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Cat. No.: HY-144395

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HDAC6-IN-4

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.

CAS No.: 2709103-20-6
Formula: C₃₀H₃₈N₂O₅
Molecular Weight:506.63

Storage:

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

Data Sheet (269 KB)

HDAC6-IN-4 Chemical Structure

CAS No.: 2709103-20-6

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

HDAC6

23 nM (IC₅₀)

HDAC3

46 nM (IC₅₀)

HDAC2

172 nM (IC₅₀)

HDAC8

2175 nM (IC₅₀)

HDAC1

3604 nM (IC₅₀)

All HDAC Isoforms :

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.

Chemical Information

CAS No. 2709103-20-6
Molecular Weight 506.63
Formula C₃₀H₃₈N₂O₅
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (269 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
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]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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HDAC6-IN-4

All HDAC Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

HDAC6-IN-4 Related Classifications

HY-144395 Related Classifications