A BD1 inhibitor
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GSK778

Item No. 41280

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
7-(3,5-dimethyl-4-isoxazolyl)-2-(methoxymethyl)-1-[(1R)-1-phenylethyl]-8-[(3S)-3-pyrrolidinylmethoxy]-1H-imidazo[4,5-c]quinoline
CAS Number
2451862-42-1
Synonyms
  • iBET-BD1
  • iBET-Bromodomain 1
Molecular Formula
C30H33N5O3
Formula Weight
511.6
Purity
≥95%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥10 mg/mlEthanol: Soluble: ≥10 mg/ml
SMILES
C[C@H](C1=CC=CC=C1)N2C(COC)=NC(C=NC3=C4)=C2C3=CC(OC[C@H]5CCNC5)=C4C6=C(ON=C6C)C
InChi Code
InChI=1S/C30H33N5O3/c1-18-29(20(3)38-34-18)24-12-25-23(13-27(24)37-16-21-10-11-31-14-21)30-26(15-32-25)33-28(17-36-4)35(30)19(2)22-8-6-5-7-9-22/h5-9,12-13,15,19,21,31H,10-11,14,16-17H2,1-4H3/t19-,21+/m1/s1
InChi Key
ZORLJXWXFABTPZ-CTNGQTDRSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Cayman Chemical
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    Product Description

    GSK778 is a bromodomain 1 (BD1) inhibitor.1 It selectively inhibits BD1 in bromodomain-containing protein 2 (BRD2), BRD3, BRD4, and bromodomain testis-specific protein (BRDT; IC50s = 79.43, 39.81, 39.81, and 158.49 nM, respectively, in time-resolved FRET assays) over BD2 in BRD2, BRD3, BRD4, and BRDT (IC50s = 3,162, 1,000, 6,309, and >10,000 nM, respectively, in time-resolved FRET assays). GSK778 inhibits LPS-induced increases in IL-6 and chemokine (C-C motif) ligand 2 (CCL2) secretion from primary human peripheral blood mononuclear cells (PBMCs; IC50s = 63.12 and 50.12 nM, respectively). It inhibits the proliferation of MV4-11 acute myeloid leukemia cells (IC50 = 200 nM). 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. Wellaway, C.R., Bamborough, P., Bernard, S.G., et al. Structure-based design of a bromodomain and extraterminal domain (BET) inhibitor selective for the N-terminal bromodomains that retains an anti-inflammatory and antiproliferative phenotype. J. Med. Chem. 63(17), 9020-9044 (2020).