MKC-8866 | B2785

MKC-8866 is a potent, and selective IRE1 RNase inhibitor with an IC50 of 0.29 μM in human vitro. MKC-8866 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. MKC-8866 also strongly inhibits prostate cancer (PCa) tumor growth as monotherapy in multiple preclinical models in mice and shows synergistic antitumor effects with current PCa drugs.

MKC-8866 is a potent, and selective IRE1 RNase inhibitor with an IC50 of 0.29 μM in human vitro. MKC-8866 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. MKC-8866 also strongly inhibits prostate cancer (PCa) tumor growth as monotherapy in multiple preclinical models in mice and shows synergistic antitumor effects with current PCa drugs.

B2785 | MKC-8866 DataSheet

Alternate Name/Synonyms: IRE1-IN-8866,MKC8866,7-Hydroxy-6-methoxy-4-methyl-3-(2-morpholino-2-oxoethyl)-2-oxo-2H-chromene-8-carbaldehyde

Appearance: Crystalline solid

Formulation:

CAS Number: 1338934-59-0

Structure Available?: Yes

Peptide sequence: N/A

Salt Form: No

Molecular Formula: C₁₈H₁₉NO₇

Molecular Weight: 361.35

Cell-Permeable?: TRUE

Purity: ≥98%

Solubilities: ~ 3 mg/ml DMSO

Handling: Do not take internally. Wear gloves and mask when handling the product! Avoid contact by all modes of exposure.

Country of Origin: USA

Tag Line: A selective IRE1 RNase inhibitor

MDL Number:

PubChem CID: 89542346

SMILES: O=CC1=C(O)C(OC)=CC2=C1OC(C(CC(N3CCOCC3)=O)=C2C)=O

InChi: InChI=1S/C18H19NO7/c1-10-11-7-14(24-2)16(22)13(9-20)17(11)26-18(23)12(10)8-15(21)19-3-5-25-6-4-19/h7,9,22H,3-6,8H2,1-2H3

InChi Key: IFDGMRMUJYGWQQ-UHFFFAOYSA-N