For research use only. Not for therapeutic Use.
Chidamide (Cat No.:I004761) is a small molecule histone deacetylase inhibitor (HDACi) that has been approved for the treatment of certain lymphomas in China. As an HDACi, Chidamide acts by inhibiting the activity of histone deacetylases, which are enzymes responsible for removing acetyl groups from histone proteins. By inhibiting HDACs, Chidamide promotes histone acetylation, leading to alterations in chromatin structure and gene expression. This can result in various biological effects, including the inhibition of tumor cell growth, induction of cell cycle arrest, and promotion of apoptosis. Chidamide’s approval and use in the treatment of lymphomas highlight its potential as an anticancer agent targeting epigenetic modifications.
| Catalog Number | I004761 |
| CAS Number | 743420-02-2 |
| Synonyms | (1Z,2E)-N-(4-((2-amino-5-fluorophenyl)carbamoyl)benzyl)-3-(pyridin-3-yl)acrylimidic acid |
| Molecular Formula | C₂₂H₁₉FN₄O₂ |
| Purity | ≥95% |
| Target | HDAC |
| Solubility | DMSO: ≥ 41 mg/mL |
| Storage | Store at -20°C |
| IC50 | 95/160/67/733 nM(HDAC1/2/3/8) |
| IUPAC Name | N-(2-amino-5-fluorophenyl)-4-[[[(E)-3-pyridin-3-ylprop-2-enoyl]amino]methyl]benzamide |
| InChI | InChI=1S/C22H19FN4O2/c23-18-8-9-19(24)20(12-18)27-22(29)17-6-3-16(4-7-17)14-26-21(28)10-5-15-2-1-11-25-13-15/h1-13H,14,24H2,(H,26,28)(H,27,29)/b10-5+ |
| InChIKey | WXHHICFWKXDFOW-BJMVGYQFSA-N |
| SMILES | C1=CC(=CN=C1)/C=C/C(=O)NCC2=CC=C(C=C2)C(=O)NC3=C(C=CC(=C3)F)N |
| Reference | </br>1:Chidamide tablets: HDAC inhibition to treat lymphoma. Xu Y, Zhang P, Liu Y.Drugs Today (Barc). 2017 Mar;53(3):167-176. doi: 10.1358/dot.2017.53.3.2595452. PMID: 28447074 </br>2:Chidamide in FLT3-ITD positive acute myeloid leukemia and the synergistic effect in combination with cytarabine. Li X, Yan X, Guo W, Huang X, Huang J, Yu M, Ma Z, Xu Y, Huang S, Li C, Zhou Y, Jin J.Biomed Pharmacother. 2017 Jun;90:699-704. doi: 10.1016/j.biopha.2017.04.037. Epub 2017 Apr 15. PMID: 28419965 </br>3:Chidamide in relapsed or refractory peripheral T cell lymphoma: a multicenter real-world study in China. Shi Y, Jia B, Xu W, Li W, Liu T, Liu P, Zhao W, Zhang H, Sun X, Yang H, Zhang X, Jin J, Jin Z, Li Z, Qiu L, Dong M, Huang X, Luo Y, Wang X, Wang X, Wu J, Xu J, Yi P, Zhou J, He H, Liu L, Shen J, Tang X, Wang J, Yang J, Zeng Q, Zhang Z, Cai Z, Chen X, Ding K, Hou M, Huang H, Li X, Liang R, Liu Q, Song Y, Su H, Gao Y, Liu L, Luo J, Su L, Sun Z, Tan H, Wang H, Wang J, Wang S, Zhang H, Zhang X, Zhou D, Bai O, Wu G, Zhang L, Zhang Y.J Hematol Oncol. 2017 Mar 15;10(1):69. doi: 10.1186/s13045-017-0439-6. PMID: 28298231 Free PMC Article</br>4:Chidamide in the treatment of peripheral T-cell lymphoma. Chan TS, Tse E, Kwong YL.Onco Targets Ther. 2017 Jan 12;10:347-352. doi: 10.2147/OTT.S93528. eCollection 2017. Review. PMID: 28138258 Free PMC Article</br>5:Chidamide Inhibits Aerobic Metabolism to Induce Pancreatic Cancer Cell Growth Arrest by Promoting Mcl-1 Degradation. He M, Qiao Z, Wang Y, Kuai Q, Li C, Wang Y, Jiang X, Wang X, Li W, He M, Ren S, Yu Q.PLoS One. 2016 Nov 22;11(11):e0166896. doi: 10.1371/journal.pone.0166896. eCollection 2016. PMID: 27875574 Free PMC Article</br>6:A novel histone deacetylase inhibitor Chidamide induces G0/G1 arrest and apoptosis in myelodysplastic syndromes. Liu Z, Ding K, Li L, Liu H, Wang Y, Liu C, Fu R.Biomed Pharmacother. 2016 Oct;83:1032-1037. doi: 10.1016/j.biopha.2016.08.023. Epub 2016 Aug 16. PMID: 27541047 </br>7:Development of chidamide for peripheral T-cell lymphoma, the first orphan drug approved in China. Lu X, Ning Z, Li Z, Cao H, Wang X.Intractable Rare Dis Res. 2016 Aug;5(3):185-91. doi: 10.5582/irdr.2016.01024. Review. PMID: 27672541 Free PMC Article</br>8:A phase I trial of an oral subtype-selective histone deacetylase inhibitor, chidamide, in combination with paclitaxel and carboplatin in patients with advanced non-small cell lung cancer. Hu X, Wang L, Lin L, Han X, Dou G, Meng Z, Shi Y.Chin J Cancer Res. 2016 Aug;28(4):444-51. doi: 10.21147/j.issn.1000-9604.2016.04.08. PMID: 27647973 Free PMC Article</br>9:Preclinical and clinical studies of chidamide (CS055/HBI-8000), an orally available subtype-selective HDAC inhibitor for cancer therapy. Gao S, Li X, Zang J, Xu W, Zhang Y.Anticancer Agents Med Chem. 2016 Sep 1. [Epub ahead of print] PMID: 27592546 </br>10:Chidamide, a novel histone deacetylase inhibitor, inhibits the viability of MDS and AML cells by suppressing JAK2/STAT3 signaling. Zhao S, Guo J, Zhao Y, Fei C, Zheng Q, Li X, Chang C.Am J Transl Res. 2016 Jul 15;8(7):3169-78. eCollection 2016. PMID: 27508038 Free PMC Article |
