A pan-family VIII BRD inhibitor
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SGC-SMARCA-BRDVIII

Item No. 33567

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[3-amino-6-(2-hydroxyphenyl)-4-pyridazinyl]-1-piperazinecarboxylic acid, 1,1-dimethylethyl ester
CAS Number
1997319-84-2
Molecular Formula
C19H25N5O3
Formula Weight
371.4
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble
λmax
219, 265, 313 nm
SMILES
O=C(N1CCN(CC1)C2=C(N)N=NC(C3=CC=CC=C3O)=C2)OC(C)(C)C
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)
InChi Key
AQTNUGRRZDRZIA-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $28

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    5 mg

    $83

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    10 mg

    $138

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    25 mg

    $241

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    Cayman Chemical
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    OBESITY RESEARCH SOLUTIONS
    Product Description

    SGC-SMARCA-BRDVIII is a pan-inhibitor of family VIII bromodomain-containing proteins (BRDs), which are components of switch/sucrose nonfermentable (SWI/SNF) chromatin remodeling complexes.1 It selectively binds to polybromo-1D (PBRM1) bromodomain 5, BRM, also known as SMARCA2, and BRG1, also known as SMARCA4 (Kds = 13, 35, and 36 nM, respectively), over PBRM1 bromodomain 2, PBRM1 bromodomain 3, and PBRM1 bromodomain 4 (Kds = 3,655, 1,963, and >10,000 nM, respectively). SGC-SMARCA-BRDVIII (1 µM) decreases lipid accumulation induced by the PPARγ agonist rosiglitazone (Item Nos. 71740 | 11884 | 71742) in 3T3-L1 mouse fibroblasts differentiated into adipocytes by a combination of the phosphodiesterase (PDE) inhibitor IBMX (Item No. 13347), the glucocorticoid dexamethasone (Item No. 11015), and insulin. It decreases expression of the genes encoding PPARγ, C/EBPα, and fatty acid binding protein 4 (FABP4), markers of adipocytes, in the same cells when used at a concentration of 0.5 µM. See the Structural Genomics Consortium (SGC) website for more information.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Wanior, M., Preuss, F., Ni, X., et al. Pan-SMARCA/PB1 bromodomain inhibitors and their role in regulating adipogenesis. J. Med. Chem. 63(23), 14680-14699 (2020).