MedKoo Cat#: 463732 | Name: SGC-SMARCA-BRDVIII
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Description:

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

SGC-SMARCA-BRDVIII is a selective and high affinity SMARCA2/4 and PB1(bromo 5)-selective SWI/SNF bromodomains (Kd(ITC) values are 35, 36 and 13 nM, respectively). SGC-SMARCA-BRDVIII exhibits selectivity over 25 other bromodomain families and shows no off-target activity on 85 protein kinases screened using temperature-shift binding assays. SGC-SMARCA-BRDVIII suppresses formation of 3T3-L1 mouse fibroblasts into adipocytes (EC50 <1.0 μM).

Chemical Structure

SGC-SMARCA-BRDVIII
SGC-SMARCA-BRDVIII
CAS#1997319-84-2

Theoretical Analysis

MedKoo Cat#: 463732

Name: SGC-SMARCA-BRDVIII

CAS#: 1997319-84-2

Chemical Formula: C19H25N5O3

Exact Mass: 371.1957

Molecular Weight: 371.44

Elemental Analysis: C, 61.44; H, 6.78; N, 18.85; O, 12.92

Price and Availability

Size Price Availability Quantity
10mg USD 150.00 Ready to Ship
25mg USD 250.00 Ready to Ship
50mg USD 450.00 Ready to Ship
100mg USD 750.00 Ready to Ship
200mg USD 1,250.00 Ready to Ship
500mg USD 2,450.00 Ready to Ship
1g USD 3,850.00 Ready to ship
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Related CAS #
Synonym
SGC-SMARCA-BRDVIII; SGCSMARCABRDVIII; SGC SMARCA BRDVIII;
IUPAC/Chemical Name
tert-butyl 4-(3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl)piperazine-1-carboxylate
InChi Key
AQTNUGRRZDRZIA-UHFFFAOYSA-N
InChi Code
InChI=1S/C19H25N5O3/c1-19(2,3)27-18(26)24-10-8-23(9-11-24)15-12-14(21-22-17(15)20)13-6-4-5-7-16(13)25/h4-7,12,25H,8-11H2,1-3H3,(H2,20,22)
SMILES Code
O=C(N1CCN(C2=CC(C3=CC=CC=C3O)=NN=C2N)CC1)OC(C)(C)C
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
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
Biological target:
SGC-SMARCA-BRDVIII is a potent and selective inhibitor of SMARCA2/4 and PB1(5), with Kds of 35 nM, 36 nM, and 13 nM.
In vitro activity:
This study characterized a set of potent and cell-active bromodomain inhibitors with pan-selectivity for canonical family VIII bromodomains. Targeted SWI/SNF bromodomain inhibition blocked the expression of key genes during adipogenesis, including the transcription factors PPARγ and C/EBPα, and impaired the differentiation of 3T3-L1 murine fibroblasts into adipocytes. Reference: J Med Chem. 2020 Dec 10;63(23):14680-14699. https://pubmed.ncbi.nlm.nih.gov/33216538/
In vivo activity:
This study characterized a set of potent and cell-active bromodomain inhibitors with pan-selectivity for canonical family VIII bromodomains. Targeted SWI/SNF bromodomain inhibition blocked the expression of key genes during adipogenesis, including the transcription factors PPARγ and C/EBPα, and impaired the differentiation of 3T3-L1 murine fibroblasts into adipocytes. Reference: J Med Chem. 2020 Dec 10;63(23):14680-14699. https://pubmed.ncbi.nlm.nih.gov/33216538/
Solvent mg/mL mM
Solubility
DMSO 37.1 100.00
Ethanol 3.7 10.00
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 371.44 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:
Wanior M, Preuss F, Ni X, Krämer A, Mathea S, Göbel T, Heidenreich D, Simonyi S, Kahnt AS, Joerger AC, Knapp S. Pan-SMARCA/PB1 Bromodomain Inhibitors and Their Role in Regulating Adipogenesis. J Med Chem. 2020 Dec 10;63(23):14680-14699. doi: 10.1021/acs.jmedchem.0c01242. Epub 2020 Nov 20. PMID: 33216538.
In vitro protocol:
Wanior M, Preuss F, Ni X, Krämer A, Mathea S, Göbel T, Heidenreich D, Simonyi S, Kahnt AS, Joerger AC, Knapp S. Pan-SMARCA/PB1 Bromodomain Inhibitors and Their Role in Regulating Adipogenesis. J Med Chem. 2020 Dec 10;63(23):14680-14699. doi: 10.1021/acs.jmedchem.0c01242. Epub 2020 Nov 20. PMID: 33216538.
In vivo protocol:
Wanior M, Preuss F, Ni X, Krämer A, Mathea S, Göbel T, Heidenreich D, Simonyi S, Kahnt AS, Joerger AC, Knapp S. Pan-SMARCA/PB1 Bromodomain Inhibitors and Their Role in Regulating Adipogenesis. J Med Chem. 2020 Dec 10;63(23):14680-14699. doi: 10.1021/acs.jmedchem.0c01242. Epub 2020 Nov 20. PMID: 33216538.
Wanior, M., Krämer, A., Knapp, S., & Joerger, A. C. (2021). Exploiting vulnerabilities of SWI/SNF chromatin remodelling complexes for cancer therapy. Oncogene, 40(21), 3637-3654. Schwalm, M. P., Babaahmadi, A. K., Ackloo, S., & Knapp, S. (2024). Targeting the Acetylation Reader Family: Bromodomain Proteins. Agbo, L. (2023). Caractérisation des fonctions bromodomaine dépendantes des complexes mSWI/SNF dans les cancers du sein.