hrs by CellTiter Glo assay
Antiproliferative activity against imatinib-resistant human K562 cells over expressing MDR1 after 72 hrs by CellTiter Glo assay
[PMID: 35797900]
MCF7 IC50
0.78 nM
Compound: 12a
Antiproliferative activity against human MCF7 cells after 72 hrs by CellTiter Glo assay
Antiproliferative activity against human MCF7 cells after 72 hrs by CellTiter Glo assay
[PMID: 35797900]
MDA-MB-231 IC50
0.7 nM
Compound: 12a
Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by CellTiter Glo assay
Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by CellTiter Glo assay
[PMID: 35797900]
MIA PaCa-2 IC50
0.94 nM
Compound: 12a
Antiproliferative activity against human MIA PaCa-2 cells after 72 hrs by CellTiter Glo assay
Antiproliferative activity against human MIA PaCa-2 cells after 72 hrs by CellTiter Glo assay
[PMID: 35797900]
NCI-N87 IC50
0.1 nM
Compound: 12a
Antiproliferative activity against human NCI-N87 cells after 72 hrs by CellTiter Glo assay
Antiproliferative activity against human NCI-N87 cells after 72 hrs by CellTiter Glo assay
[PMID: 35797900]
SK-OV-3 IC50
0.6 nM
Compound: 12a
Antiproliferative activity against human SK-OV-3 cells after 72 hrs by CellTiter Glo assay
Antiproliferative activity against human SK-OV-3 cells after 72 hrs by CellTiter Glo assay
[PMID: 35797900]
体外研究
(In Vitro)

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 RLM RLM HLM HLM
t1/2 (h) CLint t1/2 CLint
Tubulin/HDAC-IN-1 6.6 1.75 32 0.36

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

Tubulin/HDAC-IN-1 相关抗体:

Cell Proliferation Assay[1]

Cell Line: Various tumor cell lines as below
Concentration:
Incubation Time: 72 h
Result: Activities of Tubulin/HDAC-IN-1 (Compound 12a) against various tumor cell lines (IC50 nM):
NCIN87 K562 K562R MiaPaca2 SKOV3 A549 MCF-7 MDA-MB-231 HCT116 HT-29
Tubulin/HDAC-IN-1 0.1 0.35 0.56 0.94 0.6 0.84 0.78 0.7 0.6 0.62

Western Blot Analysis[1]

Cell Line: HT-29 cells
Concentration: 0.5, 1, 5, 10 nM for γH2AX; 0.5, 1, 100 nM for acetylated SMC3
Incubation Time: 24 h for γH2AX, 30 min for acetylated SMC3
Result: Dose-dependently increased γH2AX level and acetylated SMC3.
体内研究
(In Vivo)

Tubulin/HDAC-IN-1 (Compound 12a, intratumoral injection, 0.25 mg/kg, three times a week for two weeks) decreases MCA205 tumor growth and extends the overall survival of treated mice in allogeneic sarcoma mice model[1].

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

Animal Model: Allogeneic sarcoma model in C57BL/6 mice[1]
Dosage: 0.1, 0.25, 0.50 mg/kg, three times a week for two weeks.
Administration: Intratumoral injection
Result: Decreased tumor growth and extended the overall survival of treated mice with no obvious side effects.
分子量

374.39

Formula

C21H18N4O3
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

Tubulin/HDAC-IN-1 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

Tubulin/HDAC-IN-12413587-26-3Microtubule/TubulinHDACApoptosisMitochondrial MetabolismHistone deacetylasesCancertubulin polymerizationmultitargetedallogeneic sarcoma modelHT29γH2AXSMC3neuroblastomaleukemiaInhibitorinhibitorinhibit

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