2. Cell Cycle/DNA Damage Epigenetics Apoptosis Immunology/Inflammation NF-κB Metabolic Enzyme/Protease
  3. HDAC Apoptosis Reactive Oxygen Species
  4. TH-6

TH-6 is a potent HDAC inhibitor with IC50s of 0.115, 0.135, 0.242, 0.138, 2.120 µM for HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, respectively. TH-6 inhibits cell migration and invasion. TH-6 induces apoptosis and cell cycle arrest at G2/M phase. TH-6 shows anti-tumor activity.

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TH-6 Chemical Structure

TH-6 Chemical Structure

CAS No. : 3031349-25-1

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 348 In-stock
Solution
10 mM * 1 mL in DMSO USD 348 In-stock
Solid
1 mg USD 175 In-stock
5 mg USD 368 In-stock
10 mg USD 590 In-stock
25 mg USD 1180 In-stock
50 mg USD 1887 In-stock
100 mg USD 3020 In-stock
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Based on 1 publication(s) in Google Scholar

TH-6 Related Antibodies

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View All HDAC Isoform Specific Products:

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

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Description

TH-6 is a potent HDAC inhibitor with IC50s of 0.115, 0.135, 0.242, 0.138, 2.120 µM for HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, respectively. TH-6 inhibits cell migration and invasion. TH-6 induces apoptosis and cell cycle arrest at G2/M phase. TH-6 shows anti-tumor activity[1].

IC50 & Target[1]

HDAC1

0.115 μM (IC50)

HDAC2

0.135 μM (IC50)

HDAC3

0.242 μM (IC50)

HDAC6

0.138 μM (IC50)

HDAC8

2.120 μM (IC50)

In Vitro

TH-6 (0-2 µM) shows antiproliferative activities in cancer cell lines and normal human lung cells[1].
TH-6 (0-10 µM) inhibits tubulin polymerization with an IC50 value of 4.06 µM[1].
TH-6 (0.03, 0.1, 0.3 1 µM; 24 h) increases the expression of Ac-α-Tubulin and AC-Histone H3 in HepG2 cells[1].
TH-6 (7.5, 15, 30 nM) induces apoptosis and cell cycle arrest at G2/M phase[1].
TH-6 (0-30 nM) decreases the MMP and increase ROS levels of HepG2 cells in a dose-dependent manner[1].
TH-6 (7.5, 15, 30 nM; 48 h) inhibits cell migration and invasion in MDA-MB-231 cells and suppress the migration of HUVECs in a concentration-dependent manner[1].
TH-6 shows favorable liver microsomal stability in vitro with t1/2 of 50.3 min[1].

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

TH-6 Related Antibodies

Cell Viability Assay[1]

Cell Line: K562, GepG2, HCT-116, MDA-MB-231, H22, MCF-7, HFL-1 cells
Concentration: 0-2 µM
Incubation Time:
Result: Showed antiproliferative activities with an IC50 values of 18, 29, 28, 30, 26, 27, 134 nM for K562, GepG2, HCT-116, MDA-MB-231, H22, MCF-7, HFL-1 cells, respectively.

Western Blot Analysis[1]

Cell Line: HepG2 cells
Concentration: 0.03, 0.1, 0.3 1 µM
Incubation Time: 24 h
Result: Increased the intracellular levels of HDAC6 substrate acetyl-α-tubulin and the HDAC1/2/3 substrate acetyl-histone H3 in a dose-dependent manner.

Cell Cycle Analysis[1]

Cell Line: HepG2 cells
Concentration: 7.5, 15, 30 nM
Incubation Time:
Result: Induced cell cycle arrest at G2/M phase with decreased the expression of Cdc2, Cdc25c, and Cyclin B1 proteins in a dose dependent manner.

Apoptosis Analysis[1]

Cell Line: HepG2 cells
Concentration: 7.5, 15, 30 nM
Incubation Time:
Result: Showed an accumulation of apoptotic cells from 27.04 to 50.54% and upregulated the expression of the pro-apoptotic protein (Bax and Bad) and downregulated the expression of the antiapoptotic protein (Bcl-2 and Bcl-xL) in a dose-dependent manner.
In Vivo

TH-6 (10, 20 mg/kg; i.v.; daily for 21 days) shows anti-tumor activity in mouse[1].
TH-6 (20 mg/kg) shows antivascular activity and a good cardiovascular safety profile in mouse[1].

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

Animal Model: 4-5 weeks, 18-22 g female ICR mice (H22 allograft mouse model)[1]
Dosage: 10, 20 mg/kg
Administration: I.v.; daily for 21 days
Result: Reduced tumor weights at day 21 by 82% and did not affect body weight during treatment, indicating the low toxicity.
Molecular Weight

429.44

Formula

C22H24FN3O5
CAS No.
Appearance

Solid

Color

Light yellow to khaki

SMILES

ONC(/C=C/C(C=C1CNC(C2=C(N3CCOCC3)C=CC(F)=C2)=O)=C(C=C1)OC)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (116.43 mM; ultrasonic and warming and heat to 60°C; 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 2.3286 mL 11.6431 mL 23.2861 mL
5 mM 0.4657 mL 2.3286 mL 4.6572 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 (protect from light). 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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In Vivo Dissolution Calculator
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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 (protect from light). 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 2.3286 mL 11.6431 mL 23.2861 mL 58.2153 mL
5 mM 0.4657 mL 2.3286 mL 4.6572 mL 11.6431 mL
10 mM 0.2329 mL 1.1643 mL 2.3286 mL 5.8215 mL
15 mM 0.1552 mL 0.7762 mL 1.5524 mL 3.8810 mL
20 mM 0.1164 mL 0.5822 mL 1.1643 mL 2.9108 mL
25 mM 0.0931 mL 0.4657 mL 0.9314 mL 2.3286 mL
30 mM 0.0776 mL 0.3881 mL 0.7762 mL 1.9405 mL
40 mM 0.0582 mL 0.2911 mL 0.5822 mL 1.4554 mL
50 mM 0.0466 mL 0.2329 mL 0.4657 mL 1.1643 mL
60 mM 0.0388 mL 0.1941 mL 0.3881 mL 0.9703 mL
80 mM 0.0291 mL 0.1455 mL 0.2911 mL 0.7277 mL
100 mM 0.0233 mL 0.1164 mL 0.2329 mL 0.5822 mL
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TH-6 Related Classifications

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:

TH-63031349-25-1TH6TH 6HDACApoptosisReactive Oxygen SpeciesHistone deacetylasesantiproliferativemigrationinvasionapoptosisG2/M phaseROSInhibitorinhibitorinhibit

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