JCS-1 

JCS-1 is a potent DcpS PROTAC degrader. JCS-1 non-covalently binds DcpS with a RG3039-based warhead and recruits the E3 ligase VHL. JCS-1 promotes ubiquitination and degradation of DcpS at nanomolar concentrations (DC₅₀ in MOLM-14 cells: 87 nM). JCS-1 can be used for the research of AML and other DcpS-dependent genetic disorders (Pink: DcpS ligand (HY-102020); Blue: E3 ligase VHL ligand (HY-151227); Black: linker (HY-141230))^[1].

JCS-1 (0.1-10000 nM, 24 h) degrades DcpS in MOLM-14 cells in a dose-dependent manner with a DC₅₀ of 87 nM^[1].
JCS-1 (1 μM) degrades DcpS rapidly and continuously in MOLM-14 cells, with degradation occurring rapidly within 2 h of treatment and maximum degradation occurring between 12 and 24 h^[1].
JCS-1 (1 μM, every 3 days for 12 days) inhibits the proliferation and viability of MOLM-14 cells with an IC₅₀ value of 1.1 μM^[1].
JCS-1 (1 μM, 6 h) influences the mRNA pool of MOLM-14 cells with significant increase in SNORD99 and DDX24 expression^[1].
Degradation by JCS-1 is inhibited by the neddylation inhibitor MLN4924 (HY-70062) and proteasome inhibitor Epoxomicin (HY-13821) ^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

1174.41

C₆₂H₇₉N₉O₁₂S

O=C([C@H]1N(C([C@@H](N(CC2=C3C=CC=C2)C3=O)C(C)C)=O)C[C@H](O)C1)NCC4=CC=C(C5=C(C)N=CS5)C=C4OCCOCCOCCOCCOCCOCCOC6=CC=CC(CN7CCC(COC8=CC=CC9=NC(N)=NC(N)=C89)CC7)=C6

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• [1]. Swartzel, et al. Targeted Degradation of mRNA Decapping Enzyme DcpS by a VHL-Recruiting PROTAC. ACS chemical biology. 2022, 17(7), 1789–1798.  [Content Brief]