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CUR 61414 (Synonyms: G-856)

Catalog No.GC11217

CUR 61414 est un nouvel inhibiteur de la voie de signalisation Hedgehog puissant et perméable aux cellules (IC50 \u003d 100-200 nM).

Products are for research use only. Not for human use. We do not sell to patients.

CUR 61414 Chemical Structure

Cas No.: 334998-36-6

Taille Prix Stock Qté
5mg
130,00 $US
En stock
10mg
213,00 $US
En stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

IC50: 100-200 nM for hedgehog-induced cellular activity

CUR 61414 is a potent inhibitor of hedgehog-induced cellular activity.

The link between basal cell carcinoma (BCC) and aberrant activation of the Hedgehog (Hh) signaling pathway has been well established in humans and in mouse models.

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].

Clinical trial: So far, no clinical study has been conducted.

Reference:
[1] Williams, J. A.,Guicherit, O.M.,Zaharian, B.I., et al. Identification of a small molecule inhibitor of the hedgehog signaling pathway: Effects on basal cell carcinoma-like lesions. Proceedings of the National Academy of Sciences of the United States of America 100(8), 4616-4621 (2003).

Chemical Properties

Cas No. 334998-36-6 SDF
Synonymes G-856
Chemical Name N-[(3S,5S)-1-(1,3-benzodioxol-5-ylmethyl)-5-(1-piperazinylcarbonyl)-3-pyrrolidinyl]-N-[(3-methoxyphenyl)methyl]-3,3-dimethyl-butanamide
Canonical SMILES O=C(CC(C)(C)C)N([C@H]1C[C@@H](C(N2CCN([H])CC2)=O)N(CC3=CC=C(OCO4)C4=C3)C1)CC5=CC(OC)=CC=C5
Formula C31H42N4O5 M.Wt 550.7
Solubility ≤10mg/ml in ethanol;10mg/ml in DMSO;10mg/ml in dimethyl formamide Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 1.8159 mL 9.0794 mL 18.1587 mL
5 mM 0.3632 mL 1.8159 mL 3.6317 mL
10 mM 0.1816 mL 0.9079 mL 1.8159 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 14 reference(s) in Google Scholar.)

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