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Germinone A

Catalog No. T9007 CAS T9007

Synonyms: 3-Methyl-5-((3-nitro-[1,1'-biphenyl]-4-yl)oxy)furan-2(5H)-one

Germinone A (3-Methyl-5-((3-nitro-[1,1'-biphenyl]-4-yl)oxy)furan-2(5H)-one) is a novel potent agonist of HTL/KAI2, stimulating activity for Arabidopsis seed germination, has antitumor activity in multiple types of carcinomas.

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Germinone A, CAS T9007

Pack Size	Availability	Price/USD
1 mg	In stock	$ 133.00
5 mg	In stock	$ 302.00
10 mg	In stock	$ 453.00
25 mg	In stock	$ 747.00
50 mg	In stock	$ 1,050.00
100 mg	In stock	$ 1,420.00
500 mg	In stock	$ 2,830.00
1 mL * 10 mM (in DMSO)	In stock	$ 297.00

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Purity: 99.97%

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Description

In vitro

CRT0066101 suppressed the proliferation and migration of four bladder cancer cell lines in vitro.?CRT0066101 blocked tumor growth in a mouse flank xenograft model of bladder cancer.?To further assess the role of PKD in bladder carcinoma, examined the three PKD isoforms and found that PKD2 was highly expressed in eight bladder cancer cell lines and in urothelial carcinoma tissues from the TCGA database,?and that short hairpin RNA (shRNA)-mediated knockdown of PKD2 dramatically reduced bladder cancer growth and invasion in vitro and in vivo, suggesting that the effect of the compound in bladder cancer is mediated through inhibition of PKD2.?This notion was corroborated by demonstrating that the levels of phospho-PKD2 were markedly decreased in CRT0066101-treated bladder tumor explants.?CRT0066101 treatment or PKD2 silencing arrested bladder cancer cells at the G2/M phase, the arrest being accompanied by decreases in the levels of cyclin B1, CDK1 and phospho-CDK1 (Thr161) and increases in the levels of p27Kip1 and phospho-CDK1 (Thr14/Tyr15).?Moreover, CRT0066101 downregulated the expression of Cdc25C, which dephosphorylates/activates CDK1, but enhanced the activity of the checkpoint kinase Chk1, which inhibits CDK1 by phosphorylating/inactivating Cdc25C.?CRT0066101 was found to elevate the levels of Myt1, Wee1, phospho-Cdc25C (Ser216), Gadd45α, and 14-3-3 proteins, all of which reduce the CDK1-cyclin B1 complex activity.?CRT0066101 suppresses bladder cancer growth by inhibiting PKD2 through induction of G2/M cell cycle arrest, leading to the blockade of cell cycle progression[1].

Synonyms	3-Methyl-5-((3-nitro-[1,1'-biphenyl]-4-yl)oxy)furan-2(5H)-one
Molecular Weight	311.29
Formula	C17H13NO5
CAS No.	T9007

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 22.5 mg/mL (72.28 mM)

References and Literature

1. Li Q Q , Hsu I , Sanford T , et al. Protein kinase D inhibitor CRT0066101 suppresses bladder cancer growth in vitro and xenografts via blockade of the cell cycle at G2/M[J]. Cellular & Molecular Life Sciences, 2017. 2. Borges S , EA Perez, EA Thompson, et al. Effective Targeting of Estrogen Receptor-Negative Breast Cancers with the Protein Kinase D Inhibitor CRT0066101.[J]. Molecular Cancer Therapeutics, 2015, 14(6).

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library NO PAINS Compound Library Bioactive Compound Library Bioactive Compounds Library Max Anti-Cancer Compound Library

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Keywords

Germinone A T9007 Others 3-Methyl-5-((3-nitro-[1,1'-biphenyl]-4-yl)oxy)furan-2(5H)-one inhibitor inhibit

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