GL-637
GL-637 is a covalent and selective inhibitor of SARS-CoV-1/2 papain-like protease (PLpro), with IC50 values of 42.4 nM and 50.5 nM against the two viruses, respectively. GL-637 covalently modifies the catalytic Cys111 of PLpro, binds to Glu167 and occupies the BL2 groove, thereby inhibiting the deubiquitinase and deISGylase activities of PLpro. GL-637 can be used in the research of coronaviruses.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 3132184-09-6
- 分子式: C37H45FN6O5S
- 分子量:704.85
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
IC50 & Target
[1]|
SARS-CoV-1 PLpro 42.4 nM (IC50) |
SARS-CoV-2 PLpro 50.5 nM (IC50) |
体外実験
GL-637 (treated for 30 min) potently inhibits purified SARS-CoV-1 PLpro, with an IC50 value of 42.4 nM[1].
GL-637 (incubated for 30 min) potently inhibits purified SARS-CoV-2 PLpro, with an IC50 of 50.5 nM[1].
GL-637 is a time-dependent covalent inhibitor of purified SARS-CoV-2 PLpro, with a kinact/KI value of 18,317 M-1 s-1[1].
GL-637 inhibits SARS-CoV-2 PLpro-mediated hydrolysis of Ub-AMC and ISG15-AMC, with IC50 values of 318.4 nM and 438.4 nM, respectively[1].
GL-637 (1-30 μM) shows selectivity for SARS-CoV-1 and SARS-CoV-2 PLpro. It exerts no effect on MERS-CoV PLpro at a concentration of 1 μM, and has no impact on human deubiquitinases USP7 and USP14 even at the highest tested concentration of 30 μM[1].
GL-637 potently inhibits the replication of SARS-CoV-2 in A549-ACE2 cells, with an EC50 of 0.313 μM; this compound shows no detectable cytotoxicity (CC50 > 10 μM), and has a therapeutic index of 31.94[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
化学情報
-
CAS 番号 3132184-09-6
-
分子量 704.85
-
分子式 C37H45FN6O5S
-
SMILES
O=C(OC)/C=C/C(NNC(CCC1=CC=C(N2CCN(C)CC2)C=C1C(N[C@@H](C3=CC=CC(C4=CC=C(CN5C[C@@H](F)CC5)S4)=C3)C)=O)=O)=O
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
-
Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)