An ABHD17 inhibitor
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ABD957

Item No. 44290

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
8-[2-[[(3S)-4-[[3-[(dimethylamino)sulfonyl]-1H-pyrazol-1-yl]carbonyl]-3-methyl-1-piperazinyl]methyl]-5-(trifluoromethyl)phenyl]-3,8-diazabicyclo[3.2.1]octane-3-acetic acid
CAS Number
3007772-60-0
Molecular Formula
C27H36F3N7O5S
Formula Weight
627.7
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble
SMILES
C[C@H](N(CC1)C(N2N=C(C=C2)S(N(C)C)(=O)=O)=O)CN1CC3=C(N4C5CCC4CN(CC(O)=O)C5)C=C(C(F)(F)F)C=C3
InChi Code
InChI=1S/C27H36F3N7O5S/c1-18-13-33(10-11-35(18)26(40)36-9-8-24(31-36)43(41,42)32(2)3)14-19-4-5-20(27(28,29)30)12-23(19)37-21-6-7-22(37)16-34(15-21)17-25(38)39/h4-5,8-9,12,18,21-22H,6-7,10-11,13-17H2,1-3H3,(H,38,39)/t18-,21?,22?/m0/s1
InChi Key
ISNXAOFEMNFJCO-XTWGIRIWSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $655

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    Product Description

    ABD957 is an inhibitor of α/β-hydrolase domain-containing protein 17 (ABHD17; IC50 = 0.21 µM for ABHD17B).1 It is selective for ABHD17A-C over a panel of 52 serine hydrolases, including the depalmitoylases ABHD10, palmitoyl-protein thioesterase 1 (PPT1), and lysophospholipase 1 (LYPLA1) and LYPLA2, at 10 µM but does inhibit ABHD6, ABHD11, ABHD13, and carboxylesterase 1 (CES1) and CES2 at the same concentration. ABD957 increases the palmitoylation of N-Ras in OCI-AML-3 acute myeloid leukemia (AML) cells expressing GFP-N-RasG12D (EC50 = 29 nM). It also increases the plasma membrane localization of N-Ras in the same cells when used at a concentration of 500 nM. ABD957 inhibits the growth of OCI-AML-3 cells in a concentration-dependent manner.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Remsberg, J.R., Suciu, R.M., Zambetti, N.A., et al. ABHD17 regulation of plasma membrane palmitoylation and N-Ras-dependent cancer growth. Nat. Chem. Biol. 17(8), 856-864 (2021).