For research use only. Not for therapeutic Use.
CI-994（Cat No.:I000472）, also known as BMS-181,101, is a histone deacetylase (HDAC) inhibitor that selectively targets class I and II HDACs. By inhibiting these enzymes, CI-994 promotes histone acetylation, leading to the activation of tumor suppressor genes and the repression of oncogenes, which can trigger cancer cell apoptosis. It has shown potential in treating various cancers, including leukemia and solid tumors, often in combination with other therapies. Additionally, CI-994 has been studied for its neuroprotective effects, suggesting a broader therapeutic potential beyond oncology.
| Catalog Number | I000472 |
| CAS Number | 112522-64-2 |
| Synonyms | 4-acetamido-N-(2-aminophenyl)benzamide |
| Molecular Formula | C₁₅H₁₅N₃O₂ |
| Purity | ≥95% |
| Target | HDAC |
| Solubility | DMSO: ≥ 58 mg/mL |
| Storage | 3 years -20C powder |
| IC50 | 0.57 uM (For HDAC1,MTT assay) |
| IUPAC Name | 4-acetamido-N-(2-aminophenyl)benzamide |
| InChI | InChI=1S/C15H15N3O2/c1-10(19)17-12-8-6-11(7-9-12)15(20)18-14-5-3-2-4-13(14)16/h2-9H,16H2,1H3,(H,17,19)(H,18,20) |
| InChIKey | VAZAPHZUAVEOMC-UHFFFAOYSA-N |
| SMILES | CC(=O)NC1=CC=C(C=C1)C(=O)NC2=CC=CC=C2N |
| Reference | </br>1:Class I HDAC imaging using [ (3)H]CI-994 autoradiography. Wang Y, Zhang YL, Hennig K, Gale JP, Hong Y, Cha A, Riley M, Wagner F, Haggarty SJ, Holson E, Hooker J.Epigenetics. 2013 Jul;8(7):756-64. doi: 10.4161/epi.25202. Epub 2013 Jun 11. PMID: 23803584 Free PMC Article</br>2:Synthesis and biological evaluation of glucuronide prodrugs of the histone deacetylase inhibitor CI-994 for application in selective cancer chemotherapy. Thomas M, Clarhaut J, Tranoy-Opalinski I, Gesson JP, Roche J, Papot S.Bioorg Med Chem. 2008 Sep 1;16(17):8109-16. doi: 10.1016/j.bmc.2008.07.048. Epub 2008 Jul 23. PMID: 18692397 </br>3:CI-994 (N-acetyl-dinaline) in combination with conventional anti-cancer agents is effective against acute myeloid leukemia in vitro and in vivo. Hubeek I, Comijn EM, Van der Wilt CL, Merriman RL, Padron JM, Kaspers GJ, Peters GJ.Oncol Rep. 2008 Jun;19(6):1517-23. PMID: 18497959 </br>4:Improved synthesis of histone deacetylase inhibitors (HDIs) (MS-275 and CI-994) and inhibitory effects of HDIs alone or in combination with RAMBAs or retinoids on growth of human LNCaP prostate cancer cells and tumor xenografts. Gediya LK, Belosay A, Khandelwal A, Purushottamachar P, Njar VC.Bioorg Med Chem. 2008 Mar 15;16(6):3352-60. doi: 10.1016/j.bmc.2007.12.007. Epub 2007 Dec 8. PMID: 18166465 Free PMC Article</br>5:Gemcitabine plus CI-994 offers no advantage over gemcitabine alone in the treatment of patients with advanced pancreatic cancer: results of a phase II randomized, double-blind, placebo-controlled, multicenter study. Richards DA, Boehm KA, Waterhouse DM, Wagener DJ, Krishnamurthi SS, Rosemurgy A, Grove W, Macdonald K, Gulyas S, Clark M, Dasse KD.Ann Oncol. 2006 Jul;17(7):1096-102. Epub 2006 Apr 26. PMID: 16641168 </br>6:In vitro study of CI-994, a histone deacetylase inhibitor, in non-small cell lung cancer cell lines. Loprevite M, Tiseo M, Grossi F, Scolaro T, Semino C, Pandolfi A, Favoni R, Ardizzoni A.Oncol Res. 2005;15(1):39-48. PMID: 15839304 </br>7:Phase I study of oral CI-994 in combination with carboplatin and paclitaxel in the treatment of patients with advanced solid tumors. Pauer LR, Olivares J, Cunningham C, Williams A, Grove W, Kraker A, Olson S, Nemunaitis J.Cancer Invest. 2004;22(6):886-96. PMID: 15641487 </br>8:A phase I study of the oral combination of CI-994, a putative histone deacetylase inhibitor, and capecitabine. Undevia SD, Kindler HL, Janisch L, Olson SC, Schilsky RL, Vogelzang NJ, Kimmel KA, Macek TA, Ratain MJ.Ann Oncol. 2004 Nov;15(11):1705-11. PMID: 15520075 </br>9:Phase I study of oral CI-994 in combination with gemcitabine in treatment of patients with advanced cancer. Nemunaitis JJ, Orr D, Eager R, Cunningham CC, Williams A, Mennel R, Grove W, Olson S.Cancer J. 2003 Jan-Feb;9(1):58-66. PMID: 12602769 </br>10:Induction of Apoptosis in Rat Peripheral Blood Lymphocytes by the Anticancer Drug CI-994 (Acetyldinaline)(*). Graziano MJ, Spoon TA, Cockrell EA, Rowse PE, Gonzales AJ.J Biomed Biotechnol. 2001;1(2):52-61. PMID: 12488610 Free PMC Article |
