(S)-2,2-dimethyl-1-(5-phenyl-4,5-dihydro-1H-pyrazol-1-yl)propan-1-one
- Product Name
- (S)-2,2-dimethyl-1-(5-phenyl-4,5-dihydro-1H-pyrazol-1-yl)propan-1-one
- CAS No.
- 2049868-46-2
- Chemical Name
- (S)-2,2-dimethyl-1-(5-phenyl-4,5-dihydro-1H-pyrazol-1-yl)propan-1-one
- Synonyms
- GSK'963;GSK963, 10 mM in DMSO;GSK-963;GSK 963;GSK'963;(S)-2,2-dimethyl-1-(5-phenyl-4,5-dihydro-1H-pyrazol-1-yl)propan-1-one;1-Propanone, 1-[(5S)-4,5-dihydro-5-phenyl-1H-pyrazol-1-yl]-2,2-dimethyl-;GSK963,Inhibitor,RIP kinase,GSK 963,Receptor-interacting protein kinases,inhibit,GSK-963,RIPK
- CBNumber
- CB94656211
- Molecular Formula
- C14H18N2O
- Formula Weight
- 230.31
- MOL File
- 2049868-46-2.mol
(S)-2,2-dimethyl-1-(5-phenyl-4,5-dihydro-1H-pyrazol-1-yl)propan-1-one Property
- Boiling point:
- 342.8±45.0 °C(Predicted)
- Density
- 1.06±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO : 25 mg/mL (108.55 mM; Need ultrasonic)
- form
- Solid
- pka
- 0.98±0.40(Predicted)
- color
- Light yellow to yellow
N-Bromosuccinimide Price
- Product number
- SML2376
- Product name
- GSK′963
- Purity
- ≥98% (HPLC)
- Packaging
- 5MG
- Price
- $132
- Updated
- 2025/07/31
- Product number
- SML2376
- Product name
- GSK′963
- Purity
- ≥98% (HPLC)
- Packaging
- 25MG
- Price
- $528
- Updated
- 2025/07/31
- Product number
- G797815
- Product name
- GSK''963
- Packaging
- 1mg
- Price
- $220
- Updated
- 2021/12/16
- Product number
- 023013
- Product name
- GSK963
- Packaging
- 001
- Price
- $550
- Updated
- 2021/12/16
- Product number
- 023013
- Product name
- GSK963
- Packaging
- 002
- Price
- $950
- Updated
- 2021/12/16
(S)-2,2-dimethyl-1-(5-phenyl-4,5-dihydro-1H-pyrazol-1-yl)propan-1-one Chemical Properties,Usage,Production
Uses
GSK''963 is a novel highly potent and selective RIP1 inhibitor.
Biological Activity
GSKμ963 (GSKμ963A) is a brain-penetrant, highly potent and selective ATP site-targeting receptor-interacting protein 1 kinase (RIP1; RIPK1) inhibitor (IC50 = 0.8-8 nM with 50 μM ATP; IC50 >10 μM against RIPK2/3/5 and 335 other kinases) th at protects against TNFα/zVAD-induced necroptosis (EC50 = 1/4 nM in mouse L929/human U937 cultures) and blocks Y. pestis-induced death of murine fetal liver macrophages (1 μM). GSKμ963 prevents lethal hypothermia by acute sterile shock (2 mg/kg i.p. 15 min prior to TNFα/zVAD i.v.) and protects against acute neuronal death upon autologous blood intracerebral hemorrhage induction in mice in vivo (25 mg/kg/3 hr i.p.).
in vivo
GSK963 (2 mg/kg) results in a complete protection from TNF+zVAD-induced temperature loss. GSK963 (0.2 mg/kg) also shows a significant response[1].
| Animal Model: | C57BL/6 mice[1]. |
| Dosage: | 0.2 mg/kg, 2 mg/kg, 10?mg/kg. |
| Administration: | IP once. |
| Result: | Protected mice from TNF+zVAD-induced hypothermia. |
(S)-2,2-dimethyl-1-(5-phenyl-4,5-dihydro-1H-pyrazol-1-yl)propan-1-one Preparation Products And Raw materials
Raw materials
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