SH514 is an orally active IRF4 inhibitor (IC50 = 2.63 µM). SH514 binds to the IRF4-DBD domain, thereby inhibiting the interaction of IRF4 protein with DNA (KD = 1.28 µM). SH514 can inhibit the proliferation of IRF4-high-expressing NCI-H929 and MM.1R cells, and displays no cytotoxicity for normal cells. SH514 significantly downregulates the expression of IRF4 downstream target genes concentration-dependently. SH514 inhibits the expression of cell cycle-related proteins CDC2, Cyclin B1, Cyclin D1, Cyclin E1, and CMYC in Multiple Myeloma cells. SH514 can induce DNA damage and increase the expression of gammaH2AX. SH514 effectively inhibits the proliferation of multiple myeloma tumors [1].
Molecular Weight:
514.66
Purity:
99.94
Formula:
C32H38N2O4
Target:
CDK,c-Myc,DNA/RNA Synthesis,IFNAR
Application Notes:
MCE Product type: Reference compound
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