JY-1-106
| Code | Size | Price |
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| TAR-T32344-100mg | 100mg | Enquire | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Quantity:
| TAR-T32344-500mg | 500mg | Enquire | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Quantity:
Prices exclude any Taxes / VAT
Overview
Regulatory Status: RUO
Shipping:
cool pack
Storage:
-20°C
Documents
Further Information
Bioactivity:
JY-1-106 is a BH3 α-helix mimetic, inducing apoptosis in a subset of cancer cells (lung cancer, colon cancer and mesothelioma) by disrupting Bcl-xL and Mcl-1 protein-protein interactions with Bak.
CAS:
T32344
Molecular Weight:
550.61
Purity:
0.98
SMILES:
O=C(O)C1=CC=C(NC(C2=NC(OC(C)C)=C(NC(C3=CC=C(N)C(OC(C)C)=C3)=O)C=C2)=O)C(OC(C)C)=C1
References
Cao X, Yap JL, Newell-Rogers MK, Peddaboina C, Jiang W, Papaconstantinou HT, Jupitor D, Rai A, Jung KY, Tubin RP, Yu W, Vanommeslaeghe K, Wilder PT, MacKerell AD Jr, Fletcher S, Smythe RW. The novel BH3 ?-helix mimetic JY-1-106 induces apoptosis in a subset of cancer cells (lung cancer, colon cancer and mesothelioma) by disrupting Bcl-xL and Mcl-1 protein-protein interactions with Bak. Mol Cancer. 2013 May 16;12(1):42. doi: 10.1186/1476-4598-12-42. PubMed PMID: 23680104; PubMed Central PMCID: PMC3663763.
Perri M, Yap JL, Yu J, Cione E, Fletcher S, Kane MA. BCL-xL/MCL-1 inhibition and RAR? antagonism work cooperatively in human HL60 leukemia cells. Exp Cell Res. 2014 Oct 1;327(2):183-91. doi: 10.1016/j.yexcr.2014.07.024. Epub 2014 Aug 1. PubMed PMID: 25088254; PubMed Central PMCID: PMC4727751.
Perri M, Yap JL, Fletcher S, Cione E, Kane MA. Therapeutic potential of Bcl-x(L)/Mcl-1 synthetic inhibitor JY-1-106 and retinoids for human triple-negative breast cancer treatment. Oncol Lett. 2018 May;15(5):7231-7236. doi: 10.3892/ol.2018.8258. Epub 2018 Mar 14. PubMed PMID: 29849791; PubMed Central PMCID: PMC5962833.
Drennen B, Scheenstra JA, Yap JL, Chen L, Lanning ME, Roth BM, Wilder PT, Fletcher S. Structural Re-engineering of the ?-Helix Mimetic JY-1-106 into Small Molecules: Disruption of the Mcl-1-Bak-BH3 Protein-Protein Interaction with 2,6-Di-Substituted Nicotinates. ChemMedChem. 2016 Apr 19;11(8):827-33. doi: 10.1002/cmdc.201500461. Epub 2016 Feb 4. PubMed PMID: 26844930; PubMed Central PMCID: PMC4838500.