CCS1477 MedChemExpress (MCE)

Product Name	(S)-1-(3,4-difluorophenyl)-6-(5-(3,5-dimethylisoxazol-4-yl)-1-((1r,4S)-4-methoxycyclohexyl)-1H-benzo[d]imidazol-2-yl)piperidin-2-one
Synonyms	CCS147 CCS1477 CBP-IN-1 CCS-1477 Inobrodib CBP inhibitor 1 CBP-IN-1 (CCS1477) Synonyms CCS147 CCS1477 CBP-IN-1 CCS-1477 Inobrodib CBP inhibitor 1 CBP-IN-1 (CCS1477) CCS-1477(CBP-IN-1) 2-Piperidinone, 1-(3,4-difluorophenyl)-6-[5-(3,5-dimethyl-4-isoxazolyl)-1-(trans-4-methoxycyclohexyl)-1H-benzimidazol-2-yl]-, (6S)- (S)-1-(3,4-difluorophenyl)-6-(5-(3,5-dimethylisoxazol-4-yl)-1-((1r,4S)-4-methoxycyclohexyl)-1H-benzo[d]imidazol-2-yl)piperidin-2-one
CAS	2222941-37-7
EINECS
Chemical Formula	C30H32F2N4O3
Molecular Weight	534.6
inchi
Package	10 mM * 1 mL;1 mg;5 mg;10 mg
Price	Get quote
Descriptions	Inobrodib Inobrodib MedChemExpress (MCE) HY-111784 2222941-37-7 CCS1477 99.94% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US Descriptions Inobrodib Inobrodib MedChemExpress (MCE) HY-111784 2222941-37-7 CCS1477 99.94% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US may vary elsewhere. Inobrodib (CCS1477) is an orally active, potent, and selective inhibitor of the p300/CBP bromodomain. Inobrodib binds to p300 and CBP with Kd values of 1.3 and 1.7 nM, respectively, and with 170/130-fold selectivity compared with BRD4 with a Kd of 222 nM. CCS1477 inhibits cell proliferation in prostate cancer cell lines and decreases androgen receptor (AR)- and C-MYC-regulated gene expression. Inobrodib binding to cellular histones in an in-cell BRET assay gives an IC50 of 19 nM for p300 and 1060 nM for BRD4. Inobrodib shows potent growth-inhibitory activity in VCaP, 22Rv1, and LNCaP95 (all IC50 [1].?Inobrodib (0-3000 nM 48 hours) reduces expression of AR-regulated genes (KLK2, KLK3, and TMPRSS2) in both 22Rv1 and LNCaP95 cells. Inobrodib also reduces C-MYC protein expression in both 22Rv1 and LNCaP95 cells and AR-V7 protein expression in 22Rv1 cells, without clear impact on AR-FL protein expression in 22Rv1 and LNCaP95 cells. Inobrodib reduces C-MYC mRNA and downstream AR and C-MYC signaling in 22Rv1 and C4-2 cells at 16 hours. Inobrodib regulates AR signaling by affecting the recruitment of CBP, p300, and AR-FL to known AR binding sites, and has the potential to abrogate persistent AR signaling in CRPC[1]. Inobrodib (10-30 mg/kg oral gavage 10 or 20 mg/kg daily (QD) or 30 mg/kg every other day (QOD) for 28 days) suppresses growth of a 22Rv1 mouse xenograft model with associated reduction in AR signaling[1].?Inobrodib (20 mg/kg oral gavage daily for 8 days) decreases AR and AR-V7 signaling and inhibits growth in a patient- derived model of lethal prostate cancer (NOD/SCID gamma (NSG) male castrated mice)[1]. p300/CBP[1] Cellular Effect Cell Line Type Value Description References \| \| \| \| \| \| \| \| \| \| [1]. Rasool RU, et al. Toppling the HAT to Treat Lethal Prostate Cancer. Cancer Discov. 2021 11(5):1011-1013. [Content Brief]
Last Update	2025-04-01 14:45:47

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