A PROTAC that drives BRM, BRG1, and PBRM1 degradation
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ACBI1

Item No. 36612

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(2S,4R)-N-(2-(2-(4-((4-(3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)methyl)phenoxy)ethoxy)-4-(4-methylthiazol-5-yl)benzyl)-1-((S)-2-(1-fluorocyclopropane-1-carboxamido)-3,3-dimethylbutanoyl)-4-hydroxypyrrolidine-2-carboxamide
CAS Number
2375564-55-7
Molecular Formula
C49H58FN9O7S
Formula Weight
936.1
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble
λmax
266 nm
SMILES
NC1=C(N2CCN(CC2)CC3=CC=C(C=C3)OCCOC4=C(C=CC(C5=C(N=CS5)C)=C4)CNC([C@H]6N(C[C@@H](C6)O)C([C@H](C(C)(C)C)NC(C7(CC7)F)=O)=O)=O)C=C(C8=C(C=CC=C8)O)N=N1
InChi Code
InChI=1S/C49H58FN9O7S/c1-30-42(67-29-53-30)32-11-12-33(26-52-45(62)39-24-34(60)28-59(39)46(63)43(48(2,3)4)54-47(64)49(50)15-16-49)41(23-32)66-22-21-65-35-13-9-31(10-14-35)27-57-17-19-58(20-18-57)38-25-37(55-56-44(38)51)36-7-5-6-8-40(36)61/h5-14,23,25,29,34,39,43,60-61H,15-22,24,26-28H2,1-4H3,(H2,51,56)(H,52,62)(H,54,64)/t34-,39+,43-/m1/s1
InChi Key
IVARZBJJMMUJHI-SQKKEFIPSA-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

    ACBI1 is a proteolysis-targeting chimera (PROTAC) composed of a ligand for BRM, also known as SMARCA2, BRG1, also known as SMARCA4, and polybromo-1D (PBRM1), which are components of switch/sucrose nonfermentable (SWI/SNF) chromatin remodeling complexes, conjugated to a von Hippel-Lindau (VHL) E3 ligase ligand.1 It induces degradation of BRM, BRG1, and PBRM1 with 50% degradation concentration (DC50) values of 6, 11, and 32 nM, respectively, in MV4-11 acute myeloid leukemia (AML) cells. ACBI1 decreases the proliferation of MV4-11 cells (IC50 = 28 nM) but is inactive against NCI H1703 non-small cell lung cancer (NSCLC) cells, which do not express BRM or BRG1. It prevents exhaustion of isolated human CD8+ T cells when used at concentrations of 50 and 100 nM.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Farnaby, W., Koegl, M., Roy, M.J., et al. BAF complex vulnerabilities in cancer demonstrated via structure-based PROTAC design. Nat. Chem. Biol. 15(7), 672-680 (2019).

    2. Battistello, E., Hixon, K.A., Comstock, D.E., et al. Stepwise activities of mSWI/SNF family chromatin remodeling complexes direct T cell activation and exhaustion. Mol. Cell. S1097-2765(23), 00153-00153 (2023).