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Cat. No.: HY-150722

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HDAC6-IN-12

HDAC6-IN-12 (compound GZ) is a potent HDAC6 inhibitor. HDAC6-IN-12 has anticancer activity through merges into DNA strands causing DNA damage. HDAC6-IN-12 can be used for cancer research.

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

CAS No.: 2803866-44-4
Formula: C₂₄H₃₉F₂N₃O₅
Molecular Weight:487.58

Storage:

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

Data Sheet (267 KB)

HDAC6-IN-12 Chemical Structure

CAS No.: 2803866-44-4

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Use of MCE Products

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

Biological Activity
- Description
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Protocols (1)
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

HDAC6-IN-12 (compound GZ) is a potent HDAC6 inhibitor. HDAC6-IN-12 has anticancer activity through merges into DNA strands causing DNA damage. HDAC6-IN-12 can be used for cancer research^[1].

All HDAC Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
4T1	IC₅₀	0.66 μM Compound: GZ	Antiproliferative activity against mouse 4T1 cells assessed as inhibition of cell growth Antiproliferative activity against mouse 4T1 cells assessed as inhibition of cell growth	[PMID: 35810950]
A549	IC₅₀	0.14 μM Compound: GZ	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth Antiproliferative activity against human A549 cells assessed as inhibition of cell growth	[PMID: 35810950]
HCT-116	IC₅₀	0.3 μM Compound: GZ	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth	[PMID: 35810950]
HeLa	IC₅₀	0.43 μM Compound: GZ	Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth	[PMID: 35810950]
Huh-7	IC₅₀	0.12 μM Compound: GZ	Antiproliferative activity against human Huh-7 cells assessed as inhibition of cell growth Antiproliferative activity against human Huh-7 cells assessed as inhibition of cell growth	[PMID: 35810950]
MDA-MB-231	IC₅₀	0.072 μM Compound: GZ	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated in presence of 10 uM imatinib Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated in presence of 10 uM imatinib	[PMID: 35810950]
MDA-MB-231	IC₅₀	0.14 μM Compound: GZ	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth	[PMID: 35810950]
MDA-MB-231	IC₅₀	0.17 μM Compound: GZ	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth pretreated with hENT1 inhibitor, dipyridamole at 10 uM followed by compound addition Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth pretreated with hENT1 inhibitor, dipyridamole at 10 uM followed by compound addition	[PMID: 35810950]
PANC-1	IC₅₀	1.08 μM Compound: GZ	Antiproliferative activity against human PANC-1 cells assessed as inhibition of cell growth Antiproliferative activity against human PANC-1 cells assessed as inhibition of cell growth	[PMID: 35810950]
SGC-7901	IC₅₀	3.7 μM Compound: GZ	Antiproliferative activity against human SGC-7901 cells assessed as inhibition of cell growth Antiproliferative activity against human SGC-7901 cells assessed as inhibition of cell growth	[PMID: 35810950]
SK-OV-3	IC₅₀	0.62 μM Compound: GZ	Antiproliferative activity against human SK-OV-3 cells assessed as inhibition of cell growth Antiproliferative activity against human SK-OV-3 cells assessed as inhibition of cell growth	[PMID: 35810950]

In Vitro

HDAC6-IN-12 (compound GZ) (72 h) has anti-proliferative activity on tumor cells against HuH-7, HeLa, MDA-MB-231, SKOV3, A549, PANC-1, HCT-116, SGC7901 and 4T1 cells with IC₅₀ values of 0.12 μM, 0.43 μM, 0.14 μM, 0.62 μM, 0.14 μM, 1.08 μM, 0.30 μM, 3.70 μM and 0.66 μM, respectively^[1].
HDAC6-IN-12 (compound GZ) (0-3 μM; 24 h; MBA-MB-231 cells) merges into DNA strands causing DNA damage and increases the level of phospho-γ-H2A.X, which is the marker of DNA strand break^[1].
HDAC6-IN-12 (compound GZ) (0-100 μM; 30 min) has major metabolic enzymes including CYP3A2, CYP1A1/2 isoforms^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.

Western Blot Analysis^[1]

View Protocol

Cell Line:

MBA-MB-231 cells
Concentration:

0, 0.1, 0.3, 1 and 3 μM
Incubation Time:

24 hours
Result:

Increased the level of phospho-γ-H2A.X in a dose-dependent manner.

In Vivo

HDAC6-IN-12 (compound GZ) (5-10 mg/kg; i.p.; once every three days, for 15 d; bablc female mice) inhibits tumor growth in a dose-dependent manner^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Bablc female mice^[1]
Dosage:

5 and 10 mg/kg
Administration:

Intraperitoneal injection; once every three days, for 15 days
Result:

Inhibited tumor growth with TGI of 73.2% at 5 mg/kg and 83.8% at 10 mg/kg, respectively.

Chemical Information

CAS No. 2803866-44-4
Molecular Weight 487.58
Formula C₂₄H₃₉F₂N₃O₅
SMILES

CCCCCCCCCCCCCCC(NC(C=CN1[C@@H]2O[C@H](CO)[C@H](C2(F)F)O)=NC1=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Protocols

All Animals and Diseases

Genotoxicity/Mutagenicity Study
The bacterial reverse mutation assay detects point mutations that restore amino-acid prototrophy in auxotrophic Salmonella typhimurium or Escherichia coli tester strains; after exposure to a test article, mutagenic activity is read out as an increased number of revertant colonies on minimal agar compared with the vehicle control. The assay uses tester strains with different mutation targets so that base-substitution and frameshift mutagens can be detected, and testing is performed with and without exogenous mammalian metabolic activation because some chemicals require biotransformation to become mutagenic.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (267 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]. Li Y, et, al. Design, synthesis and antitumor activity study of a gemcitabine prodrug conjugated with a HDAC6 inhibitor. Bioorg Med Chem Lett. 2022 Sep 15;72:128881. [Content Brief]

Calculators

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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.

Bioz

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100 mg

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