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Germinone A

Germinone A

产品编号 T9007   CAS T9007
别名: 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) 是一种新型强效 HTL/KAI2 激动剂,可刺激拟南芥种子萌发,在多种癌症中具有抗肿瘤活性。

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Germinone A Chemical Structure
Germinone A, CAS T9007
规格 价格/CNY 货期 数量
1 mg ¥ 1,300 现货
5 mg ¥ 2,920 现货
10 mg ¥ 4,320 现货
25 mg ¥ 6,890 现货
50 mg ¥ 9,330 现货
100 mg ¥ 12,500 现货
500 mg ¥ 25,200 现货
1 mL * 10 mM (in DMSO) ¥ 2,760 现货
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
Paclitaxel限时半价
产品目录号及名称: Germinone A (T9007)
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纯度: 99.97%
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生物活性
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存储 & 溶解度
参考文献
产品描述 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.
体外活性 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].
别名 3-Methyl-5-((3-nitro-[1,1'-biphenyl]-4-yl)oxy)furan-2(5H)-one
分子量 311.29
分子式 C17H13NO5
CAS No. T9007

存储

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

溶解度

DMSO: 22.5 mg/mL (72.28 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.2124 mL 16.0622 mL 32.1244 mL 80.311 mL
5 mM 0.6425 mL 3.2124 mL 6.4249 mL 16.0622 mL
10 mM 0.3212 mL 1.6062 mL 3.2124 mL 8.0311 mL
20 mM 0.1606 mL 0.8031 mL 1.6062 mL 4.0155 mL
50 mM 0.0642 mL 0.3212 mL 0.6425 mL 1.6062 mL

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TargetMol Library Books参考文献

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).

相关化合物库

该产品包含在如下化合物库中:
抗癌活性化合物库 NO PAINS 化合物库 经典已知活性库 已知活性化合物库 抗癌化合物库

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母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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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 inhibitor inhibit

 

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