Identification | Back Directory | [Name]
CUR 61414 | [CAS]
334998-36-6 | [Synonyms]
CUR 61414 N-[(3S,5S)-1-(1,3-Benzodioxol-5-ylmethyl)-5-(1-piperazinylcarbonyl)-3-pyrrolidinyl]-N-[(3-methoxyphenyl)methyl]-3,3-dimethylbutanamide N-[(3S,5S)-1-(1,3-Benzodioxol-5-ylmethyl)-5-(1-piperazinylcarbonyl)-3-pyrrolidinyl]-N-[(3-methoxyphenyl)methyl]-3,3-dimethyl-benzamide N-[(3S,5S)-1-(1,3-benzodioxol-5-ylmethyl)-5-(piperazine-1-carbonyl)pyrrolidin-3-yl]-N-[(3-methoxyphenyl)methyl]-3,3-dimethylbutanamide Butanamide, N-[(3S,5S)-1-(1,3-benzodioxol-5-ylmethyl)-5-(1-piperazinylcarbonyl)-3-pyrrolidinyl]-N-[(3-methoxyphenyl)methyl]-3,3-dimethyl- | [Molecular Formula]
C31H42N4O5 | [MDL Number]
MFCD20275055 | [MOL File]
334998-36-6.mol | [Molecular Weight]
550.69 |
Chemical Properties | Back Directory | [Melting point ]
35-40°C | [Boiling point ]
714.1±60.0 °C(Predicted) | [density ]
1.24±0.1 g/cm3(Predicted) | [storage temp. ]
Hygroscopic, -20°C Freezer, Under Inert Atmosphere | [solubility ]
DMSO: soluble2mg/mL (clear solution, warmed) | [form ]
powder | [pka]
8.42±0.10(Predicted) | [color ]
white to beige | [Stability:]
Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 2 months. |
Hazard Information | Back Directory | [Description]
CUR 61414 is a potent inhibitor of hedgehog-induced cellular activity (IC50 = 100-200 nM). It binds directly with the pathway activator Smoothened (Ki = 44 nM). CUR 61414 blocks proliferation and induces apoptosis in mouse basal cell carcinoma and causes regression of basaloid lesions triggered by ultraviolet light in mouse skin. | [Chemical Properties]
Pale Yellow Solid | [Uses]
CUR 61414 is a proline derivative as mediator of hedgehog signaling pathways for pharmaceutical and cosmetic uses. CUR 61414 is a Nucleoside analog. CUR 61414 is an antimetabolite antitumor combination Gemcitabine cancer treatment | [in vitro]
previous study found that cur61414 was able to arrest proliferation of basal cells within the bcc-like lesions and induce cells to undergo apoptosis resulting in complete regression of the lesions, without affecting neighboring skin cells [1]. | [in vivo]
the efficacy of cur61414 against basaloid lesions induced when mice were exposed to uv light. these mice were uv irradiated for 6-9 months, producing many microscopic bcc-like basaloid lesions throughout their skin. results showed that the treatment with cur61414 could cause regression of these lesions, as demonstrated by both x-gal staining and histological analyses. moreover, the regression in the cur61414-treated mice seemed to be the result of massive cell death, becuase a significant increase in apoptotic nuclei was seen in basaloid nests after treatment. in addition, no overt toxicity was observed in the skin surrounding the lesions [1]. | [IC 50]
100-200 nm for hedgehog-induced cellular activity | [storage]
Store at -20°C | [References]
1) Williams et al. (2003), Identification of a small molecule inhibitor of the hedgehog signaling pathway: effects on basal cell carcinoma-like lesions; Proc.Natl. Acad. Sci. USA, 100 4616
2) Tang et al. (2011), Targeting superficial or nodular Basal cell carcinoma with topically formulated small molecule inhibitor of smoothened; Clin. Cancer Res., 17 3378
3) Athar et al. (2004), Inhibition of smoothened signaling prevents ultraviolet B-induced basal cell carcinomas through regulation of Fas expression and apoptosis; Sci. Signal., 64 7545 |
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BOC Sciences
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https://www.bocsci.com |
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