2. Cell Cycle/DNA Damage Epigenetics
  3. HDAC
  4. HDAC3-IN-4

HDAC3-IN-4 是一种选择性且具有口服活性的 HDAC3 抑制剂，IC50 为 89 nM。HDAC3-IN-4 通过调节溶酶体中的组织蛋白酶 B（CTSB）来诱导 PD-L1 的降解，DC50 为 5.7 μM。与 HDAC1、HDAC6、HDAC7 和 HDAC8 相比，HDAC3-IN-4 对 HDAC3 的选择性更好。

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HDAC3-IN-4 Chemical Structure

HDAC3-IN-4 Chemical Structure

CAS No. : 2988762-46-3

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HDAC3-IN-4 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

HDAC3-IN-4 is a selective and orally active HDAC3 inhibitor with an IC50 of 89 nM. HDAC3-IN-4 induces the degradation of PD-L1 by regulating cathepsin B (CTSB) in the lysosomes, with a DC50 of 5.7 μM. HDAC3-IN-4 shows better selectivity for HDAC3 over HDAC1, HDAC6, HDAC7, and HDAC8[1].

IC50 & Target[1]

HDAC3

89 nM (IC50)

HDAC1

730 nM (IC50)

HDAC6

>10 μM (IC50)

HDAC7

>10 μM (IC50)

HDAC8

>10 μM (IC50)

体外研究
(In Vitro)

HDAC3-IN-4（compound HQ-30）表现出强效的抗增殖作用，对 Jurkat（T 淋巴瘤）、HCT-116（结直肠癌）、B16-F10（黑色素瘤）、MCF-7（乳腺癌）和 HepG2（肝癌）细胞的 IC50 值分别为 0.09 μM、0.43 μM、1.20 μM、2.94 μM 和 0.24 μM[1]。
HDAC3-IN-4（0.5-8 μM; 48 h）以浓度依赖性方式诱导 B16-F10 细胞凋亡[1]。
HDAC3-IN-4 (0.5-4 μM; 48 h) 剂量依赖性地增加 B16-F10 细胞中 G2/M 期细胞周期停滞的百分比，并降低 G0/G1 期细胞百分比[1]。
HDAC3-IN-4 (0.5-4 μM; 24 h) 导致乙酰化-H3 (Ac-H3) 显著上调。HDAC3-IN-4 通过溶酶体途径下调/降低 PD-L1 表达[1]。

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

HDAC3-IN-4 相关抗体:

Apoptosis Analysis[1]

Cell Line: B16-F10 cells
Concentration: 0.5 μM, 1 μM, 2 μM, 4 μM, and 8 μM
Incubation Time: 48 h
Result: Induced cancer cell apoptosis.

Cell Cycle Analysis[1]

Cell Line: B16-F10 cells
Concentration: 0.5 μM, 1 μM, 2 μM, 4 μM
Incubation Time: 48 h
Result: Dose-dependently increased the percentage of cell cycle arrest.

Western Blot Analysis[1]

Cell Line: B16-F10 cells
Concentration: 0.5 μM, 1 μM, 2 μM, 4 μM
Incubation Time: 24 h
Result: Caused significant upregulation of acetylated-H3.
体内研究
(In Vivo)

HDAC3-IN-4（compound HQ-30；25 mg/kg；口服；每天；持续 9 天）可减少肿瘤体积和肿瘤重量，并抑制肿瘤生长[1]。
雄性 Sprague-Dawley 大鼠中 HDAC3-IN-4 的药代动力学参数[1]。
1.19

PK parameters i.v. administration (2 mg/kg, n = 6) p.o. administration (20 mg/kg, n = 6)
AUC0-t (ng/mL·h) 521.85 ± 93.78 2742.08 ± 768.82
AUC0-∞ (ng/mL·h) 529.16 ± 91.38 3032.62 ± 805.03
MRT0-t (h) 0.52 ± 0.09 3.19 ± 0.84
MRT0-∞ (h) 0.55 ± 0.10 4.48 ± 1.75
t1/2 (h) 0.4 ± 0.10 3.6 ± 1.6
Tmax (h) 0.14 ± 0.08 0.50 ± 0
CL (L/h/kg) 3.87 ± 0.65 7.27 ± 3.10
Vz (L/kg) 2.21 ± 0.64 34.45 ± 12.38
Cmax (ng/mL) 725.25 ± 169.59 1038.18 ± 514.59
F (%) - 57

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

Animal Model: Six weeks old C57BL/6J male mice (6 weeks old) injected B16 cells[1]
Dosage: 25 mg/kg
Administration: p.o.; per day; for 9 days
Result: Decreased the tumor volume and tumor weight with tumor growth inhibitions.
分子量

423.53

Formula

C22H25N5O2S
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

HDAC3-IN-4 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:

HDAC3-IN-42988762-46-3HDACHistone deacetylasesHDAC3 InhibitorAntitumor Immune EffectsPD-L1Inhibitorinhibitorinhibit

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