1. Cell Cycle/DNA Damage Epigenetics Apoptosis
  2. HDAC Apoptosis
  3. HDAC6-IN-82

HDAC6-IN-82 是一种选择性的 HDAC6 抑制剂,对 HDAC6IC50 为 4.9 nM。HDAC6-IN-82 可抑制 HDAC1 (112 nM)、HDAC2 (737 nM)、HDAC3 (623 nM)、HDAC8 (1140 nM)、HDAC10 (91.4 nM) 和 HDAC11 (219 nM)。HDAC6-IN-82 可降低癌细胞活力、促进细胞周期阻滞、诱导细胞凋亡 (apoptosis)、提高 H3K9 和 α-微管蛋白的乙酰化水平。HDAC6-IN-82 可用于白血病等癌症相关研究。

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HDAC6-IN-82

HDAC6-IN-82 Chemical Structure

CAS No. : 1228571-33-2

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HDAC6-IN-82 is a selective HDAC6 inhibitor with an IC50 of 4.9 nM against HDAC6. HDAC6-IN-82 inhibits HDAC1 (112 nM), HDAC2 (737 nM), HDAC3 (623 nM), HDAC8 (1140 nM), HDAC10 (91.4 nM) and HDAC11 (219 nM). HDAC6-IN-82 reduces cancer cell viability, induces cell cycle arrest, triggers apoptosis, and increases the acetylation levels of H3K9 and α-tubulin. HDAC6-IN-82 can be used in cancer-related research such as leukemia[1].

IC50 & Target[1]

HDAC6

4.9 nM (IC50)

HDAC1

112 nM (IC50)

HDAC2

737 nM (IC50)

HDAC3

623 nM (IC50)

HDAC4

71300 nM (IC50)

HDAC5

14900 nM (IC50)

HDAC7

NI nM (IC50)

HDAC8

1140 nM (IC50)

HDAC9

NI nM (IC50)

HDAC10

33.1 nM (IC50)

HDAC11

219 nM (IC50)

体外研究
(In Vitro)

HDAC6-IN-82 (Compound 14b) (48 h) 可降低一组人类实体瘤和血液系统癌细胞系的细胞活力,其中对 HL60 和 U937 白血病细胞的效力最强 (CC50 = 1.2 μM 和 1.3 μM)[1]
HDAC6-IN-82 (0.125-0.25 μM; 24-48 h) 以时间和剂量依赖的方式诱导 U937 急性髓系白血病细胞发生凋亡[1]
HDAC6-IN-82 (0.0675-0.25 μM; 48 h) 可抑制 U937 急性髓系白血病细胞的细胞核及细胞质 HDAC 活性[1]
HDAC6-IN-82 (0.0675-0.25 μM; 48 h) 处理 U937 急性髓系白血病细胞 48 小时后,可调控细胞周期和凋亡调控因子的 mRNA 表达,上调 p21、Bak 和 Bax,同时下调 cyclin D1 和 Bcl-2[1]
HDAC6-IN-82 (0.0675-0.25 μM; 48 h) 可在处理 48 小时后调控 U937 急性髓系白血病细胞中的 miRNA 表达,下调参与凋亡调控的抗凋亡 miRNA 并上调促凋亡 miRNA[1]

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

Cell Cycle Analysis[1]

Cell Line: AML U937 cells
Concentration: 0.125 and 0.25 μM
Incubation Time: 24 h, 48 h
Result: Induced a time- and dose-dependent accumulation of cells in the sub-G1 phase: at 24 h, 0.125 μM caused ~30% sub-G1 cells and 0.25 μM caused ~40% sub-G1 cells; at 48 h, 0.125 μM caused ~45% sub-G1 cells and 0.25 μM caused ~70% sub-G1 cells.
Triggered a time- and dose-dependent increase in Annexin V-positive cells: at 24 h, 0.125 μM caused ~40% Annexin V-positive cells and 0.25 μM caused ~50% Annexin V-positive cells; at 48 h, 0.125 μM caused ~80% Annexin V-positive cells and 0.25 μM caused ~90% Annexin V-positive cells.

Western Blot Analysis[1]

Cell Line: AML U937 cells
Concentration: 0.0675, 0.125 and 0.25 μM
Incubation Time: 48 h
Result: Induced hyperacetylation of histone H3K9 (fold changes relative to DMSO: 3.47 at 0.0675 μM, 5.23 at 0.125 μM, 3.51 at 0.25 μM) and α-tubulin (fold changes relative to DMSO: 3.5 at 0.0675 μM, 4.4 at 0.125 μM, 4.3 at 0.25 μM).
Upregulated the cyclin-dependent kinase inhibitor p21 (fold changes relative to DMSO: 11.1 at 0.0675 μM, 9.9 at 0.125 μM, 6.5 at 0.25 μM).
Downregulated cyclin D1 (fold changes relative to DMSO: 0.42 at 0.0675 μM, 0.53 at 0.125 μM, 0.37 at 0.25 μM).

Real Time qPCR[1]

Cell Line: AML U937 cells
Concentration: 0.0675, 0.125 and 0.25 μM
Incubation Time: 48 h
Result: Significantly upregulated mRNA levels of p21, pro-apoptotic Bak, and pro-apoptotic Bax across all tested concentrations.
Significantly downregulated mRNA levels of cyclin D1 and anti-apoptotic Bcl-2 across all tested concentrations.
SAHA showed no significant effect on Bak, Bax, or Bcl-2 mRNA levels.\nSignificantly downregulated anti-apoptotic miRNAs miR-17-5p, miR-18-5p, miR-20a-5p, miR-21-5p, and miR-22-3p across all tested concentrations, with effects stronger than SAHA for miR-18-5p and miR-22-3p.
Significantly upregulated pro-apoptotic miRNAs miR-122-5p, miR-769-5p, miR-181a-5p, and miR-181b-5p across all tested concentrations.
SAHA showed no significant effect on miR-122-5p or miR-181b-5p.
分子量

409.50

Formula

C22H23N3O3S

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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  • 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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产品名称:
HDAC6-IN-82
目录号:
HY-183560
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