FINDY
| Code | Size | Price |
|---|
| AG-CR1-3662-M001 | 1 mg | £60.00 |
Quantity:
| AG-CR1-3662-M005 | 5 mg | £210.00 |
Quantity:
Prices exclude any Taxes / VAT
Overview
Regulatory Status: RUO
Shipping:
-20°C
Storage:
Short Term: +4°C. Long Term: -20°C
Documents
Further Information
Alternate Names/Synonyms:
(Z)-5-(4-Methoxy-3-((trimethylsilyl)ethynyl)benzylidene)-2-thioxothiazolidin-4-one
Appearance:
Light to dark yellow solid.
CAS:
1507367-37-4
EClass:
32160000
Form (Short):
liquid
Handling Advice:
Keep cool and dry.Protect from light and moisture.
InChi:
InChI=1S/C16H17NO2S2Si/c1-19-13-6-5-11(9-12(13)7-8-22(2,3)4)10-14-15(18)17-16(20)21-14/h5-6,9-10H,1-4H3,(H,17,18,20)/b14-10-
InChiKey:
JHFDWHHUUUMRLK-UVTDQMKNSA-N
Long Description:
Chemical. CAS: 1507367-37-4. Formula: C16H17NO2S2Si. MW: 347.5. Synthetic. Suppressor of DYKR1A intramolecular Ser97 autophosphorylation. Cell permeable thioxothiazolidinone derivative that 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. Highly selective inhibitor for DYKR1A over other DYRK family members. Unlike INDY and other ATP-competitive DYRK inhibitors, ineffective against the kinase activity of DYRK1A, DYRK1B, DYRK2 or DYRK3 (IC50>10µM). Inhibits only GSK3beta, MARK4, PIM1, PIM3, PLK3 by over 75% at 10µM among a panel of 271 kinases. Selectively rescues the developmental defect of Xenopus embryos induced by the overexpression of DYRK1A, but not DYRK1B.
MDL:
MFCD30718582
Molecular Formula:
C16H17NO2S2Si
Molecular Weight:
347.5
Package Type:
Plastic Vial
Product Description:
Suppressor of DYKR1A intramolecular Ser97 autophosphorylation. Cell permeable thioxothiazolidinone derivative that 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. Highly selective inhibitor for DYKR1A over other DYRK family members. Unlike INDY and other ATP-competitive DYRK inhibitors, ineffective against the kinase activity of DYRK1A, DYRK1B, DYRK2 or DYRK3 (IC50>10µM). Inhibits only GSK3beta, MARK4, PIM1, PIM3, PLK3 by over 75% at 10µM among a panel of 271 kinases. Selectively rescues the developmental defect of Xenopus embryos induced by the overexpression of DYRK1A, but not DYRK1B.
Purity:
>98% (HPLC)
SMILES:
O=C1NC(S/C1=CC2=CC=C(OC)C(C#C[Si](C)(C)C)=C2)=S
Solubility Chemicals:
Soluble in DMSO (25mg/ml).
Transportation:
Non-hazardous
UNSPSC Category:
Protein Kinase Modulators
UNSPSC Number:
12352200
Use & Stability:
Stable for at least 2 years after receipt when stored at -20°C.
References
Selective inhibition of the kinase DYRK1A by targeting its folding process: I. Kii, et al.; Nat. Commun. 7, 11391 (2016)
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