HDAC6-IN-4

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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.

For research use only. We do not sell to patients.

HDAC6-IN-4 Chemical Structure

CAS No. : 2709103-20-6

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•Related Small Molecules:

•Related Proteins:

View All HDAC Isoform Specific Products:

View All Isoforms

HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

HDAC6

23 nM (IC₅₀)

HDAC3

46 nM (IC₅₀)

HDAC2

172 nM (IC₅₀)

HDAC8

2175 nM (IC₅₀)

HDAC1

3604 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	5.77 μM Compound: C10	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay Antiproliferative activity against human A549 cells after 72 hrs by MTT assay	[PMID: 35245830]
B16	IC₅₀	1.52 μM Compound: C10	Antiproliferative activity against mouse B16 cells after 72 hrs by MTT assay Antiproliferative activity against mouse B16 cells after 72 hrs by MTT assay	[PMID: 35245830]
CT26	IC₅₀	2.09 μM Compound: C10	Antiproliferative activity against mouse CT26 cells after 72 hrs by MTT assay Antiproliferative activity against mouse CT26 cells after 72 hrs by MTT assay	[PMID: 35245830]
HepG2	IC₅₀	2.36 μM Compound: C10	Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay	[PMID: 35245830]

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].

MedChemExpress (MCE) 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].

MedChemExpress (MCE) 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⁺CD127^low/- T regulatory cells. Showed no obvious toxicity.

Molecular Weight

506.63

Formula

C₃₀H₃₈N₂O₅

CAS No.

2709103-20-6

SMILES

O=C(NO)CCCCCCNCC1=C(OC)C=C(OCC2=C(C)C(C3=CC=CC=C3)=CC=C2)C=C1OC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[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. [Content Brief]

HDAC6-IN-4 Related Classifications

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This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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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:

HDAC6-IN-42709103-20-6HDACApoptosisHistone deacetylasesB16HepG2A549CT26Ac-TubIFN-gT cellHDAC2HDAC3Inhibitorinhibitorinhibit

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