PKCα/β inhibitor Cmpd 1 | PKCα/β inhibitor

Chemical Structure : PKCα/β inhibitor Cmpd 1

CAS No.: 1046787-18-1

PKCα/β inhibitor Cmpd 1 (PKC-IN-1)

Catalog No.: PC-63224Not For Human Use, Lab Use Only.

PKCα/β inhibitor Cmpd 1 is a potent and selective inhibitor of Protein Kinase C (PKC) family members PKCα and PKCβ with IC50 of 2 nM and 11 nM, respectively.

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5 mg	$298	In stock
10 mg	$478	In stock
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Biological Activity

PKCα/β inhibitor Cmpd 1 is a potent and selective inhibitor of Protein Kinase C (PKC) family members PKCα and PKCβ with IC50 of 2 nM and 11 nM, respectively.

PKCα/β inhibitor Cmpd 1 shows moderate activity against PKCθ (IC50 28 nM) and PKCγ (IC50 96 nM), >40-fold selectivity over other PKC family members.

PKCα/β inhibitor Cmpd 1inhibits production of IL-8 in response to the DAG mimic and PKC activator phorbol 12-myristate 13-acetate (PMA) with IC50 of 26 nM.

PKCα/β inhibitor Cmpd 1 inhibits PKC in vitro in PKC activity assays using glomerular source material.

PKCα/β inhibitor Cmpd 1 (100 mpk/day) decreases food consumption and causes weight loss in ZSF1 obese animals.

Physicochemical Properties

M.Wt	500.623
Formula	C25H37FN8O2
Appearance	Solid
CAS No.
Storage	Solide Powder -20 °C 12 Months; 4°C 6 Months	In Solvent -80 °C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	((2S,5R)-2,5-dimethyl-4-((tetrahydro-2H-pyran-4-yl)methyl)piperazin-1-yl)(3-((5-fluoro-2-methylpyrimidin-4-yl)amino)-6,6-dimethyl-4,6-dihydropyrrolo[3,4-c]pyrazol-5(1H)-yl)methanone

References

1. Wang J, et al. Sci Rep. 2023 Oct 7;13(1):16919.
2. Patent WO2021113766 (Cmpd A).

PKCα/β inhibitor Cmpd 1 (PKC-IN-1)

Biological Activity

Physicochemical Properties

References

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