Cat. No.: HY-149029

TH-6

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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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Pureté: 95.00%
CAS No.: 3031349-25-1
Formule: C₂₂H₂₄FN₃O₅
Masse moléculaire:429.44

Stockage:

4°C, protect from light

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

TH-6 Chemical Structure

CAS No.: 3031349-25-1

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Fluorescent Dye

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

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Solvant et solubilité
- In Vitro
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

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)

Voir tous les produits spécifiques à Isoform HDAC :

Cellular Effect

Cell Line	Type	Value	Description	References
H22	IC₅₀	26 nM Compound: TH-6	Antiproliferative activity against mouse H22 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay Antiproliferative activity against mouse H22 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay	[PMID: 35926141]
HCT-116	IC₅₀	28 nM Compound: TH-6	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay	[PMID: 35926141]
HepG2	IC₅₀	29 nM Compound: TH-6	Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay	[PMID: 35926141]
HFL1	IC₅₀	13 nM Compound: TH-6	Antiproliferative activity against human HFL1 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay Antiproliferative activity against human HFL1 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay	[PMID: 35926141]
HUVEC	IC₅₀	0.271 μM Compound: TH-6	Antiproliferative activity against HUVEC cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay Antiproliferative activity against HUVEC cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay	[PMID: 35926141]
K562	IC₅₀	0.018 μM Compound: TH-6	Antiproliferative activity against human K562 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay Antiproliferative activity against human K562 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay	[PMID: 35926141]
MCF7	IC₅₀	27 nM Compound: TH-6	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay	[PMID: 35926141]
MDA-MB-231	IC₅₀	30 nM Compound: TH-6	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay	[PMID: 35926141]

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 t_1/2 of 50.3 min^[1].

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

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.

Chemical Information

CAS No. 3031349-25-1
Appearance Solid
Masse moléculaire 429.44
Formule C₂₂H₂₄FN₃O₅
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
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

4°C, protect from light

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

Publications (1)

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Journal Impact Factor

Int J Parasitol Drugs Drug Resist

2026 May 17;31:100649.

Solvant et solubilité

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

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Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.3286 mL

11.6431 mL

23.2861 mL

5 mM

0.4657 mL

2.3286 mL

4.6572 mL

10 mM

0.2329 mL

1.1643 mL

2.3286 mL

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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (276 KB)
SDS (251 KB)
- English - EN (251 KB)
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- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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)
Instruction de manipulation (2659 KB)

Références

[1]. Zhu H, et al. Discovery of a Novel Vascular Disrupting Agent Inhibiting Tubulin Polymerization and HDACs with Potent Antitumor Effects. J Med Chem. 2022 Aug 4. [Content Brief]

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.

Complete Stock Solution Preparation Table

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

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

NF-κB Signaling Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Covalent Screening Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Anti-Breast Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Liver Cancer Compound Library

Osteogenesis Compound Library

Cell Death Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

High-Efficiency Gene Editing Compound Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) TH-6

Voir tous les produits spécifiques à Isoform HDAC

Activité biologique

Chemical Information

Publications (1)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

TH-6

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

NF-κB Signaling Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Covalent Screening Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Anti-Breast Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Liver Cancer Compound Library

Osteogenesis Compound Library

Cell Death Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

High-Efficiency Gene Editing Compound Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) TH-6

Voir tous les produits spécifiques à Isoform HDAC

Activité biologique

Chemical Information

Publications (1)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

TH-6 Related Classifications

HY-149029 Related Classifications