An ACL inhibitor
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BMS 303141

Item No. 16239

Technical Information
Formal Name
3,5-dichloro-2-hydroxy-N-(4-methoxy[1,1'-biphenyl]-3-yl)-benzenesulfonamide
CAS Number
943962-47-8
Molecular Formula
C19H15Cl2NO4S
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
DMF: 30 mg/mlDMF:PBS (pH 7.2) (1:1): 0.5 mg/mlDMSO: 25 mg/mlEthanol: 15 mg/ml
λmax
208, 261 nm
SMILES
O=S(NC1=CC(C2=CC=CC=C2)=CC=C1OC)(C3=C(O)C(Cl)=CC(Cl)=C3)=O
InChi Code
InChI=1S/C19H15Cl2NO4S/c1-26-17-8-7-13(12-5-3-2-4-6-12)9-16(17)22-27(24,25)18-11-14(20)10-15(21)19(18)23/h2-11,22-23H,1H3
InChi Key
SIIPNDKXZOTLEA-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    ATP citrate lyase (ACL) catalyzes the synthesis of acetyl-CoA and oxaloacetate using citrate, CoA, and ATP as substrates and Mg2+ as a cofactor.1 The ACL-dependent synthesis of acetyl-CoA is important for the de novo synthesis of fatty acids and cholesterol.2 Furthermore, as a key enzyme for linking glucose and lipid metabolism, ACL is thought to contribute to the Warburg effect in cancer cells.3 BMS 303141 is a cell-permeable, 2-hydroxy-N-arylbenzenesulfonamide that inhibits ACL with an IC50 value of 0.13 µM.4 At an oral dose of 100 mg/kg/day, BMS 303141 has been reported to reduce weight gain and lower plasma cholesterol, triglycerides, and glucose in a mouse model of hyperlipidemia.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ma, Z., Chu, C.H., and Cheng, D. A novel direct homogeneous assay for ATP citrate lyase. J. Lipid Res. 50(10), 2131-2135 (2009).

    2. Dufort, F.J., Gumina, M.R., Ta, N.L., et alGlucose-dependent de novo lipogenesis in B lymphocytes: A requirement for ATP-citrate lyase in lipopolysaccharide-induced differentiation. The Journal of Biological Chemisty 289(10), 7011-7024 (2014).

    3. Zu, X.Y., Zhang, Q.H., Liu, J.H., et alATP citrate lyase inhibitors as novel cancer therapeutic agents. Recent Pat.Anticancer Drug Discov. 7(2), 154-167 (2012).

    4. Li, J.J., Wang, H., Tino, J.A., et al2-hydroxy-N-arylbenzenesulfonamides as ATP-citrate lyase inhibitors. Bioorg. Med. Chem. Lett. 17(11), 3208-3211 (2007).