MKC8866

Product NameMKC8866
CAS1338934-59-0
MFC18H19NO7
MW361.35
EINECS
MOL File1338934-59-0.mol

Chemical Properties

Boiling point	620.0±55.0 °C(Predicted)
Density	1.373±0.06 g/cm3(Predicted)
storage temp.	Store at -20°C
solubility	DMSO:16.67(Max Conc. mg/mL);46.13(Max Conc. mM)
form	A solid
pka	6.20±0.20(Predicted)
color	Light yellow to yellow

Usage And Synthesis

Uses

MKC8866, a salicylaldehyde analog, is a potent, selective IRE1 RNase inhibitor with an IC50 of 0.29 μM in human vitro. MKC8866 strongly inhibits Dithiothreitol-induced X-box-binding protein 1-spliced (XBP1s) expression with an EC50 of 0.52 μM and unstresses RPMI 8226 cells with an IC50 of 0.14 μM[1]. MKC8866 inhibits IRE1 RNase in breast cancer cells leading to the decreased production of pro-tumorigenic factors and it can inhibits prostate cancer (PCa) tumor growth[2].

Biological Activity

MKC8866 (IRE1-IN-8866) is a salicylaldehyde analog, a specific IRE1α RNase inhibitor with IC50 of 0.29 μM against human IRE1α in vitro.

in vivo

MKC8866 (oral ; 300 mg/kg; for 28 days) reduces tumor regrowth post-NSC 125973 withdrawal^[1].

Animal Model:	Female athymic nude mice with MDA-MB-231 tumor^[1]
Dosage:	300 mg/kg
Administration:	Oral; for 28 days
Result:	Reduced tumor regrowth post-NSC 125973 withdrawal.

target

Target	Value
hIRE1α (Cell-free assay)	0.29 μM

References

[1] Sheng X, et al. IRE1α-XBP1s pathway promotes prostate cancer by activating c-MYC signaling. Nat Commun. 2019 Jan 24;10(1):323. DOI:10.1038/s41467-018-08152-3
[2] Logue SE, et al. Inhibition of IRE1 RNase activity modulates the tumor cell secretome and enhances response to chemotherapy. Nat Commun. 2018 Aug 15;9(1):3267. DOI:10.1038/s41467-018-05763-8