TM-2-51
Based on 1 Customer Validation
TM-2-51 is a HDAC8 activator with a Kd value of 0.28 μM. TM-2-51 inhibits α-glucosidase with an IC50 of 171.21 μM. TM-2-51 upregulates HDAC8 expression, modulates the TP53, STAT3/ERK and PI3K-AKT pathways, alleviates LeTx-induced cell cycle arrest, downregulates JMJD3 and increases H3K27me3 levels. TM-2-51 selectively induces apoptosis in tumor cell and upregulates p53/p21 expression. TM-2-51 inhibits tumor cell proliferation, migration and invasion, induces G1-phase arrest and suppresses tumor growth in vivo. TM-2-51 can be used in research on osteosarcoma, anthrax, type 2 diabetes and neuroblastoma.
For research use only. We do not sell to patients.
- Purity: 99.84%
- CAS No.: 4921-82-8
- Formula: C14H12N2OS
- Molecular Weight:256.32
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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HDAC8 0.28 μM (Kd) |
α-Glucosidase 171.21 μM (IC50) |
TM-2-51 (72 h) potently reduces the viability of U2OS and 143B osteosarcoma cells in a concentration-dependent manner[1].
TM-2-51 (6 days) significantly inhibits the colony-forming ability of U2OS and 143B osteosarcoma cells[1].
TM-2-51 (24 h) significantly reduces the proliferation rate of U2OS and 143B osteosarcoma cells[1].
TM-2-51 (24 h) potently inhibits the migration and invasion abilities of U2OS and 143B osteosarcoma cells[1].
TM-2-51 increases the expression levels of HDAC8 and TP53 proteins above the DMSO baseline in U2OS and 143B osteosarcoma cells, while reduces the expression levels of p-STAT3 and p-ERK proteins below the DMSO baseline, without altering the expression levels of total STAT3 and ERK[1].
TM-2-51 (13-50 μM; 48-96 h) protects the human monocytic cell line THP-1 cells against LeTx-induced cytotoxicity, with its cytoprotective effect peaking at 25 μM and enabling continuous cell proliferation within 96 h[2].
TM-2-51 (25 μM; 24-72 h) enhances the phosphorylation level of AKT at Ser-473 in LeTx-treated human monocytic THP-1 cells at a concentration of 25 μM[2].
TM-2-51 (25 μM) increases the level of histone H3K27 trimethylation in LeTx-treated human monocytic THP-1 cells[2].
TM-2-51 (10-80 μM; 24-72 h) selectively inhibits the proliferation of human neuroblastoma SH-SY5Y cells: at a concentration of 80 μM for 72 h, the proliferation inhibition rate is approximately 22%, while it exerts no effect on human neuroblastoma BE (2)-C cells[4].
TM-2-51 (80 μM; 48 h) enhances the expression of p53 and p21 proteins in SH-SY5Y human neuroblastoma cells when treated at a concentration of 80 μM for 48 h, but exerts no effect on the expression of p53 and p21 in BE (2)-C human neuroblastoma cells[4].
TM-2-51 (48 h) increases the proportion of U2OS and 143B osteosarcoma cells in the G1 phase of the cell cycle and induces cell cycle arrest[1].
TM-2-51 (25 μM; 48-72 h) inhibits LeTx-induced G0-G1 cell cycle arrest in the human monocytic cell line THP-1, and restores the cell cycle to a near-normal progression at 72 h[2].
TM-2-51 potently inhibits α-glucosidase with an IC50 of 171.21 μM[3].
TM-2-51 exhibits no cytotoxicity against 3T3 mouse fibroblasts[3].
TM-2-51 (2-20 μM) activates purified recombinant human HDAC8 by decreasing the Michaelis constant (Km, from 650 μM to 184 μM) and increasing the catalytic constant (kcat, from 0.0072 s-1 to 0.035 s-1; all these changes are measured at the highest tested concentration of 20 μM)[4].
TM-2-51 activates purified recombinant human HDAC8 with positive cooperativity; at subsaturating substrate concentrations, its apparent activation constant is 6.1 μM and Hill coefficient is 1.7, whereas cooperativity decreases at saturating substrate concentrations[4].
TM-2-51 (up to 1.8 μM) binds to purified recombinant human HDAC8, with an equilibrium dissociation constant of 0.28 μM and a stoichiometric ratio close to 1:1[4].
TM-2-51 binds to two functional sites on purified recombinant human HDAC8, with negative cooperativity during the binding process; it exhibits the strongest binding affinity at the first site, with a binding constant of 2.09 × 106 M-1[4].
TM-2-51 (100 μM) increases the binding affinity of SAHA to purified recombinant human HDAC8 by approximately 2-fold, and alters the enthalpic and entropic contributions to the binding process[4].
TM-2-51 (80 μM; 72 h) induces approximately 45% apoptosis in human neuroblastoma SH-SY5Y cells when treated at 80 μM for 72 h, but exerts no effect on human neuroblastoma BE (2)-C cells[4].
TM-2-51 (10-48 μM; saturating concentration) potently and selectively activates recombinant human HDAC-8, reaching a maximum activation fold of 26.8 at saturating concentrations (apparent Ka = 12.4 μM), with no activating effect on other tested human HDAC isozymes[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human monocytic THP-1 cells
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Concentration:6, 13, 25 and 50 μM
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Incubation Time:24, 48, 72 and 96 h
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Result:Exerted a cytoprotective effect against LeTx-induced cytotoxicity, with significant effects starting at 13 μM and maximal effects at 25 μM.
Allowed continuous increases in live cell numbers over 96 h in cells treated with both LeTx and 25 μM TM-2-51, albeit at a slower rate than non-treated cells.
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Cell Line:human monocytic THP-1 cells
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Concentration:25 μM
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Incubation Time:48 h and 72 h
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Result:Reduced G0-G1 phase distribution to 62.0% at 48 h post-LeTx treatment, compared to 99.5% G0-G1 arrest in LeTx-only cells.
Resulted in near-normal cell cycle distribution (37.6% G0-G1, 8.2% G2-M, 54.2% S phase) at 72 h post-LeTx treatment, compared to LeTx-only cells with 30.8% G0-G1, 1.11% G2-M, and 68.2% S phase.
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Cell Line:human monocytic THP-1 cells
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Concentration:25 μM
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Incubation Time:24 h, 48 h and 72 h
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Result:Enhanced LeTx-induced AKT phosphorylation at Ser-473 significantly at 24 h, 48 h, and 72 h post-LeTx treatment.
Showed the highest AKT phosphorylation at Ser-473 detected at 72 h post-LeTx treatment.
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Cell Line:SH-SY5Y human neuroblastoma cells, BE(2)-C human neuroblastoma cells
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Concentration:0, 10, 40 and 80 μM
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Incubation Time:24 h, 48 h, 72 h
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Result:Induced concentration- and time-dependent growth inhibition in SH-SY5Y cells.
Decreased SH-SY5Y cell proliferation by approximately 22% at 80 μM for 72 hours compared to control.
Exerted no growth inhibition effect on BE(2)-C cells under the same conditions.
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Cell Line:SH-SY5Y human neuroblastoma cells, BE(2)-C human neuroblastoma cells
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Concentration:80 μM
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Incubation Time:72 h
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Result:Induced approximately 45% apoptosis in SH-SY5Y cells compared to DMSO-treated control cells.
Exerted no apoptotic effect on BE(2)-C cells under the same conditions.
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Cell Line:SH-SY5Y human neuroblastoma cells, BE(2)-C human neuroblastoma cells
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Concentration:80 μM
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Incubation Time:48 h
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Result:Moderately enhanced p53 protein expression in SH-SY5Y cells compared to DMSO-treated controls.
Noticeably enhanced p21 protein expression in SH-SY5Y cells compared to DMSO-treated controls.
Exerted no changes in p53 or p21 expression in BE(2)-C cells under the same conditions.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/C nude mice[1]
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Dosage:10 mg/kg
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Administration:i.p.; every 2 days; 14 days
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Result:Reduced tumor weight and tumor volume compared to vehicle control.
Suppressed tumor cell proliferation confirmed by Ki67 staining, with statistically significant differences (***P<0.001).
Chemical Information
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CAS No. 4921-82-8
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Appearance Solid
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Molecular Weight 256.32
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Formula C14H12N2OS
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Color White to off-white
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SMILES
O=C(NC(=S)NC=1C=CC=CC1)C=2C=CC=CC2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (390.14 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (286 KB)
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SDS (762 KB)
- English - EN (762 KB)
- Français - FR (762 KB)
- Deutsch - DE (762 KB)
- Norwegian - NO (762 KB)
- Español - ES (762 KB)
- Swedish - SV (762 KB)
- Italian - IT (762 KB)
- Korean - KR (762 KB)
- Portuguese - PT (762 KB)
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Handling Instructions (2659 KB)
References
[1]. Wang L, et al. Activation of HDAC8 Can Suppress the Proliferation of Osteosarcoma Cells via and STAT3/ERK Signaling Pathways. Annals of clinical and laboratory science. 2023 Nov;53(6):920-930. [Content Brief]
[2]. Ha SD, et al. HDAC8 Prevents Anthrax Lethal Toxin-induced Cell Cycle Arrest through Silencing PTEN in Human Monocytic THP-1 Cells. Toxins. 2017 May 16;9(5):162. [Content Brief]
[3]. Akhter S, et al. Synthesis, crystal structure and Hirshfeld Surface analysis of benzamide derivatives of thiourea as potent inhibitors of α-glucosidase in-vitro. Bioorganic chemistry. 2021 Feb;107:104531. [Content Brief]
[4]. Singh RK, et al. Mechanism of N-Acylthiourea-mediated activation of human histone deacetylase 8 (HDAC8) at molecular and cellular levels. The Journal of biological chemistry. 2015 Mar 06;290(10):6607-19. [Content Brief]
[5]. Singh RK, et al. Histone deacetylase activators: N-acetylthioureas serve as highly potent and isozyme selective activators for human histone deacetylase-8 on a fluorescent substrate. Bioorganic & medicinal chemistry letters. 2011 Oct 01;21(19):5920-3. [Content Brief]
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 | 3.9014 mL | 19.5069 mL | 39.0137 mL | 97.5343 mL |
| 5 mM | 0.7803 mL | 3.9014 mL | 7.8027 mL | 19.5069 mL | |
| 10 mM | 0.3901 mL | 1.9507 mL | 3.9014 mL | 9.7534 mL | |
| 15 mM | 0.2601 mL | 1.3005 mL | 2.6009 mL | 6.5023 mL | |
| 20 mM | 0.1951 mL | 0.9753 mL | 1.9507 mL | 4.8767 mL | |
| 25 mM | 0.1561 mL | 0.7803 mL | 1.5605 mL | 3.9014 mL | |
| 30 mM | 0.1300 mL | 0.6502 mL | 1.3005 mL | 3.2511 mL | |
| 40 mM | 0.0975 mL | 0.4877 mL | 0.9753 mL | 2.4384 mL | |
| 50 mM | 0.0780 mL | 0.3901 mL | 0.7803 mL | 1.9507 mL | |
| 60 mM | 0.0650 mL | 0.3251 mL | 0.6502 mL | 1.6256 mL | |
| 80 mM | 0.0488 mL | 0.2438 mL | 0.4877 mL | 1.2192 mL | |
| 100 mM | 0.0390 mL | 0.1951 mL | 0.3901 mL | 0.9753 mL |
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