MKC-8866
MKC-8866, also known as IRE1-IN-8866, is an inhibitor of IRE1 RNase activity. MKC8866 strongly inhibits prostate cancer (PCa) tumor growth as monotherapy in multiple preclinical models in mice and shows synergistic antitumor effects with current PCa drugs. Interestingly, global transcriptomic analysis reveal that IRE1α-XBP1s pathway activity is required for c-MYC signaling, one of the most highly activated oncogenic pathways in PCa.
For research use only. We do not sell to patients.
Chemical Information
| Name | MKC-8866 |
|---|---|
| Iupac Chemical Name | 7-Hydroxy-6-methoxy-4-methyl-3-(2-morpholino-2-oxoethyl)-2-oxo-2H-chromene-8-carbaldehyde |
| Synonyms | MKC-8866; MKC 8866; MKC8866; IRE1-IN-8866; IRE1IN8866; IRE1 IN 8866; IRE1-IN8866; IRE1-IN 8866; IRE1IN-8866; IRE1IN 8866 |
| Molecular Formula | C18H19NO7 |
| Molecular Weight | 361.35 |
| Smile | O=CC1=C(O)C(OC)=CC2=C1OC(C(CC(N3CCOCC3)=O)=C2C)=O |
| InChiKey | IFDGMRMUJYGWQQ-UHFFFAOYSA-N |
| 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 |
| CAS Number | 1338934-59-0 |
| Related CAS |
Ordering Information
| Packaging | Price | Availability | Purity | Shipping Time |
|---|---|---|---|---|
| Bulk | Enquiry | Enquiry | Enquiry |
| Formulation | Solid powder |
|---|---|
| Purity | 98% Min. |
| Storage | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| Solubility | Soluble in DMSO |
| Handling | |
| Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
| HS Code |
| Targets | |
|---|---|
| Mechanism | |
| Cell study | |
| Animal study | |
| Clinical study |
1: Dastghaib S, Shojaei S, Mostafavi-Pour Z, Sharma P, Patterson JB, Samali A, Mokarram P, Ghavami S. Simvastatin Induces Unfolded Protein Response and Enhances Temozolomide-Induced Cell Death in Glioblastoma Cells. Cells. 2020 Oct 22;9(11):2339. doi: 10.3390/cells9112339. PMID: 33105603; PMCID: PMC7690447.
2: Vieri M, Preisinger C, Schemionek M, Salimi A, Patterson JB, Samali A, Brümmendorf TH, Appelmann I, Kharabi Masouleh B. Targeting of BCR-ABL1 and IRE1α induces synthetic lethality in Philadelphia-positive acute lymphoblastic leukemia. Carcinogenesis. 2021 Feb 25;42(2):272-284. doi: 10.1093/carcin/bgaa095. PMID: 32915195.
3: Le Reste PJ, Pineau R, Voutetakis K, Samal J, Jégou G, Lhomond S, Gorman AM, Samali A, Patterson JB, Zeng Q, Pandit A, Aubry M, Soriano N, Etcheverry A, Chatziioannou A, Mosser J, Avril T, Chevet E. Local intracerebral inhibition of IRE1 by MKC8866 sensitizes glioblastoma to irradiation/chemotherapy in vivo. Cancer Lett. 2020 Dec 1;494:73-83. doi: 10.1016/j.canlet.2020.08.028. Epub 2020 Sep 1. PMID: 32882336.
4: McCarthy N, Dolgikh N, Logue S, Patterson JB, Zeng Q, Gorman AM, Samali A, Fulda S. The IRE1 and PERK arms of the unfolded protein response promote survival of rhabdomyosarcoma cells. Cancer Lett. 2020 Oct 10;490:76-88. doi: 10.1016/j.canlet.2020.07.009. Epub 2020 Jul 15. PMID: 32679165.
5: Sheng X, Nenseth HZ, Qu S, Kuzu OF, Frahnow T, Simon L, Greene S, Zeng Q, Fazli L, Rennie PS, Mills IG, Danielsen H, Theis F, Patterson JB, Jin Y, Saatcioglu F. 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. PMID: 30679434; PMCID: PMC6345973.
6: Wilhelm T, Bick F, Peters K, Mohta V, Tirosh B, Patterson JB, Kharabi- Masouleh B, Huber M. Infliction of proteotoxic stresses by impairment of the unfolded protein response or proteasomal inhibition as a therapeutic strategy for mast cell leukemia. Oncotarget. 2017 Dec 17;9(3):2984-3000. doi: 10.18632/oncotarget.23354. PMID: 29423023; PMCID: PMC5790440.
Chemical Structure
