TM-2-51 (Synonyms: 1-Benzoyl-3-phenyl-2-thiourea) |
Catalog No.GB40394
One-Click Copy Product Info
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TM-2-51 is a highly selective histone deacetylase 8 (HDAC8) activator.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 4921-82-8
Sample solution is provided at 25 µL, 10mM.
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TM-2-51 is a highly selective histone deacetylase 8 (HDAC8) activator. TM-2-51 binds to two sites on HDAC8 with positive cooperativity and can enhance the activity of recombinant HDAC8[1-2]. TM-2-51 can be used for research related to cancer[3-4].
In vitro, SH-SY5Y neuroblastoma cells were treated with TM-2-51 (80μM) for 24, 48, and 72 hours. TM-2-51 selectively induced growth inhibition and apoptosis in SH-SY5Y cells and enhanced the expression levels of p53 and p21 proteins[5]. Human renal proximal tubule HK-2 cells and rat renal proximal tubule NRK-52E cells were treated with TM-2-51 (25–50μM) (cobalt stimulation; 20-22 hours; or during hypoxia/reoxygenation (H/R) stimulation; 16-18h). TM-2-51 significantly prevented cobalt- and H/R-induced cytotoxicity, mitochondrial fission and dysfunction, and inhibited the upregulation of DRP1 expression and the increase in histone H3 lysine 27 acetylation (H3K27ac) levels[6].
In vivo, BALB/C nude mice subcutaneously inoculated with 143B osteosarcoma cells received intraperitoneal injections of TM-2-51 (10mg/kg) every two days for two weeks. TM-2-51 significantly inhibited tumor growth[7].
References:
[1] Li Y, Xiao G, Fu X, et al. CH25H/25-HC promotes pulmonary fibrosis via AMPK/STAT6 pathway-dependent M2 macrophage polarization in COPD. Immunobiology. 2025 May;230(3):152908.
[2] Du J, Li W, Liu B, et al. An in silico mechanistic insight into HDAC8 activation facilitates the discovery of new small-molecule activators. Bioorg Med Chem. 2020 Aug 15;28(16):115607.
[3] Singh RK, Mandal T, Balsubramanian N, et al. Histone deacetylase activators: N-acetylthioureas serve as highly potent and isozyme selective activators for human histone deacetylase-8 on a fluorescent substrate. Bioorg Med Chem Lett. 2011 Oct 1;21(19):5920-3.
[4] Mukhtar YM, Huang Y, Liu J, et al. Acetanilide and bromoacetyl-lysine derivatives as activators for human histone deacetylase 8. Bioorg Med Chem Lett. 2017 Jun 1;27(11):2319-2323.
[5] Singh RK, Cho K, Padi SK, et al. Mechanism of N-Acylthiourea-mediated activation of human histone deacetylase 8 (HDAC8) at molecular and cellular levels. J Biol Chem. 2015 Mar 6;290(10):6607-19.
[6] Ha SD, Solomon O, Akbari M, et al. Histone deacetylase 8 protects human proximal tubular epithelial cells from hypoxia-mimetic cobalt- and hypoxia/reoxygenation-induced mitochondrial fission and cytotoxicity. Sci Rep. 2018 Jul 27;8(1):11332.
[7] Wang L, Bai X, Zhang X, et al. Activation of HDAC8 Can Suppress the Proliferation of Osteosarcoma Cells via TP53 and STAT3/ERK Signaling Pathways. Ann Clin Lab Sci. 2023 Nov;53(6):920-930.
| Cell experiment [1]: | |
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Cell lines |
SH-SY5Y and BE(2)-C human neuroblastoma cell lines |
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Preparation Method |
Cells were grown in Dulbecco's modified Eagle's medium (DMEM) supplemented with 10% (v/v) heat-inactivated fetal bovine serum (FBS) and 1% (v/v) antibiotic-antimycotic solution. Cells were treated with TM-2-51 (80μM) for 72 hours (apoptosis assay); for proliferation assay, cells were treated with different concentrations of TM-2-51 for 24, 48, and 72 hours. |
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Reaction Conditions |
80μM; 24-72 hours. |
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Applications |
TM-2-51 selectively induced growth inhibition and apoptosis in SH-SY5Y cells but showed no such effects in BE(2)-C cells. The protein expression levels of p53 and p21 were enhanced in TM-2-51-treated SH-SY5Y cells but not in BE(2)-C cells. |
| Animal experiment [2]: | |
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Animal models |
BALB/C nude mice |
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Preparation Method |
143B cells were subcutaneously inoculated into the axilla of nude mice. One week later, nude mice were randomly assigned into two groups and received DMSO or TM-2-51 (10mg/kg) via intraperitoneal injection every 2 days for the next two weeks. |
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Dosage form |
10mg/kg; i.p.; every 2 days for 2 weeks. |
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Applications |
TM-2-51 administration significantly suppressed the growth of tumors in vivo. HE and Ki67 staining revealed that the proliferation ability of tumor tissue was obviously reduced in the TM-2-51 treated group. |
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References: |
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| Cas No. | 4921-82-8 | SDF | |
| Synonyms | 1-Benzoyl-3-phenyl-2-thiourea | ||
| Formula | C14H12N2OS | M.Wt | 256.32 |
| Solubility | DMSO: ＞10mg/ml | Storage | Store at 2-8°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.9014 mL | 19.5069 mL | 39.0137 mL |
| 5 mM | 780.3 μL | 3.9014 mL | 7.8027 mL |
| 10 mM | 390.1 μL | 1.9507 mL | 3.9014 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)