WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H130093
CAS#: 2721998-87-2
Description: GSK3 Degrader PT-65 is a highly potent and selective GSK3 degrader for the treatment of Alzheimer's Disease (GSK3α DC50 = 28.3 nM and GSK3β DC50 = 34.2 nM in SH-SY5Y cells). PT-65 was found to be able to successfully suppress tau hyperphosphorylation for both in cell and invivo models of Alzheimer's Disease.
Hodoodo Cat#: H130093
Name: GSK3 Degrader PT-65
CAS#: 2721998-87-2
Chemical Formula: C51H63N13O12S
Exact Mass: 1,081.44
Molecular Weight: 1,082.200
Elemental Analysis: C, 56.60; H, 5.87; N, 16.83; O, 17.74; S, 2.96
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Synonym: GSK3 Degrader PT-65; PT-65; PT65; PT 65
IUPAC/Chemical Name: 3-Amino-6-(4-((4-(4-(1-(17-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)-3,6,9,12,15-pentaoxaheptadecyl)-1H-1,2,3-triazol-4-yl)butyl)piperazin-1-yl)sulfonyl)phenyl)-N-(pyridin-3-yl)pyrazine-2-carboxamide
InChi Key: QJSFLEBIQZMJQF-UHFFFAOYSA-N
InChi Code: InChI=1S/C51H63N13O12S/c52-47-46(49(67)56-37-6-4-15-53-33-37)57-42(34-55-47)36-9-11-39(12-10-36)77(70,71)63-20-18-61(19-21-63)17-2-1-5-38-35-62(60-59-38)22-24-73-26-28-75-30-32-76-31-29-74-27-25-72-23-16-54-41-8-3-7-40-45(41)51(69)64(50(40)68)43-13-14-44(65)58-48(43)66/h3-4,6-12,15,33-35,43,54H,1-2,5,13-14,16-32H2,(H2,52,55)(H,56,67)(H,58,65,66)
SMILES Code: O=C(C1=NC(C2=CC=C(S(=O)(N3CCN(CCCCC4=CN(CCOCCOCCOCCOCCOCCNC5=CC=CC(C(N6C(CC7)C(NC7=O)=O)=O)=C5C6=O)N=N4)CC3)=O)C=C2)=CN=C1N)NC8=CC=CN=C8
Appearance: To be determined
Purity: >98% (or refer to the Certificate of Analysis)
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.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: To be determined
Shelf Life: >2 years if stored properly
Drug Formulation: To be determined
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
| Biological target: | |
| In vitro activity: | |
| In vivo activity: |
The following data is based on the product molecular weight 1,082.20 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: |
1. Qu L, Li S, Ji L, Luo S, Ding M, Yin F, Wang C, Luo H, Lu D, Liu X, Peng W, Kong L, Wang X. Discovery of PT-65 as a highly potent and selective Proteolysis-targeting chimera degrader of GSK3 for treating Alzheimer's disease. Eur J Med Chem. 2021 Dec 15;226:113889. doi: 10.1016/j.ejmech.2021.113889. Epub 2021 Oct 2. PMID: 34649182.
