4921-82-8
Chemical Structure
TM-2-51
- CAS. Nr.: 4921-82-8
- Formula:C14H12N2OS
- Molecular Weight:256.32
IUPAC Name: N-(phenylcarbamothioyl)benzamide
InChIKey: GVHZQIIMGRLFMX-UHFFFAOYSA-N
SMILES: O=C(NC(=S)NC=1C=CC=CC1)C=2C=CC=CC2
Biological Activity: 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[1][2][3][4][5].
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TM-2-51 | 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. | |||||||||||||||||||||
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- [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]
Keywords