4-Thiazolidinone, 5-[[4-methoxy-3-[2-(trimethylsilyl)ethynyl]phenyl]methylene]-2-thioxo-, (5Z)-
- CAS No.
- 1507367-37-4
- Chemical Name:
- 4-Thiazolidinone, 5-[[4-methoxy-3-[2-(trimethylsilyl)ethynyl]phenyl]methylene]-2-thioxo-, (5Z)-
- Synonyms
- FINDY;FINDY >=98% (HPLC);4-Thiazolidinone, 5-[[4-methoxy-3-[2-(trimethylsilyl)ethynyl]phenyl]methylene]-2-thioxo-, (5Z)-
- CBNumber:
- CB98178504
- Molecular Formula:
- C16H17NO2S2Si
- Molecular Weight:
- 347.53
- MDL Number:
- MFCD30718582
- MOL File:
- 1507367-37-4.mol
4-Thiazolidinone, 5-[[4-methoxy-3-[2-(trimethylsilyl)ethynyl]phenyl]methylene]-2-thioxo-, (5Z)- price
4-Thiazolidinone, 5-[[4-methoxy-3-[2-(trimethylsilyl)ethynyl]phenyl]methylene]-2-thioxo-, (5Z)- Chemical Properties,Uses,Production
Uses
FINDY is a folding intermediate-selective inhibitor of DYRK1A. FINDY can inhibit Ser97 autophosphorylation with an IC50 value of 35 μM. FINDY can be used for the research of neurological disorder[1]. FINDY is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Biological Activity
FINDY is a cell-permeable thioxothiazolidinone derivative th at specifically targets newly synthesized cellular DYRK1A, but not DYRK1B or DYRK2, for proteasomal degradation by suppressing DYKR1A intramolecular Ser97 autophosphorylation, a necessary event for folding/maturation of newly translated DYRK1A. Unlike INDY and other ATP-competitive DYRK inhibitors, FINDY is ineffective against the kinase activity of DYRK1A, DYRK1B, DYRK2, or DYRK3 (IC50 >10 μM) and inhibits only five kinases (GSK3β, MARK4, PIM1, PIM3, PLK3) by over 75% at 10 μM among a panel of 271 other kinases. FINDY (2.5 μM) is shown to selectively rescue the developmental defect of Xenopus embryos induced by the overexpression of DYRK1A, but not DYRK1B, while INDY prodrug (2.5 μM) treatment indiscriminately prevents defect caused by both DYRK1A and DYRK1B expression.', 'FINDY is a structural analog of RD0392, a canonical ATP-competitive inhibitor of mature dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A).
References
[1] Yuka Miyazaki, et al. Structure-activity relationship for the folding intermediate-selective inhibition of DYRK1A. Eur J Med Chem. 2022 Jan 5;227:113948. DOI:10.1016/j.ejmech.2021.113948
4-Thiazolidinone, 5-[[4-methoxy-3-[2-(trimethylsilyl)ethynyl]phenyl]methylene]-2-thioxo-, (5Z)- Preparation Products And Raw materials
Raw materials
Preparation Products
4-Thiazolidinone, 5-[[4-methoxy-3-[2-(trimethylsilyl)ethynyl]phenyl]methylene]-2-thioxo-, (5Z)- Suppliers
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
TargetMol Chemicals Inc. | +8613564774135 | zijue.cai@tsbiochem.com | United States | 19881 | 58 |
Shanghai EFE Biological Technology Co., Ltd. | 021-65675885 18964387627 | info@efebio.com | China | 9803 | 58 |
Energy Chemical | 021-58432009 400-005-6266 | marketing1@energy-chemical.com | China | 44812 | 58 |
TargetMol Chemicals Inc. | 15002134094 | marketing@targetmol.cn | China | 19699 | 58 |
Adipogen Life Sciences | 41-6192660-40 | info@adipogen.com | China | 5293 | 58 |
Merck KGaA | (+86) 21 2033 8288 | sigmaname@qq.com | CHINA | 292394 | 58 |
Supplier | Advantage |
---|---|
TargetMol Chemicals Inc. | 58 |
Shanghai EFE Biological Technology Co., Ltd. | 58 |
Energy Chemical | 58 |
TargetMol Chemicals Inc. | 58 |
Adipogen Life Sciences | 58 |
Merck KGaA | 58 |