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製品番号: 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.

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CAS 番号: 2709103-20-6
分子式: C₃₀H₃₈N₂O₅
分子量:506.63

保管条件:

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

Data Sheet (269 KB)

HDAC6-IN-4 構造式

CAS 番号: 2709103-20-6

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価格（税別）

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数量

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Fluorescent Dye

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

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- 体内実験
化学情報
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target

HDAC6

23 nM (IC₅₀)

HDAC3

46 nM (IC₅₀)

HDAC2

172 nM (IC₅₀)

HDAC8

2175 nM (IC₅₀)

HDAC1

3604 nM (IC₅₀)

HDAC アイソフォーム固有の製品をすべて表示 :

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]

体外実験

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.

体内実験

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.

化学情報

CAS 番号 2709103-20-6
分子量 506.63
分子式 C₃₀H₃₈N₂O₅
SMILES

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

Room temperature in continental US; may vary elsewhere.
保管条件

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

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (269 KB)
COA (2659 KB)
元素分析報告書 (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)
取扱説明書 (2659 KB)

参考文献

[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]

Calculators

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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希釈計算機

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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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Amount: USD 0.00

生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
- 体内実験
化学情報
純度とドキュメンテーション
参考文献

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HDAC6-IN-4

HDAC アイソフォーム固有の製品をすべて表示

生物活性

化学情報

純度とドキュメンテーション

参考文献

Calculators

Help & FAQs

HDAC6-IN-4 関連分類

HY-144395 関連分類