SJ1008030 (compound 8) formic is a JAK2 PROTAC which selectively degrades JAK2. SJ1008030 formic inhibits MHH–CALL-4 cell growth with an IC50 of 5.4 nM. SJ1008030 formic can be used for the research of leukemia.
SJ1008030 (compound 8) formic (72 h) shows activity in CRLF2r cell lines (MHH–CALL-4), with an IC50 of 5.4 nM[1].SJ1008030 (0-4.3 μM; 72 h) formic degrades JAKs, GSPT1, and IKZF1 in a dose-dependent manner in MHH–CALL-4 cells[1].SJ1008030 (0-10 μM; 24h) formic dose-dependently degrades JAK2 and GSPT1 protein in xenograft bone marrow SJBALL021415 cells, indicating the inhibition of JAK-STAT signaling pathway[1].
References:
[1]. Chang Y, et al. Degradation of Janus kinases in CRLF2-rearranged acute lymphoblastic leukemia. Blood. 2021 Dec 9;138(23):2313-2326.