HDAC3-IN-4

CAS: 2988762-46-3 F: C22H25N5O2S W: 423.53

HDAC3-IN-4 is a selective and orally active HDAC3 inhibitor with an IC50 of 89 nM. HDAC3-IN-4 induces the degradation of

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Bioactivity	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].
Invitro	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. 0 --> HDAC3-IN-4 相关抗体: Apoptosis Analysis[1] Cell Line:
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
CAS	2988762-46-3
Formula	C22H25N5O2S
Molar Mass	423.53
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Zhiqiang Sun, et al. Discovery of Novel HDAC3 Inhibitors with PD-L1 Downregulating/Degrading and Antitumor Immune Effects. J Med Chem. 2024 Jul 20.

Antitumor agent-182