An sPLA2 (Type IIA) inhibitor
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GK241

Item No. 37689

Technical Information
Formal Name
N-(1,2-dioxohexadecyl)-L-valine
CAS Number
1899930-93-8
Molecular Formula
C21H39NO4
Formula Weight
Purity
≥98%
A crystalline solid
DMF: Slightly solubleDMSO: 2 mg/mlEthanol: 1 mg/ml
λmax
244 nm
SMILES
CCCCCCCCCCCCCCC(C(N[C@H](C(O)=O)C(C)C)=O)=O
InChi Code
InChI=1S/C21H39NO4/c1-4-5-6-7-8-9-10-11-12-13-14-15-16-18(23)20(24)22-19(17(2)3)21(25)26/h17,19H,4-16H2,1-3H3,(H,22,24)(H,25,26)/t19-/m0/s1
InChi Key
ZVJNWONHYXBMJL-IBGZPJMESA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    Product Description

    GK241 is a secretory phospholipase A2 (sPLA2) (Type IIA) inhibitor (IC50s = 0.143 and 0.068 µM for the human and mouse enzymes, respectively).1,2 It inhibits IL-1β-induced production of prostaglandin E2 (PGE2; Item No. 14010) in isolated rat renal mesangial cells when used at concentrations of 3 and 10 µM.3 GK241 also inhibits the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) main protease (Mpro), also known as 3C-like protease (3CLpro; IC50 = 24 µM).1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Theodoropoulou, M.A., Koutoulogenis, G.S., Zhang, L., et alIdentification of a dual inhibitor of secreted phospholipase A2 (GIIA sPLA2) and SARS-CoV-2 main protease. Pharmaceuticals (Basel) 15(8), 961 (2021).

    2. Vasilakaki, S., Barbayianni, E., Leonis, G., et alDevelopment of a potent 2-oxoamide inhibitor of secreted phospholipase A2 guided by molecular docking calculations and molecular dynamics simulations. Bioorg. Med. Chem. 24(8), 1683-1695 (2016).

    3. Vasilakaki, S., Barbayianni, E., Magrioti, V., et alInhibitors of secreted phospholipase A2 suppress the release of PGE2 in renal mesangial cells. Bioorg. Med. Chem. 24(13), 3029-3034 (2016).