MKC8866

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].

Product Specifications

CAS Number

[1338934-59-0]

Product Name Alternative

Orin1001

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

IRE1

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/IRE-1_alpha__inhibitor_1.html

Concentration

10mM

Purity

99.95

Solubility

DMSO : 6.67 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=CC1=C(O2)C(C(C)=C(CC(N3CCOCC3)=O)C2=O)=CC(OC)=C1O

Molecular Formula

C18H19NO7

Molecular Weight

361.35

Precautions

H302, H315, H319, H335

References & Citations

[1]Sheng X, et al. IRE1α-XBP1s pathway promotes prostate cancer by activating c-MYC signaling. Nat Commun. 2019 Jan 24;10 (1) :323.|[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.