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Chemical Structure : KME-2780
Catalog No.: PC-21201Not For Human Use, Lab Use Only.
KME-2780 (KME2780) is a potent and selective dual IRAK1 and IRAK4 (IRAK1/4) inhibitor with IC50 of 19 and 0.5 nM, respectively.
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KME-2780 (KME2780) is a potent and selective dual IRAK1 and IRAK4 (IRAK1/4) inhibitor with IC50 of 19 and 0.5 nM, respectively.
KME-2780 shows Kd values of 2.2 and 0.2 nM for IRAK1 and IRAK4, respectively.
KME-2780 is significantly more effective at suppressing TLR2-mediated activation of NF-κB and autophosphorylation of IRAK1 in AML cells as compared with the IRAK4 seleective inhibitor KME-3859.
KME-2780 downregulats genes in MAPK/AP1, ATF4, IGFBP, and EGFR signaling in AML cells.
KME-2780 suppresses eukemia stem/progenitor cells (LSPCs), suppresses OCI-AML3 cells, which is insensitive to the genetic inactivation of IRAK1 and IRAK4.
KME-2780 treatment also resulted in a greater expression of CD38, a glycoprotein expressed on mature immune cells.
KME-2780 (30 mg/kg, orally daily) suppresses MDS/AML in xenografted mice.
| M.Wt | 333.44 | |
| Formula | C20H23N5 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Bennett J, et al. Blood. 2023 Sep 14;142(11):989-1007.
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