ICBP112

• CAT Number: I029063
• CAS Number: 1640282-31-0
• Molecular Formula: C27H36N2O5
• Molecular Weight: 468.59
• Purity: 98%
• Synonyms: ICBP112; ICBP 112; ICBP-112
• Solubility: To be determined
• Appearance: Solid powder
• Storage: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
• IUPAC Name: 1-[7-(3,4-dimethoxyphenyl)-9-[[(3S)-1-methylpiperidin-3-yl]methoxy]-3,5-dihydro-2H-1,4-benzoxazepin-4-yl]propan-1-one
• InChI: InChI=1S/C27H36N2O5/c1-5-26(30)29-11-12-33-27-22(17-29)13-21(20-8-9-23(31-3)24(14-20)32-4)15-25(27)34-18-19-7-6-10-28(2)16-19/h8-9,13-15,19H,5-7,10-12,16-18H2,1-4H3/t19-/m0/s1
• InChIKey: YKNAKDFZAWQEEO-IBGZPJMESA-N
• SMILES: CCC(=O)N1CCOC2=C(C1)C=C(C=C2OC[C@H]3CCCN(C3)C)C4=CC(=C(C=C4)OC)OC

ICBP112（Cat No.:I029063）is an investigational small molecule compound that functions as an inhibitor of the protein phosphatase 2A (PP2A), a serine/threonine phosphatase involved in regulating key cellular processes like cell growth, differentiation, and apoptosis. By selectively inhibiting PP2A, ICBP112 alters signaling pathways, potentially enhancing the immune response and modulating the tumor microenvironment. This makes it a promising candidate for cancer immunotherapy, particularly in overcoming resistance mechanisms that limit the effectiveness of traditional therapies. Preclinical studies suggest that ICBP112 could be effective in treating various cancers, though its safety and efficacy are still under investigation in clinical trials.

Reference

1: Yuan YG, Wang JL, Mesalam A, Li L, Choi YJ, Talimur Reza AMM, Zhou D, Chen L, Qian C. Nicotinamide-induced mouse embryo developmental defect rescued by resveratrol and I-CBP112. Mol Reprod Dev. 2020 Sep;87(9):1009-1017. doi: 10.1002/mrd.23405. Epub 2020 Aug 20. PMID: 32818292.
2: Yuan YG, Xu L, Zhang S, Mesalam A, Lee KL, Liu H, Joo MD, Idrees M, Kong IK. Polydatin and I-CBP112 protects early bovine embryo against nicotinamide-induced mitochondrial dysfunction. Theriogenology. 2019 Aug;134:1-10. doi: 10.1016/j.theriogenology.2019.05.007. Epub 2019 May 9. PMID: 31108431.
3: Zucconi BE, Makofske JL, Meyers DJ, Hwang Y, Wu M, Kuroda MI, Cole PA. Combination Targeting of the Bromodomain and Acetyltransferase Active Site of p300/CBP. Biochemistry. 2019 Apr 23;58(16):2133-2143. doi: 10.1021/acs.biochem.9b00160. Epub 2019 Apr 11. PMID: 30924641; PMCID: PMC6948846.
4: Dhaliwal A, Pelka S, Gray DS, Moghe PV. Engineering Lineage Potency and Plasticity of Stem Cells using Epigenetic Molecules. Sci Rep. 2018 Nov 2;8(1):16289. doi: 10.1038/s41598-018-34511-7. PMID: 30389989; PMCID: PMC6215020.
5: Popp TA, Tallant C, Rogers C, Fedorov O, Brennan PE, Müller S, Knapp S, Bracher F. Development of Selective CBP/P300 Benzoxazepine Bromodomain Inhibitors. J Med Chem. 2016 Oct 13;59(19):8889-8912. doi: 10.1021/acs.jmedchem.6b00774. Epub 2016 Sep 27. PMID: 27673482.
6: Zucconi BE, Luef B, Xu W, Henry RA, Nodelman IM, Bowman GD, Andrews AJ, Cole PA. Modulation of p300/CBP Acetylation of Nucleosomes by Bromodomain Ligand I-CBP112. Biochemistry. 2016 Jul 12;55(27):3727-34. doi: 10.1021/acs.biochem.6b00480. Epub 2016 Jul 1. PMID: 27332697; PMCID: PMC5007619.
7: Picaud S, Fedorov O, Thanasopoulou A, Leonards K, Jones K, Meier J, Olzscha H, Monteiro O, Martin S, Philpott M, Tumber A, Filippakopoulos P, Yapp C, Wells C, Che KH, Bannister A, Robson S, Kumar U, Parr N, Lee K, Lugo D, Jeffrey P, Taylor S, Vecellio ML, Bountra C, Brennan PE, O’Mahony A, Velichko S, Müller S, Hay D, Daniels DL, Urh M, La Thangue NB, Kouzarides T, Prinjha R, Schwaller J, Knapp S. Generation of a Selective Small Molecule Inhibitor of the CBP/p300 Bromodomain for Leukemia Therapy. Cancer Res. 2015 Dec 1;75(23):5106-5119. doi: 10.1158/0008-5472.CAN-15-0236. Epub 2015 Nov 9. PMID: 26552700; PMCID: PMC4948672.