1. Cell Cycle/DNA Damage Epigenetics Metabolic Enzyme/Protease Immunology/Inflammation NF-κB Apoptosis MAPK/ERK Pathway
  2. HDAC DNA/RNA Synthesis Reactive Oxygen Species (ROS) Apoptosis Caspase p38 MAPK
  3. HDAC9-IN-1

HDAC9-IN-1 is a selective class IIa HDAC inhibitor that binds to HDAC9 with an IC50 of 40 nM. HDAC9-IN-1 potently inhibits HDACs 4 and 7 while showing weak activity against HDAC6 (IC50 values: 180 nM (HDAC4), 190 nM (HDAC7), 970 nM (HDAC6)). HDAC9-IN-1 significantly inhibits several human cancer cells, induces apoptosis and DNA damage in human cancer cells, and modulates caspase-related proteins and p38 in human cancer cells. HDAC9-IN-1 can be used for the research of oral cancer, breast cancer, gastric cancer.

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

HDAC9-IN-1

HDAC9-IN-1 Chemical Structure

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
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10 mg In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

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  • Customer Review

Description

HDAC9-IN-1 is a selective class IIa HDAC inhibitor that binds to HDAC9 with an IC50 of 40 nM. HDAC9-IN-1 potently inhibits HDACs 4 and 7 while showing weak activity against HDAC6 (IC50 values: 180 nM (HDAC4), 190 nM (HDAC7), 970 nM (HDAC6)). HDAC9-IN-1 significantly inhibits several human cancer cells, induces apoptosis and DNA damage in human cancer cells, and modulates caspase-related proteins and p38 in human cancer cells. HDAC9-IN-1 can be used for the research of oral cancer, breast cancer, gastric cancer[1].

IC50 & Target

HDAC9

40 nM (IC50)

HDAC4

180 nM (IC50)

HDAC7

190 nM (IC50)

HDAC6

970 nM (IC50)

Caspase-8

 

Caspase-9

 

In Vitro

HDAC9-IN-1 (compound 7g) (5-30 min) potently inhibits HDAC 9 and class IIa HDACs 4 and 7 while showing weak activity against HDAC 6 and no activity against class I HDACs (IC50 values: 40 nM (HDAC9), 180 nM (HDAC4), 190 nM (HDAC7), 970 nM (HDAC6), >40 μM (class I))[1].
HDAC9-IN-1 (24 h) inhibits viability of cancer cells and normal lung fibroblasts (IC50 values: 3.0 μM (SCC2095), 8.4 μM (MDA-MB-231), 5.8 μM (SCM-1), 8.0 μM (normal lung fibroblasts))[1].
HDAC9-IN-1 (1-10 μM; 24-48 h) induces dose- and time-dependent apoptosis in SCC2095 cells[1].
HDAC9-IN-1 (1-10 μM; 24 h) modulates apoptotic, HDAC substrate, and stress response proteins in SCC2095 cells[1].
HDAC9-IN-1 (2.5-5 μM; 12-24 h) increases ROS generation accompanied by the increased DNA damage in SCC2095 cells in a time-dependent manner[1].

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

Apoptosis Analysis[1]

Cell Line: Human oral cancer SCC2095 cells
Concentration: 1 μM, 2.5 μM, 5 μM, 7.5 μM, and 10 μM
Incubation Time: 24 h, 48 h
Result: Induced apoptosis in a dose- and time-dependent manner: 10 μM for 24 h increased apoptotic cells to 83.6%; 1, 2.5, 5, 7.5, 10 μM for 48 h resulted in apoptosis rates of 29.2%, 35.9%, 44.4%, 78.2%, and 87.1%, respectively.

Western Blot Analysis[1]

Cell Line: SCC2095 cells
Concentration: 1 μM, 2.5 μM, 5 μM, 7.5 μM, and 10 μM
Incubation Time: 24 h
Result: Down-regulated the levels of pro-caspase 8 and up-regulated the levels of cleaved caspase 9.
The levels of HDAC6 substrates such as acetyl-α-tubulin and Hsp90, and two class IIa HDAC-related proteins including
PPARγ and p21 were increased.
Up-regulated the phosphorylation of p38 in a dose-dependent manner in SCC2095 cells.
Increased the phosphorylation of Histone H2A.X, a DNS damage biomarker.
Molecular Weight

482.55

Formula

C27H22N4O3S

Appearance

Solid

Color

Light brown to brown

SMILES

N/C(C1=CC2=C(SC3=CC=CC=C3N2CC4=CC=C(C(C5=CC=CC=C5)=C4)C(NO)=O)C=C1)=N\O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (103.62 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0723 mL 10.3616 mL 20.7232 mL
5 mM 0.4145 mL 2.0723 mL 4.1446 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0723 mL 10.3616 mL 20.7232 mL 51.8081 mL
5 mM 0.4145 mL 2.0723 mL 4.1446 mL 10.3616 mL
10 mM 0.2072 mL 1.0362 mL 2.0723 mL 5.1808 mL
15 mM 0.1382 mL 0.6908 mL 1.3815 mL 3.4539 mL
20 mM 0.1036 mL 0.5181 mL 1.0362 mL 2.5904 mL
25 mM 0.0829 mL 0.4145 mL 0.8289 mL 2.0723 mL
30 mM 0.0691 mL 0.3454 mL 0.6908 mL 1.7269 mL
40 mM 0.0518 mL 0.2590 mL 0.5181 mL 1.2952 mL
50 mM 0.0414 mL 0.2072 mL 0.4145 mL 1.0362 mL
60 mM 0.0345 mL 0.1727 mL 0.3454 mL 0.8635 mL
80 mM 0.0259 mL 0.1295 mL 0.2590 mL 0.6476 mL
100 mM 0.0207 mL 0.1036 mL 0.2072 mL 0.5181 mL
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  • 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.

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Product Name:
HDAC9-IN-1
Cat. No.:
HY-169259
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