Synonym
GSK 962; GSK962; GSK-962; GSK-962A; GSK962A; GSK 962A; GSK′ 962A; GSK′962A; GSK′-962A; GSK 963 inactive control; GSK 963 negative control; GSK′963 inactive control; GSK′963 negative control;
IUPAC/Chemical Name
2,2-Dimethyl-1-(5(R)-phenyl-4,5-dihydro-pyrazol-1-yl)-propan-1-one
InChi Key
NJQVSLWJBLPTMD-GFCCVEGCSA-N
InChi Code
InChI=1S/C14H18N2O/c1-14(2,3)13(17)16-12(9-10-15-16)11-7-5-4-6-8-11/h4-8,10,12H,9H2,1-3H3/t12-/m1/s1
SMILES Code
CC(C)(C)C(N1N=CC[C@@H]1C2=CC=CC=C2)=O
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
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
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
Biological target:
GSK962 is an inactive enantiomer of GSK963 and can be used to confirm on-target effects.
In vitro activity:
GSK′963 efficiently blocked necroptosis in both murine and human cells with IC50 values of 1 nM and 4 nM, respectively, whereas the inactive analog GSK′962 was at least 1000-fold less potent in these assays (Figures 2a and b).
Reference: Cell Death Discov. 2015 Jul 27;1:15009. https://pubmed.ncbi.nlm.nih.gov/27551444/
In vivo activity:
Treatment of animals with 2 mg/kg of GSK′963 resulted in a complete protection from TNF+zVAD-induced temperature loss, with the 0.2 mg/kg dose also showing a significant response (Figure 3c). As expected, GSK′962 had no effect on the TNF+zVAD-induced shock, confirming that GSK′963 was acting selectively through RIP1 kinase inhibition (Figure 3d).
Reference: Cell Death Discov. 2015 Jul 27;1:15009. https://pubmed.ncbi.nlm.nih.gov/27551444/
|
Solvent |
mg/mL |
mM |
| Solubility |
| DMSO |
75.0 |
325.65 |
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.
Preparing Stock Solutions
The following data is based on the
product
molecular weight
230.31
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:
1. Berger SB, Harris P, Nagilla R, Kasparcova V, Hoffman S, Swift B, Dare L, Schaeffer M, Capriotti C, Ouellette M, King BW, Wisnoski D, Cox J, Reilly M, Marquis RW, Bertin J, Gough PJ. Characterization of GSK'963: a structurally distinct, potent and selective inhibitor of RIP1 kinase. Cell Death Discov. 2015 Jul 27;1:15009. doi: 10.1038/cddiscovery.2015.9. PMID: 27551444; PMCID: PMC4979471.
In vitro protocol:
1. Berger SB, Harris P, Nagilla R, Kasparcova V, Hoffman S, Swift B, Dare L, Schaeffer M, Capriotti C, Ouellette M, King BW, Wisnoski D, Cox J, Reilly M, Marquis RW, Bertin J, Gough PJ. Characterization of GSK'963: a structurally distinct, potent and selective inhibitor of RIP1 kinase. Cell Death Discov. 2015 Jul 27;1:15009. doi: 10.1038/cddiscovery.2015.9. PMID: 27551444; PMCID: PMC4979471.
In vivo protocol:
1. Berger SB, Harris P, Nagilla R, Kasparcova V, Hoffman S, Swift B, Dare L, Schaeffer M, Capriotti C, Ouellette M, King BW, Wisnoski D, Cox J, Reilly M, Marquis RW, Bertin J, Gough PJ. Characterization of GSK'963: a structurally distinct, potent and selective inhibitor of RIP1 kinase. Cell Death Discov. 2015 Jul 27;1:15009. doi: 10.1038/cddiscovery.2015.9. PMID: 27551444; PMCID: PMC4979471.
1: Berger SB, Harris P, Nagilla R, Kasparcova V, Hoffman S, Swift B, Dare L, Schaeffer M, Capriotti C, Ouellette M, King BW, Wisnoski D, Cox J, Reilly M, Marquis RW, Bertin J, Gough PJ. Characterization of GSK'963: a structurally distinct, potent and selective inhibitor of RIP1 kinase. Cell Death Discov. 2015 Jul 27;1:15009. doi: 10.1038/cddiscovery.2015.9. eCollection 2015. PubMed PMID: 27551444; PubMed Central PMCID: PMC4979471.
