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MedKoo Cat#: 562697 | Name: SGC OF-1
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Description:

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

SGC OF-1, also known as just OF-1, is a selective inhibitor of the bromodomains of the proteins BRPF family (BRPF1/2/3).

Chemical Structure

SGC OF-1
SGC OF-1
CAS#919973-83-4

Theoretical Analysis

MedKoo Cat#: 562697

Name: SGC OF-1

CAS#: 919973-83-4

Chemical Formula: C17H18BrN3O4S

Exact Mass: 439.0201

Molecular Weight: 440.31

Elemental Analysis: C, 46.37; H, 4.12; Br, 18.15; N, 9.54; O, 14.53; S, 7.28

Price and Availability

Size Price Availability Quantity
5mg USD 350.00
10mg USD 600.00
25mg USD 950.00
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Synonym
SGC OF-1; SGC OF 1; SGC OF1; SGCOF1; SGC-OF-1; OF-1; OF 1, OF1
IUPAC/Chemical Name
4-Bromo-N-(6-methoxy-1,3-dimethyl-2-oxo-2,3-dihydro-1H-benzoimidazol-5-yl)-2-methyl-benzenesulfonamide
InChi Key
YUNQZQREIHWDQT-UHFFFAOYSA-N
InChi Code
InChI=1S/C17H18BrN3O4S/c1-10-7-11(18)5-6-16(10)26(23,24)19-12-8-13-14(9-15(12)25-4)21(3)17(22)20(13)2/h5-9,19H,1-4H3
SMILES Code
O=S(C1=CC=C(Br)C=C1C)(NC2=C(OC)C=C(N3C)C(N(C)C3=O)=C2)=O
Appearance
Solid powder
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
Soluble in DMSO and DMF
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
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
Product Data
Product Data
Instruction
View handling instruction
Biological target:
SGC OF-1 is a potent pan-BRPF BRD inhibitor, with IC50 values of 270 nM and 1.2 μM for TRIM24 and BRPF1B, respectively.
In vitro activity:
The BRPF inhibitors investigated, one being SGC OF-1, displaced BRPF BRDs from chromatin and did not inhibit cell growth and proliferation. The inhibitors impaired RANKL-induced differentiation of primary murine bone marrow cells and human primary monocytes into bone resorbing osteoclasts by specifically repressing transcriptional programs required for osteoclastogenesis. Reference: ACS Chem Biol. 2017 Oct 20;12(10):2619-2630. https://pubmed.ncbi.nlm.nih.gov/28849908/
In vivo activity:
To be determined
Solvent mg/mL mM comments
Solubility
DMF 5.0 11.36
DMSO 1.0 2.27
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 440.31 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
Formulation protocol:
1. Meier JC, Tallant C, Fedorov O, Witwicka H, Hwang SY, van Stiphout RG, Lambert JP, Rogers C, Yapp C, Gerstenberger BS, Fedele V, Savitsky P, Heidenreich D, Daniels DL, Owen DR, Fish PV, Igoe NM, Bayle ED, Haendler B, Oppermann UCT, Buffa F, Brennan PE, Müller S, Gingras AC, Odgren PR, Birnbaum MJ, Knapp S. Selective Targeting of Bromodomains of the Bromodomain-PHD Fingers Family Impairs Osteoclast Differentiation. ACS Chem Biol. 2017 Oct 20;12(10):2619-2630. doi: 10.1021/acschembio.7b00481. Epub 2017 Sep 12. PMID: 28849908; PMCID: PMC5662925.
In vitro protocol:
1. Meier JC, Tallant C, Fedorov O, Witwicka H, Hwang SY, van Stiphout RG, Lambert JP, Rogers C, Yapp C, Gerstenberger BS, Fedele V, Savitsky P, Heidenreich D, Daniels DL, Owen DR, Fish PV, Igoe NM, Bayle ED, Haendler B, Oppermann UCT, Buffa F, Brennan PE, Müller S, Gingras AC, Odgren PR, Birnbaum MJ, Knapp S. Selective Targeting of Bromodomains of the Bromodomain-PHD Fingers Family Impairs Osteoclast Differentiation. ACS Chem Biol. 2017 Oct 20;12(10):2619-2630. doi: 10.1021/acschembio.7b00481. Epub 2017 Sep 12. PMID: 28849908; PMCID: PMC5662925.
In vivo protocol:
To be determined
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Formation of Nitric Oxide by Aldehyde Dehydrogenase-2 Is Necessary and Sufficient for Vascular Bioactivation of Nitroglycerin. J Biol Chem. 2016 Nov 11;291(46):24076-24084. Epub 2016 Sep 27. PubMed PMID: 27679490; PubMed Central PMCID: PMC5104933. 10: Zhao M, Da-Wa ZM, Guo DL, Fang DM, Chen XZ, Xu HX, Gu YC, Xia B, Chen L, Ding LS, Zhou Y. Cytotoxic triterpenoid saponins from Clematis tangutica. Phytochemistry. 2016 Oct;130:228-37. doi: 10.1016/j.phytochem.2016.05.009. Epub 2016 Jun 1. PubMed PMID: 27262876. 11: Saroj VK, Nakade UP, Sharma A, Yadav RS, Hajare SW, Garg SK. Functional involvement of L-type calcium channels and cyclic nucleotide-dependent pathways in cadmium-induced myometrial relaxation in rats. Hum Exp Toxicol. 2017 Mar;36(3):276-286. doi: 10.1177/0960327116646840. Epub 2016 Jul 11. PubMed PMID: 27164925. 12: Xiao X, Ni Y, Jia YM, Zheng M, Xu HF, Xu J, Liao C. 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