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MedKoo Cat#: 122626 | Name: SGC-CBP30 HCl
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

SGC-CBP30 is a potent and selective inhibitor of CREBBP (CBP) and EP300; which are general transcriptional co-activators. CREBBP has also been associated with amyotrophic lateral sclerosis (ALS) or Lou Gehrig’s disease, a neurodegenerative disease with progressive degeneration of motor neurons in the brain and spinal cord, Alzheimer's disease and poly glutamine repeat diseases such as Spinal and Bulbar Muscular Atrophy and Huntington’s disease.

Chemical Structure

SGC-CBP30 HCl
SGC-CBP30 HCl
CAS#SGC-CBP30 HCl

Theoretical Analysis

MedKoo Cat#: 122626

Name: SGC-CBP30 HCl

CAS#: SGC-CBP30 HCl

Chemical Formula: C28H33ClN4O3

Exact Mass: 508.2200

Molecular Weight: 509.05

Elemental Analysis: C, 66.07; H, 6.53; Cl, 6.96; N, 11.01; O, 9.43

Price and Availability

Size Price Availability Quantity
5mg USD 450.00 2 Weeks
10mg USD 700.00 2 Weeks
50mg USD 1,550.00 2 Weeks
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Related CAS #
1613695-14-9 (free base) SGC-CBP30 HCl
Synonym
SGC-CBP30 HCl; SCG-CBP30; SCG CBP30; SCGCBP30
IUPAC/Chemical Name
(S)-4-(1-(2-(3-chloro-4-methoxyphenethyl)-5-(3,5-dimethylisoxazol-4-yl)-1H-benzo[d]imidazol-1-yl)propan-2-yl)morpholine
InChi Key
GEPYBHCJBORHCE-SFHVURJKSA-N
InChi Code
InChI=1S/C28H33ClN4O3/c1-18(32-11-13-35-14-12-32)17-33-25-8-7-22(28-19(2)31-36-20(28)3)16-24(25)30-27(33)10-6-21-5-9-26(34-4)23(29)15-21/h5,7-9,15-16,18H,6,10-14,17H2,1-4H3/t18-/m0/s1
SMILES Code
CC1=C(C2=CC(N=C(CCC3=CC=C(OC)C(Cl)=C3)N4C[C@H](C)N5CCOCC5)=C4C=C2)C(C)=NO1
Appearance
To be determined
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 509.05 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
1: Wang X, Chen X, Chen Z, Xu W, Lai R, Qiu X, Zeng Z, Wang C, Wang Z, Wang J. Integrated Anchored Stapling and Hierarchical Dynamics: MSICDA-Driven CREBBP Bromodomain Inhibition. J Chem Inf Model. 2024 Jun 24;64(12):4739-4758. doi: 10.1021/acs.jcim.4c00381. Epub 2024 Jun 11. PMID: 38863138. 2: Wen L, Xie B, Li H, Huang J, Shi Y, Tao Y, Chen Y. EP300 through upregulating the expression of vimentin to promote the progression of chordoma. Neurosurg Focus. 2024 May;56(5):E17. doi: 10.3171/2024.2.FOCUS244. PMID: 38691868. 3: Russell CN, Carter JL, Borgia JM, Bush J, Calderón F, Gabarró R, Conway SJ, Mottram JC, Wilkinson AJ, Jones NG. Bromodomain Factor 5 as a Target for Antileishmanial Drug Discovery. ACS Infect Dis. 2023 Nov 10;9(11):2340-2357. doi: 10.1021/acsinfecdis.3c00431. Epub 2023 Oct 31. PMID: 37906637; PMCID: PMC10644352. 4: Zhang Z, Zhu Y. ANRGs impact on gastric cancer progression and drug efficacy: A comprehensive study. Medicine (Baltimore). 2023 Oct 27;102(43):e34861. doi: 10.1097/MD.0000000000034861. PMID: 37904473; PMCID: PMC10615463. 5: Yin J, Zhao Z, Huang J, Xiao Y, Rehmutulla M, Zhang B, Zhang Z, Xiang M, Tong Q, Zhang Y. Single-cell transcriptomics reveals intestinal cell heterogeneity and identifies Ep300 as a potential therapeutic target in mice with acute liver failure. Cell Discov. 2023 Jul 25;9(1):77. doi: 10.1038/s41421-023-00578-4. PMID: 37488127; PMCID: PMC10366100. 6: Wang X, Wang Z, Huang R, Lu Z, Chen X, Huang D. UPP1 Promotes Lung Adenocarcinoma Progression through Epigenetic Regulation of Glycolysis. Aging Dis. 2022 Oct 1;13(5):1488-1503. doi: 10.14336/AD.2022.0218. PMID: 36186123; PMCID: PMC9466982. 7: Barghout SH, Mann MK, Aman A, Yu Y, Alteen MG, Schimmer AD, Schapira M, Arrowsmith CH, Barsyte-Lovejoy D. Combinatorial Anticancer Drug Screen Identifies Off-Target Effects of Epigenetic Chemical Probes. ACS Chem Biol. 2022 Oct 21;17(10):2801-2816. doi: 10.1021/acschembio.2c00451. Epub 2022 Sep 9. PMID: 36084291. 8: Principe DR, Xiong R, Li Y, Pham TND, Kamath SD, Dubrovskyi O, Ratia K, Huang F, Zhao J, Shen Z, Thummuri D, Daohong Z, Underwood PW, Trevino J, Munshi HG, Thatcher GRJ, Rana A. XP-524 is a dual-BET/EP300 inhibitor that represses oncogenic KRAS and potentiates immune checkpoint inhibition in pancreatic cancer. Proc Natl Acad Sci U S A. 2022 Jan 25;119(4):e2116764119. doi: 10.1073/pnas.2116764119. PMID: 35064087; PMCID: PMC8795568. 9: Navarro-Corcuera A, Sehrawat TS, Jalan-Sakrikar N, Gibbons HR, Pirius NE, Khanal S, Hamdan FH, Aseem SO, Cao S, Banales JM, Kang N, Faubion WA, LaRusso NF, Shah VH, Huebert RC. Long non-coding RNA ACTA2-AS1 promotes ductular reaction by interacting with the p300/ELK1 complex. J Hepatol. 2022 Apr;76(4):921-933. doi: 10.1016/j.jhep.2021.12.014. Epub 2021 Dec 23. PMID: 34953958; PMCID: PMC8934273. 10: Hlushchuk I, Ruskoaho H, Domanskyi A, Airavaara M, Välimäki MJ. Domain- Independent Inhibition of CBP/p300 Attenuates α-Synuclein Aggregation. ACS Chem Neurosci. 2021 Jul 7;12(13):2273-2279. doi: 10.1021/acschemneuro.1c00215. Epub 2021 Jun 10. PMID: 34110772; PMCID: PMC8291498. 11: Noguchi T, Hidaka K, Kobayashi S, Matsumoto K, Yoshioka M, Hu X, Maloney DJ, Yang SM, Kato S. A quinazoline-based bromodomain inhibitor, CN210, ameliorates indomethacin-induced ileitis in mice by inhibiting inflammatory cytokine expression. Drug Dev Res. 2021 Dec;82(8):1235-1246. doi: 10.1002/ddr.21838. Epub 2021 Jun 1. PMID: 34075610; PMCID: PMC8637501. 12: Bi X, Jiang B, Zhou J, Fan X, Yan X, Liang J, Luo L, Yin Z. CBP Bromodomain Inhibition Rescues Mice From Lethal Sepsis Through Blocking HMGB1-Mediated Inflammatory Responses. Front Immunol. 2021 Feb 2;11:625542. doi: 10.3389/fimmu.2020.625542. PMID: 33603756; PMCID: PMC7884462. 13: Rao X, Tang P, Li Y, Fu G, Chen S, Xu X, Zhou Y, Li X, Zhang L, Mo S, Cai S, Peng J, Zhang Z, Gao J, Hua G. CBP/P300 Inhibitors Mitigate Radiation-Induced GI Syndrome by Promoting Intestinal Stem Cell-Mediated Crypt Regeneration. Int J Radiat Oncol Biol Phys. 2021 Jul 15;110(4):1210-1221. doi: 10.1016/j.ijrobp.2021.01.046. Epub 2021 Feb 3. PMID: 33545304. 14: Williams LM, McCann FE, Cabrita MA, Layton T, Cribbs A, Knezevic B, Fang H, Knight J, Zhang M, Fischer R, Bonham S, Steenbeek LM, Yang N, Sood M, Bainbridge C, Warwick D, Harry L, Davidson D, Xie W, Sundstrӧm M, Feldmann M, Nanchahal J. Identifying collagen VI as a target of fibrotic diseases regulated by CREBBP/EP300. Proc Natl Acad Sci U S A. 2020 Aug 25;117(34):20753-20763. doi: 10.1073/pnas.2004281117. Epub 2020 Aug 5. PMID: 32759223; PMCID: PMC7456151. 15: Sun J, Zhang W, Tan Z, Zheng C, Tang Y, Ke X, Zhang Y, Liu Y, Li P, Hu Q, Wang H, Mao P, Zheng Z. Zika virus promotes CCN1 expression via the CaMKIIα-CREB pathway in astrocytes. Virulence. 2020 Dec;11(1):113-131. doi: 10.1080/21505594.2020.1715189. PMID: 31957543; PMCID: PMC6984649. 16: Zhu YX, Shi CX, Bruins LA, Wang X, Riggs DL, Porter B, Ahmann JM, de Campos CB, Braggio E, Bergsagel PL, Stewart AK. Identification of lenalidomide resistance pathways in myeloma and targeted resensitization using cereblon replacement, inhibition of STAT3 or targeting of IRF4. Blood Cancer J. 2019 Feb 11;9(2):19. doi: 10.1038/s41408-019-0173-0. PMID: 30741931; PMCID: PMC6370766. 17: Zhou W, Jiang D, Tian J, Liu L, Lu T, Huang X, Sun H. Acetylation of H3K4, H3K9, and H3K27 mediated by p300 regulates the expression of GATA4 in cardiocytes. Genes Dis. 2018 Oct 15;6(3):318-325. doi: 10.1016/j.gendis.2018.10.002. PMID: 32042871; PMCID: PMC6997570. 18: Tao J, Zhang M, Wen Z, Wang B, Zhang L, Ou Y, Tang X, Yu X, Jiang Q. Inhibition of EP300 and DDR1 synergistically alleviates pulmonary fibrosis in vitro and in vivo. Biomed Pharmacother. 2018 Oct;106:1727-1733. doi: 10.1016/j.biopha.2018.07.132. Epub 2018 Jul 30. PMID: 30119248. 19: Chua MJ, Robaa D, Skinner-Adams TS, Sippl W, Andrews KT. Activity of bromodomain protein inhibitors/binders against asexual-stage Plasmodium falciparum parasites. Int J Parasitol Drugs Drug Resist. 2018 Aug;8(2):189-193. doi: 10.1016/j.ijpddr.2018.03.001. Epub 2018 Mar 26. PMID: 29631126; PMCID: PMC6039313. 20: Xiang Q, Wang C, Zhang Y, Xue X, Song M, Zhang C, Li C, Wu C, Li K, Hui X, Zhou Y, Smaill JB, Patterson AV, Wu D, Ding K, Xu Y. Discovery and optimization of 1-(1H-indol-1-yl)ethanone derivatives as CBP/EP300 bromodomain inhibitors for the treatment of castration-resistant prostate cancer. Eur J Med Chem. 2018 Mar 10;147:238-252. doi: 10.1016/j.ejmech.2018.01.087. Epub 2018 Feb 6. PMID: 29448139.