A non-selective inhibitor of CaCCs
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CaCC(inh)-A01

Item No. 21922

Technical Information
Formal Name
6-(1,1-dimethylethyl)-2-[(2-furanylcarbonyl)amino]-4,5,6,7-tetrahydro-benzo[b]thiophene-3-carboxylic acid
CAS Number
407587-33-1
Synonyms
  • TMEM16 Blocker I
Molecular Formula
C18H21NO4S
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:2): 0.3 mg/ml
λmax
228, 258, 343 nm
SMILES
CC(C)(C)C1CCC(C(C(O)=O)=C(NC(C2=CC=CO2)=O)S3)=C3C1
InChi Code
InChI=1S/C18H21NO4S/c1-18(2,3)10-6-7-11-13(9-10)24-16(14(11)17(21)22)19-15(20)12-5-4-8-23-12/h4-5,8,10H,6-7,9H2,1-3H3,(H,19,20)(H,21,22)
InChi Key
ACLUEOBQFRYTQS-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    CaCC(inh)-A01 is a non-selective inhibitor of calcium-activated chloride channels (CaCCs) that blocks ATP-stimulated chloride conductance in human salivary gland, intestinal, and bronchial epithelium (mean IC50 = 10 µM).1 CaCC(inh)-A01 (30 µM) induces full vasorelaxation of preconstricted mouse isolated mesenteric arteries in the presence or absence of chloride.2 CaCC(inh)-A01 also attenuates CaCC TMEM16-A-induced proliferation in cancer cell lines through targeted degradation of the protein and reduces the activity of large-conductance calcium-activated potassium channels (KCa1.1/BK) in human red blood cells.3,4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. De La Fuente, R., Namkung, W., Mills, A., et alSmall-molecule screen identifies inhibitors of a human intestinal calcium-activated chloride channel. Mol. Pharmacol. 73(3), 758-768 (2008).

    2. Boedtkjer, D.M.B., Kim, S., Jensen, A.B., et alNew selective inhibitors of calcium-activated chloride channels - T16Ainh-A01, CaCCinh-A01 and MONNA - what do they inhibit? Br. J. Pharmacol. 172(16), 4158-4172 (2015).

    3. Bill, A., Hall, M.L., Borawski, J., et alSmall molecule-facilitated degradation of ANO1 protein: A new targeting approach for anticancer therapeutics. The Journal of Biological Chemisty 289(16), 11029-11041 (2014).

    4. Kucherenko, Y.V., Wagner-Britz, L., Bernhardt, I., et alEffect of chloride channel inhibitors on cytosolic Ca2+ Levels and Ca2+-activated K+ (Gardos) channel activity in human red blood cells. J. Membr. Biol. 246(4), 315-326 (2013).