2. Cell Cycle/DNA Damage Epigenetics Apoptosis Autophagy
  3. HDAC Apoptosis Autophagy
  4. HDAC-IN-98

HDAC-IN-98 是一种 HDAC1、HDAC2、HDAC3 抑制剂 (属于最具有选择性的 I 类 HDAC 抑制剂之一)，其 IC50 值分别为 41.2 nM、52.5 nM 和 74.3 nM。HDAC-IN-98 可诱导 H3K9 乙酰化，上调 p21 表达，引起 G2/M 期阻滞，诱导细胞凋亡 (apoptosis)，在结直肠癌细胞中表现出强烈的抗增殖活性，对正常结肠上皮细胞毒性较低，通过自噬 (autophagy) 调控短期体外效应，并在鸡胚绒毛膜尿囊膜模型 (CAM) 试验中展现出显著的抗肿瘤效果。HDAC-IN-98 可用于结直肠癌研究。

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HDAC-IN-98

HDAC-IN-98 Chemical Structure

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Customer Review

HDAC-IN-98 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

HDAC-IN-98 is a HDAC1, HDAC2, HDAC3 inhibitor (one of the most selective class I HDAC inhibitors) with human IC50 values of 41.2 nM, 52.5 nM, and 74.3 nM respectively. HDAC-IN-98 induces H3K9 acetylation, p21 upregulation, G2/M arrest, cell apoptosis, has strong antiproliferative effects in colorectal cancer cells, low toxicity in healthy colon epithelium, modulates short-term in vitro effects via autophagy, and shows strong antitumor efficacy in vivo in the chorioallantoic membrane model (CAM) assay. HDAC-IN-98 can be used for the research of colorectal cancer[1].

IC50 & Target

hHDAC1

41.2 nM (IC50)

hHDAC2

52.5 nM (IC50)

hHDAC3

74.3 nM (IC50)

hHDAC6

>10000 nM (IC50)

hHDAC8

>10000 nM (IC50)

hHDAC10

4261 nM (IC50)

hHDAC11

>10000 nM (IC50)

体外研究
(In Vitro)

HDAC-IN-98 (compound 5d) 可选择性抑制 I 类 HDAC 酶 (HDAC1、HDAC2、HDAC3)，其 IC50 值为亚纳摩尔至低纳摩尔级别，而对其他 HDAC 亚型的活性较弱或无活性 (IC50：HDAC1 = 41.26 nM、HDAC2 = 52.5 nM、HDAC3 = 74.3 nM、HDAC10 = 4261 nM、HDAC5/8/11 >10000 nM)[1]。
HDAC-IN-98 (1 μM；最长 60 min) 可在复杂的核提取物系统中抑制总 HDAC 活性 [1]。
HDAC-IN-98 (0.1-100 μM；48 h) 可选择性降低结直肠癌 (CRC) 细胞的活力，其 IC50 值范围为 1–4 μM，且对正常结肠细胞的毒性极小 (IC50：HCT116 = 1 μM、HT29 = 4 μM、DLD1 = 4 μM、HCEC >100 μM) [1]。
HDAC-IN-98 (1-4 μM；48 h) 可在不抑制 II 类 HDAC 的情况下，调控结直肠癌 (CRC) 细胞中的表观遗传标志物 (H3K9 乙酰化) 和凋亡通路 (PARP 切割)[1]。
HDAC-IN-98 (1-4 μM；48 h) 可干扰细胞周期进程，在 HCT116 细胞中诱导 subG1 积累 (凋亡)，并在 HT29/DLD1 细胞中引起 G1 期阻滞[1]。
HDAC-IN-98 (1-4 μM；48 h) 可选择性诱导 HCT116 细胞凋亡，且不引发坏死[1]。
HDAC-IN-98 (最高 10 μM) 在与其抗癌活性相关的浓度下显示出极低的 hERG 毒性 [1]。
HDAC-IN-98 (1 μM；体外预处理；48 小时) 在鸡胚结直肠癌绒毛尿囊膜模型 (CAM) 中表现出强大的抗肿瘤功效，且与 p21 状态无关。在 HCT116 p21 野生型 CAM 模型中，HDAC-IN-98 证实了 p21 的显著上调。在 HCT116 p21−/− CAM 模型中，HDAC-IN-98 显著减少了血管面积、血管长度和分支点数量，而血管厚度不受影响[1]。

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

HDAC-IN-98 相关抗体:

Cell Viability Assay[1]

Cell Line: Colorectal Cancer Cell Lines (HCT116, HT29, DLD1) and Normal Colon Epithelial Cells (HCEC)
Concentration: 0.1-100 μM
Incubation Time: 48 h
Result: Showed dose-dependent cytotoxicity with an IC₅₀ of 1 μM (HCT116); showed dose-dependent cytotoxicity with an IC₅₀ of 4 μM (HT29); showed dose-dependent cytotoxicity with an IC₅₀ of 4 μM (DLD1); showed low toxicity in HCEC with an IC₅₀ >100 μM

Western Blot Analysis[1]

Cell Line: CRC Cell Lines (HCT116, HT29, DLD1)
Concentration: 1 μM, 4 μM
Incubation Time: 48 h
Result: Slightly increased H3K9 acetylation in HCT116 cells; did not affect HDAC1/HDAC6 protein levels or α-tubulin acetylation; upregulated p21 in HCT116 cells; induced PARP cleavage in HCT116/HT29 cells.

Cell Cycle Analysis[1]

Cell Line: CRC Cell Lines (HCT116, HT29, DLD1)
Concentration: 1 μM, 4 μM
Incubation Time: 48 h
Result: Induced subG1 accumulation (apoptosis) in HCT116 cells; increased G1-phase population in HT29/DLD1 cells; reduced S-phase population across all lines; correlated with upregulated p21 and reduced Cyclin B1 in HCT116 cells.

Apoptosis Analysis[1]

Cell Line: CRC Cell Lines (HCT116, HT29, DLD1)
Concentration: 1 μM, 4 μM
Incubation Time: 48 h
Result: Induced significant apoptosis in HCT116 cells (Annexin V-positive/PI-negative cells); induced minimal apoptosis in HT29/DLD1 cells; showed no necrosis.
分子量

415.44

Formula

C24H21N3O4
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

HDAC-IN-98 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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.

Keywords:

HDAC-IN-98HDACApoptosisAutophagyHistone deacetylasesG2/M arrestHDAC3p21HDAC1autophagyH3K9 acetylationCAM assayHDAC2healthy colon epitheliumcolorectal cancer cellsInhibitorinhibitorinhibit

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