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

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)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
B16-F10 IC50
1.2 μM
Compound: HQ-30
Antiproliferative activity against mouse B16-F10 cells assessed as reduction in cell viability measured for 48 hrs by MTT assay
Antiproliferative activity against mouse B16-F10 cells assessed as reduction in cell viability measured for 48 hrs by MTT assay
[PMID: 39031090]
HCT-116 IC50
0.43 μM
Compound: HQ-30
Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability measured for 48 hrs by MTT assay
Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability measured for 48 hrs by MTT assay
[PMID: 39031090]
HepG2 IC50
0.24 μM
Compound: HQ-30
Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability measured for 48 hrs by MTT assay
Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability measured for 48 hrs by MTT assay
[PMID: 39031090]
Jurkat IC50
0.09 μM
Compound: HQ-30
Antiproliferative activity against human Jurkat T cells assessed as reduction in cell viability measured for 48 hrs by CCK-8 assay
Antiproliferative activity against human Jurkat T cells assessed as reduction in cell viability measured for 48 hrs by CCK-8 assay
[PMID: 39031090]
MCF7 IC50
2.94 μM
Compound: HQ-30
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability measured for 48 hrs by MTT assay
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability measured for 48 hrs by MTT assay
[PMID: 39031090]
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)

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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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