| Identification | Back Directory | [Name]
Porcupine-IN-1 | [CAS]
2036044-77-4 | [Synonyms]
CS-2802
PORCN-IN-1
Porcupine-IN-1
Porcn inhibitor 1
9H-Carbazole-2-carboxamide, N-[(3-fluoro-2'-methyl[2,4'-bipyridin]-5-yl)methyl]- | [Molecular Formula]
C25H19FN4O | [MOL File]
2036044-77-4.mol | [Molecular Weight]
410.44 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
DMF: 10 mg/ml; DMSO: 10 mg/ml; DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml; Ethanol: slightly soluble | [form ]
A crystalline solid | [color ]
White to off-white |
| Hazard Information | Back Directory | [Description]
Porcupine-IN-1 is an inhibitor of the Wnt and hedgehog signaling pathways (IC50s = 0.5 and 71 nM, respectively, in cell-based reporter assays). It inhibits secretion of Wnt3A from Wnt3A-transfected HEK293T cells when used at a concentration of 0.1 μM, indicating inhibition of porcupine, an enzyme that catalyzes palmitoylation of Wnt proteins. | [Uses]
Porcupine-IN-1, is a potent porcupine inhibitor with an IC50 of 0.5±0.2 nM. | [in vivo]
Porcn-IN-1 demonstrates moderate clearance under the treatment of human liver microsomes (57 mL/min/kg) and rat liver microsomes (24 mL/min/kg). It exhibits high clearance when treated with mouse microsomes (109 mL/min/kg)[1]. | [References]
[1] ZHIXIANG XU . Design, synthesis, and evaluation of novel porcupine inhibitors featuring a fused 3-ring system based on the ‘reversed’ amide scaffold[J]. Bioorganic & Medicinal Chemistry, 2016, 24 22: Pages 5861-5872. DOI: 10.1016/j.bmc.2016.09.041
[2] HAIKUO MA . Discovery and characterization of a potent Wnt and hedgehog signaling pathways dual inhibitor[J]. European Journal of Medicinal Chemistry, 2018, 149: Pages 110-121. DOI: 10.1016/j.ejmech.2018.02.034 |
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| Company Name: |
Cckinase, Inc.
|
| Tel: |
+1 (732)236-3202 |
| Website: |
www.cckinase.com |
| Company Name: |
Energy Chemical
|
| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
|