2. Cell Cycle/DNA Damage Epigenetics
  3. HDAC
  4. HDAC-IN-56

HDAC-IN-56 ((S)-17b) 是一种口服有效的 I 类组蛋白去乙酰化酶 HDAC 抑制剂，对 HDAC1，HDAC2，HDAC3 和 HDAC4-11 的 IC50 值分别为 56.0±6.0，90.0±5.9，422.2±105.1，>10000 nM。HDAC-IN-56 具有强大抑制活性的同时，强烈增加了细胞内乙酰组蛋白 H3 和 P21 的水平，并有效地诱导了 G1 细胞周期的停滞和凋亡 (Apoptosis)。HDAC-IN-56 具有抗肿瘤活性。

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HDAC-IN-56 Chemical Structure

HDAC-IN-56 Chemical Structure

CAS No. : 2814571-89-4

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HDAC-IN-56 相关抗体

Top Publications Citing Use of Products

查看 HDAC 亚型特异性产品:

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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-56 ((S)-17b) is an orally active class I histone deacetylase (HDAC) inhibitor with IC50 values of 56.0 ± 6.0, 90.0 ± 5.9, 422.2 ± 105.1, >10000 nM for HDAC1, HDAC2, HDAC3, and HDAC4-11, respectively. HDAC-IN-56 has potent inhibitory activity while strongly increasing intracellular levels of acetylhistone H3 and P21 and effectively inducing G1 cell cycle arrest and apoptosis.HDAC-IN-56 has antitumor activity [1].

IC50 & Target

HDAC1

56.0 nM (IC50)

HDAC2

90.0 nM (IC50)

HDAC3

422.2 nM (IC50)

体外研究
(In Vitro)

HDAC-IN-56 对 I 类 HDACs 1，2，和 3 有较强的选择性抑制作用，优于 MS-275 (HY-12163)[1]。
HDAC-IN-56 (0.1μM, 2 h) 在人、猴、狗、大鼠和小鼠肝细胞中的代谢存在明显的物种差异，在五个物种肝细胞中代谢稳定[1]。
HDAC-IN-56 (0.01-1 μM, 72 h) 能有效地诱导 G1 细胞周期停滞和细胞凋亡[1]。
HDAC-IN-56 (0.01-1 μM, 72 h) 处理可同时提高细胞内乙酰组蛋白 H3 和 p21 的水平，效果优于 Tucidinostat (HY-109015) 或MS-275 (HY-12163)，这意味着其对第一类组蛋白去乙酰化酶的抑制作用很强[1]。
HDAC-IN-56 对 SKM-1 的IC50 为 139.0 ± 8.0 nM[1]。

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

HDAC-IN-56 相关抗体:

Cell Cycle Analysis[1]

Cell Line: SKM-1
Concentration: 0.01, 0.1, 1 μM
Incubation Time: 72 h
Result: Downregulated the expression of c-Myc and CDK4 at 0.1 μM, which is better than MS-275 (HY-12163) or Tucidinostat (HY-109015).

Apoptosis Analysis[1]

Cell Line: SKM-1
Concentration: 0.01, 0.1, 1 μM
Incubation Time: 72 h
Result: Triggered strong apoptosis as determined by Annexin V/PI staining, stronger than MS-275 (HY-12163) or Tucidinostat (HY-109015).

Western Blot Analysis[1]

Cell Line: SKM-1
Concentration: 0.01, 0.1, 1 μM
Incubation Time: 72 h
Result: Increased the intracellular level of acetyl-histone H3 and p21 simultaneously better than that of Tucidinostat (HY-109015) or MS-275 (HY-12163).
体内研究
(In Vivo)

HDAC-IN-56 (10-80 mg/kg/d, p.o., one month) 即使在每天 80 mg/kg 的高剂量下，没有引起体重的明显变化[1]。
HDAC-IN-56 (SD: 10, 20 mg/kg ; ICR: 20, 40 mg/kg, p.o.) 具有良好的药代动力学特征，在 ICR 小鼠和 SD 大鼠中的口服生物利用度分别为47.7% 和39.5%[1]。
HDAC-IN-56 (20-60 mg/kg, p.o.) 对裸鼠 MC38 细胞的肿瘤生长有预期的抑制作用，。当接种到免疫功能正常的 C57BL/6 小鼠身上时，在相同的剂量下显示出更明显的肿瘤生长抑制作用，这意味着免疫系统可能被 HDAC-IN-56 参与并以某种方式激活以获得更强的抗肿瘤效果[1]。

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

Animal Model: Male SD rats or ICR mice[1]
Dosage: 10, 20 mg/kg ; ICR: 20, 40 mg/kg
Administration: Male SD rats or ICR mice (n = 6) were fasted for 12 h before administration and remained fasting for 2 h. SD rats were received 10 and 20 mg/kg via intravenously injection (iv) and oral administration (po), respectively, and ICR mice were received 20 and 40 mg/kg via intravenously injection (iv) and oral administration (po), respectively.
Result: Epresented a favorable pharmacokinetic profile with an oral bioavailability of 47.7% in ICR mice and 39.5% in SD rat, respectively
Animal Model: SKM-1 or MC-38 cells xenograft model[1]
Dosage: 20, 40, 60 mg/kg
Administration: Oral gavage (p.o.).
Result: Inhibited the tumor growth of MC38 cells in nude mice.
Showed more significant tumor growth inhibition at the same doses, which implie that the immune system may be engaged and somehow activated HDAC-IN-56 to gain stronger antitumor effect.
分子量

485.55

Formula

C28H28FN5O2
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

HDAC-IN-56 相关分类

  • 摩尔计算器

  • 稀释计算器

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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-562814571-89-4HDACHistone deacetylaseshistone deacetylaseHDAC1HDAC2HDAC3SKM-1HDAC4-11HepatocytesMC-38xenograft modelcancer.Inhibitorinhibitorinhibit

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