Chemical Structure : Prostetin-12k
CAS No.:
2375591-69-6
Prostetin-12k
(Prostetin/12k)
Catalog No.: PC-23624Not For Human Use, Lab Use Only.
Prostetin/12k is a highly potent, blood-brain barrier-penetrant inhibitor of mitogen-activated protein kinase kinase kinase kinase (MAP4K) family with IC50 of 0.3 nM for HGK (MAP4K4) and 23.7 nM for MLK3.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
Prostetin/12k is a highly potent, blood-brain barrier-penetrant inhibitor of mitogen-activated protein kinase kinase kinase kinase (MAP4K) family with IC50 of 0.3 nM for HGK (MAP4K4) and 23.7 nM for MLK3.
Prostetin/12k rescues cyclopiazonic acid (CPA)-induced neurodegeneration with EC50 of 0.1 uM in motor neuron survival assay.
Prostetin/12k has IC50 of 0.3 nM for HGK in cell-free radiolabeled ATP assays.
Prostetin/12k inhibits MLK3 with IC50 of 23.7 nM, potently inhibits MAP4Ks MINK1, KHS, HGK, GLK, and GCK.
Prostetin/12k significantly and dose-dependently decreased TNFα secretion in LPS-stimulated microglia with EC50 of 0.47 uM.
Physicochemical Properties
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M.Wt
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446.98
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Formula
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C26H27ClN4O
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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2-(4-(4-(3-(3-chlorophenyl)-1H-pyrrolo[2,3-b]pyridin-5-yl)benzyl)piperazin-1-yl)ethan-1-ol
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References
1. Bos PH, et al. Cell Chem Biol. 2019 Dec 19;26(12):1703-1715.e37.
2. Moreno R, et al. Eur J Med Chem. 2023 Sep 5;257:115511.
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