A p300 and CBP inhibitor
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CCS-1477

Item No. 34546

Technical Information
Formal Name
(6S)-1-(3,4-difluorophenyl)-6-[5-(3,5-dimethyl-4-isoxazolyl)-1-(trans-4-methoxycyclohexyl)-1H-benzimidazol-2-yl]-2-piperidinone
CAS Number
2222941-37-7
Synonyms
  • CBP-IN-1
Molecular Formula
C30H32F2N4O3
Formula Weight
Purity
≥98%
Formulation
A solid
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:3): 0.25 mg/mlEthanol: 10 mg/ml
SMILES
O=C1N(C2=CC(F)=C(C=C2)F)[C@](CCC1)([H])C3=NC4=CC(C5=C(C)ON=C5C)=CC=C4N3[C@]6([H])CC[C@H](CC6)OC
InChi Code
InChI=1S/C30H32F2N4O3/c1-17-29(18(2)39-34-17)19-7-14-26-25(15-19)33-30(36(26)20-8-11-22(38-3)12-9-20)27-5-4-6-28(37)35(27)21-10-13-23(31)24(32)16-21/h7,10,13-16,20,22,27H,4-6,8-9,11-12H2,1-3H3/t20-,22-,27-/m0/s1
InChi Key
SKDNDJWEBPQKCS-CLHVYKLBSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    CCS-1477 is an inhibitor of p300 and CREB-binding protein (CBP) histone acetyltransferases.1 It selectively binds to p300 and CBP over bromodomain-containing protein 4 (BRD4; Kds = 1.3, 1.7, and 222 nM, respectively). CCS-1477 inhibits the proliferation of OPM-2 multiple myeloma cells (GI50 = 5 nM). It induces tumor regression in MOLM-16 acute myeloid leukemia (AML) and OPM-2 mouse xenograft models when administered at a dose of 20 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Brooks, N., Raja, M., Young, B.W., et alCCS1477: A novel small molecule inhibitor of p300/CBP bromodomain for the treatment of acute myeloid leukaemia and multiple myeloma. Blood 134(Supplement 1), 2560 (2019).