HDAC6-IN-4 (C10) 是一种有效的、具有口服活性的、高选择性的 HDAC6 抑制剂, IC50 值为23 nM。HDAC6-IN-4 诱导肿瘤细胞凋亡 (apoptosis),具有显著的抗肿瘤作用,且无明显毒性。


HDAC6-IN-4 Chemical Structure

CAS No. : 2709103-20-6

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HDAC6-IN-4 (C10) is a potent, orally active and highly selective HDAC6 inhibitor with an IC50 value of 23 nM. HDAC6-IN-4 induces cancer cells apoptosis and shows significant antitumor efficacy, without obvious toxicity[1].

IC50 & Target


23 nM (IC50)


46 nM (IC50)


172 nM (IC50)


2175 nM (IC50)


3604 nM (IC50)

(In Vitro)

HDAC6-IN-4 (C10) (0-50 µM, 72 h) shows strong antiproliferative activity against different cancer cells with low cytotoxicity[1].
HDAC6-IN-4 (0-6 µM, 24 h) exhibits significant selectivity for HDAC6 over HDAC1[1].
HDAC6-IN-4 inhibits migration activity in a time-dependent and dose-dependent way in B16 and CT26 cells[1].
HDAC6-IN-4 (0-8 µM, 24 h) induces B16 cell apoptosis in a dose-dependent manner[1].
HDAC6-IN-4 exhibits significant plasma stability in humans (97% retention after 6 h), and exhibits significant metabolic stability in human (half-life of 101.91 min) and mouse liver (half-life of 67.94 min) microsomes[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: B16, HepG2, A549, and CT26 cells
Concentration: 0-50 µM
Incubation Time: 72 h
Result: Showed antiproliferative activity with IC50 values of 1.52, 2.36, 5.77, and 2.09 µM against B16, HepG2, A549, and CT26 cells, respectively.

Western Blot Analysis[1]

Cell Line: B16 and CT26 cancer cells
Concentration: 2, 4, and 6 µM
Incubation Time: 2, 4, 8, 12, and 24 h
Result: Dramatically increased the level of Ac-Tub (acetyl-α-tubulin) in a dose-dependent and time-dependent manner. Had almost no effect on the content of Ac-H3 (acetyl-H3).

Apoptosis Analysis[1]

Cell Line: B16 cells
Concentration: 4, 6, and 8 µM
Incubation Time: 24 h
Result: Caused moderate to potent induction of apoptosis in the B16 cell line in a dose-dependent manner. Upregulated the expression of apoptotic protein cleaved PARP.

(In Vivo)

HDAC6-IN-4 (C10) (0-100 mg/kg; i.g.; once daily for 21 days) shows excellent antitumor activity and significantly promoted T cell response in a dose-dependent manner, with no obvious toxicity[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Five-week-old C57BL/6 mice (immune-related CT26 xenograft model)[1].
Dosage: 50 and 100 mg/kg
Administration: Oral gavage, once daily for 21 days
Result: Resulted in a substantial tumor growth and tumor tissue size inhibition in a dose-dependent way. Showed significantly high antitumor activity (TGI = 75%) at 100 mg/kg. Raised the plasma IFN-g level and the numbers of CD+ and CD3+CD+ (activated cytotoxic T) cells. Decreased CD4+CD25+CD127low/- T regulatory cells. Showed no obvious toxicity.








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  • [1]. Xi Xu, et al. Novel biphenyl-based scaffold as potent and selective histone deacetylase 6 (HDAC6) inhibitors: Identification, development and pharmacological evaluation. Eur J Med Chem. 2022 Apr 5;233:114228.