1. Cell Cycle/DNA Damage Epigenetics Autophagy Apoptosis
  2. HDAC Autophagy Apoptosis
  3. HDAC6-IN-76

HDAC6-IN-76 (Compound G25) 是一种选择性 HDAC6 抑制剂,IC50 为 12 nM。HDAC6-IN-76 以 p53 依赖的方式诱导自噬 (Autophagy) 。HDAC6-IN-76 以 p53 依赖的方式诱导细胞凋亡 (Apoptosis)。HDAC6-IN-76 对血液系统恶性肿瘤,包括急性髓系白血病具有抗癌活性。

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HDAC6-IN-76

HDAC6-IN-76 Chemical Structure

CAS No. : 3110559-06-0

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HDAC6-IN-76 (Compound G25) is a selective HDAC6 inhibitor with an IC50 of 12 nM. HDAC6-IN-76 induces Autophagy in a p53-dependent manner. HDAC6-IN-76 induces Apoptosis in a p53-dependent manner. HDAC6-IN-76 exhibits anticancer activity against hematologic malignancies, including acute myeloid leukemia[1].

IC50 & Target[1]

HDAC6

12 nM (IC50)

体外研究
(In Vitro)

HDAC6-IN-76 是一种强效且选择性的 HDAC6 抑制剂,IC50 为 12 nM[1]
HDAC6-IN-76 对白血病和实体瘤细胞系均表现出广谱、强效的抗增殖活性,对 MV4-11 细胞的活性尤为突出,IC50 为 0.028 μM[1]
HDAC6-IN-76 (0.1-1 μM; 24 h) 可以剂量依赖的方式有效抑制 HCT116 结肠癌细胞的迁移[1]
HDAC6-IN-76 (0.1-1 μM; 24 h) 可在 MV4-11 和 HL60 白血病细胞中以浓度依赖的方式诱导自噬[1]

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

Western Blot Analysis[1]

Cell Line: MV4-11 and HL60 leukemia cells
Concentration: 0.1-1 μM
Incubation Time: 24 h
Result: Led to a concentration-dependent increase in LC3B-II expression (conversion of LC3B-I to LC3B-II) in both MV4-11 and HL60 cells.
Caused a concentration-dependent decrease in p62 expression in both MV4-11 and HL60 cells, indicating enhanced autophagic flux.

Cell Cycle Analysis[1]

Cell Line: MV4-11 (p53-wild type) and HL60 (p53-null) leukemia cells
Concentration: 1 μM
Incubation Time: 24 h
Result: Arrested MV4-11 cells in the G0/G1 phase, with 86.71% of cells in this phase.
Arrested HL60 cells in the G2/M phase, with 34.13% of cells in this phase.
药代动力学
(Parmacokinetics)
Species Dose Route T1/2 Tmax Cmax AUC0-t AUC0-∞ MRT0-t MRT0-∞ Bioavailability C0
Rat[1] 2 mg/kg i.v. 0.208 h 0.0833 h 123 ng/mL 39.3 ng·h/mL 40.8 ng·h/mL 0.178 h 0.220 h / 213 ng/mL
Rat[1] 10 mg/kg i.p. 0.305 h 0.25 h 221 ng/mL 135 ng·h/mL 137 ng·h/mL 0.540 h 0.566 h 67.3 % /
体内研究
(In Vivo)

HDAC6-IN-76 (20 mg/kg;腹腔注射,每日 1 次) 在 MOLM-13-Luc 急性髓系白血病异种移植小鼠模型中表现出抗白血病活性,可通过肿瘤进展受抑制及生存期呈延长趋势得到证实[1]

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

分子量

460.52

Formula

C24H32N2O7

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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HDAC6-IN-76
目录号:
HY-181805
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