2. Cell Cycle/DNA Damage Epigenetics Apoptosis Stem Cell/Wnt
  3. HDAC Apoptosis Wnt β-catenin MDM-2/p53 c-Myc
  4. HIT211504993

HIT211504993 是一种选择性组蛋白去乙酰化酶 6 (HDAC6) 抑制剂，其 IC50 为 0.070 μM。HIT211504993 可抑制癌细胞增殖，引发 G1 期细胞周期阻滞并诱导细胞凋亡 (apoptosis)。HIT211504993 可通过核质乙酰化、p53 调控及 Wnt/β-catenin 信号通路调控抑制 Myc 驱动的肿瘤发生。HIT211504993 可抑制结肠癌异种移植小鼠模型中的肿瘤生长。HIT211504993 可用于结肠癌的相关研究。

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HIT211504993

HIT211504993 Chemical Structure

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HIT211504993 相关抗体

Top Publications Citing Use of Products

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HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HIT211504993 is a selective histone deacetylase 6 (HDAC6) inhibitor with an IC50 of 0.070 μM. HIT211504993 suppresses cancer cell proliferation, cause G1 phase cell cycle arrest and induces apoptosis. HIT211504993 inhibits Myc-driven tumorigenesis via nucleocytoplasmic acetylation, p53 modulation, and Wnt/β-catenin signaling modulation. HIT211504993 inhibits tumor growth in a colon cancer xenograft mouse model. HIT211504993 can be used for the research of colon cancer[1].

IC50 & Target[1]

HDAC6

0.07 μM (IC50)

体外研究
(In Vitro)

HIT211504993 可强效且选择性地抑制 HDAC6，其 IC50 为 0.070 ± 0.002 μM，对 HDAC6 的抑制活性比对 HDAC2 高约 89 倍，比对 HDAC4 高约 486 倍[1]。
HIT211504993 (48 h) 可选择性抑制结直肠癌细胞 (HCT-8、HCT116) (IC50 值为 12.483 和 18.840 μM) 及其他肿瘤细胞系的活力，对正常 NCM460 肠上皮细胞的毒性较低[1]。
HIT211504993 (10-50 μM; 12-48 h) 可以浓度和时间依赖的方式有效增强 HCT-8 和 HCT116 结直肠癌细胞中组蛋白 H3 和非组蛋白 α-微管蛋白的乙酰化水平[1]。
HIT211504993 (20 μM; 24 h) 可抑制 HCT-8 和 HCT116 结直肠癌细胞的长期增殖能力，这可通过克隆形成能力降低来验证[1]。
HIT211504993 (20 μM; 12-48 h) 可在 HCT-8 和 HCT116 结直肠癌细胞中诱导 G1 期细胞周期阻滞并下调 Cyclin D 的表达，从而抑制细胞增殖[1]。
HIT211504993 (20 μM; 12-48 h) 可通过内源性线粒体通路在 HCT-8 和 HCT116 结直肠癌细胞中诱导时间依赖性细胞凋亡，Bcl-2/Bax 表达改变及 Annexin V 阳性细胞增加可证明这一点[1]。
HIT211504993 (60 μM; 6 h) 可在 HCT-8 结直肠癌细胞中直接结合 HDAC1 和 HDAC2，提高二者的热稳定性[1]。
HIT211504993 (20 μM; 4-24 h) 可调控 HCT-8 结直肠癌细胞的基因表达，下调 MYC 和 Wnt/β-catenin 通路组分，同时上调 p53 和 DUSP1，从而抑制肿瘤发生[1]。

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

HIT211504993 相关抗体:

Cell Viability Assay[1]

Cell Line: HCT-8, HCT116, NCM460, A2780, A549, MDA-MB-231, HepG2, HeLa, A375 cells
Concentration: 0.5-100 μM
Incubation Time: 48 h
Result: Exhibited an IC50 of 12.483 ± 0.92 μM in HCT-8 cells.
Exhibited an IC50 of 18.840 ± 0.88 μM in HCT116 cells.
Exhibited an IC50 of 46.043 ± 3.39 μM in NCM460 cells.
Exhibited an IC50 of 33.080 ± 3.98 μM in A2780 cells.
Exhibited an IC50 of 25.967 ± 5.45 μM in A549 cells.
Exhibited an IC50 of 10.782 ± 0.76 μM in MDA-MB-231 cells.
Exhibited an IC50 of 26.680 ± 1.75 μM in HepG2 cells.
Exhibited an IC50 of 56.557 ± 3.74 μM in HeLa cells.
Exhibited an IC50 of 20.983 ± 0.48 μM in A375 cells.

Western Blot Analysis[1]

Cell Line: HCT-8, HCT116 colorectal cancer cells
Concentration: 10, 20, 30, 40,50 μM
Incubation Time: 12, 24, 36, 48 h
Result: Increased acetyl-H3 and acetyl-α-tubulin levels in both cell lines, with the most substantial enhancement at 20 μM.
Induced time-dependent increases in acetyl-H3 and acetyl-α-tubulin levels in both cell lines when incubated for 12-48 h at 20 μM.

Cell Cycle Analysis[1]

Cell Line: HCT-8, HCT116 colorectal cancer cells
Concentration: 20 μM
Incubation Time: 12, 24, 36, 48 h
Result: Induced G1 phase cell cycle arrest in both HCT-8 and HCT116 cells.
Caused a significant decrease in Cyclin D protein expression in a time-dependent manner.

Apoptosis Analysis[1]

Cell Line: HCT-8, HCT116 colorectal cancer cells
Concentration: 20 μM
Incubation Time: 12, 24, 36, 48 h
Result: Induced apoptosis in a time-dependent manner, with progressive increases in apoptotic cell proportions over 12-48 h.
Downregulated anti-apoptotic Bcl-2 protein expression in both cell lines.
Upregulated pro-apoptotic Bax protein expression in both cell lines.

Real Time qPCR[1]

Cell Line: HCT-8 colorectal cancer cells
Concentration: 20 μM
Incubation Time: 4, 12, 24 h
Result: Altered the expression of 2692, 4788, and 5627 differentially expressed genes at 4, 12, and 24 h respectively, with enrichment in histone modification, cell cycle arrest, p53 signaling, and Wnt/β-catenin signaling pathways.
Induced time-dependent downregulation of MYC mRNA and protein expression.
Induced upregulation of DUSP1 and p53 mRNA and protein expression.
Downregulated mRNA levels of Wnt4, β-catenin, TCF4, and LEF1.
Reduced β-catenin protein expression in HCT-8 cells.
体内研究
(In Vivo)

HIT211504993 (25-100 mg/kg；腹腔注射；每天一次；15 天) 可呈剂量依赖性抑制 HCT-8 结直肠癌异种移植瘤的生长，在 50 mg/kg 剂量下肿瘤体积缩小率达 77%，且耐受性良好[1]。

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

Animal Model: BALB/c nude (4−6 weeks old, 16−20 g, subcutaneous xenograft via HCT-8 cell injection)[1]
Dosage: 25 mg/kg; 50 mg/kg; 100 mg/kg
Administration: I.p.; daily; 15 days
Result: Reduced tumor weight relative to vehicle control at 25 mg/kg.
Reduced tumor volume by 77% and tumor weight by 68% relative to vehicle control at 50 mg/kg.
Suppressed tumor growth to a greater extent than the 50 mg/kg dose at 100 mg/kg.
Caused no significant body weight changes or histological abnormalities in heart, liver, spleen, kidneys, or lungs across all treatment doses.
分子量

494.99

Formula

C23H27ClN2O6S
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

HIT211504993 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • 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.

Keywords:

HIT211504993HIT 211504993HIT-211504993HDACApoptosisWntβ-cateninMDM-2/p53c-MycHistone deacetylasesBeta cateninMycp53colon cancer cellscolon cancerhistone deacetylase 6HCT-8Wnt/β-catenin signalingMyc-driven tumorigenesisHCT116HDAC6colon cancer xenograft mouse modelInhibitorinhibitorinhibit

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