VPC-14337 is an nhibitor of the transcriptional activity of full-length/splice variant Ars.
CAS Number: 3546-41-6
Molecular Weight: 1151.39
Chemical Name: (E)-2-(2-(2,5-dimethyl-1-phenyl-1H-pyrrol-3-yl)vinyl)-6-(dimethylamino)-1-methylquinolin-1-ium 4,4'-methylenebis(3-hydroxy-2-naphthoate)
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Soluble in DMSO
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥360 days if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
VPC-14337 (0-500 nM) inhibits proliferation of MCF-7 (luminal), MDA-MB-231 (claudin-low), MDA-MB-468 (basal-like) and SkBr3 (HER2-OE) cells in a dose-dependent manner, with IC50 value of 1170±105.0 nM against MDA-MB-231 cell line. VPC-14337 significantly inhibits self-renewal and proliferation of BCSCs, and suppresses BCSC population with a distinct phenotype. VPC-14337 significantly decreases average expression levels of FZD1, FZD10, WNT1, WNT7B, CTNNB1, MYC, and LRP5 at transcriptional level. Moreover, VPC-14337 also efficiently down-regulates the expression of other stemness genes including ALDH1, CD44 and ABCG2. VPC-14337 blocks colon cancer cell growth in vitro in a dose-dependent manner with great differences in the inhibitory concentration (IC50), ranging from 0.6 to 65 μM for colon cancer cells with mutations in WNT signaling. VPC-14337 decreases messenger RNA (mRNA) and protein levels of known WNT target genes as c-MYC and thereby led to the induction of p21. VPC-14337 ultimately inhibits Wnt signalling despite its lack of efficacy on CK1. VPC-14337 imposes specific toxicity on cardiac fibroblasts in ischemia (IC50=9.5 nM). The cytotoxic effect of VPC-14337 on cardiac fibroblasts specifically under glucose- and glutamine-deficient condition.
In the xenograft model, VPC-14337 (500 nM)-pretreatment strongly delays tumor size and tumor weight, and the tumor volume is markedly decreased.
- In the xenograft model, VPC-14337 (500 nM)-pretreatment strongly delays tumor size and tumor weight, and the tumor volume is markedly decreased.
- Wiegering A, et al. The impact of pyrvinium pamoate on colon cancer cell viability. Int J Colorectal Dis. 2014 Oct;29(10):1189-98.
- Venerando A, et al. Pyrvinium pamoate does not activate protein kinase CK1, but promotes Akt/PKB down-regulation and GSK3 activation. Biochem J. 2013 May 15;452(1):131-7.
Products are for research use only. Not for human use.
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