b-Catenin/Tcf Inhibitor III, iCRT3

货号： 219332-10MG      产品名称： b-Catenin/Tcf Inhibitor III, iCRT3   品牌： Merck 规格： *** 3周到货 生化实验

β-Catenin/Tcf Inhibitor III, iCRT3
2-(((2-(4-Ethylphenyl)-5-methyl-1,3-oxazol-4-yl)methyl)sulfanyl)-N-(2-phenylethyl)acetamide, Inhibitor of β-Catenin Responsive Transcription, Wnt Pathway Inhibitor VIII, C3
A cell-permeable oxazole compound that acts as a selective CRT (β-catenin responsive transcription) inhibitor (IC50 = 8.2 nM against Wnt3a-dependent SuperTopFlash STF16-luc reporter activity in HEK293 cultures) by interfering with β-cat-TCF4 interaction via direct β-catenin (β-cat) binding, while exhibiting much reduced activity against Hedgehog, Jak/Stat, or Notch signaling pathway-dependent transcription activation. Effectively inhibits cellular expression of CRT target genes, including WISP1, AXN2, and CYCD1, in a dose-dependent manner (25 to 75 µM), and selectively inhibits the proliferation of HCT116 (75 µM), HT29 (75 µM), and several primary human colon cancer cultures (6.25 to 100 µg/ml; average IC50 ~36 µg/ml) that require sustained Wnt/CRT activity for survival.
产品信息
Form  Tan powder
Molar mass  394.5
Protect from Light  是的
Packaged under inert gas  是的
Purity  ≥95% by HPLC
Solubility  DMSO
Chemical formula  C23H26N2O2S
商店和运输信息
Storage  -20°C
Ship  Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Standard Handling

-20°C

b-Catenin/Tcf Inhibitor II, PKF118-310

货号： 219331-10MG      产品名称： b-Catenin/Tcf Inhibitor II, PKF118-310   品牌： Merck 规格： *** 3周到货 生化实验

β-Catenin/Tcf Inhibitor II, PKF118-310
1,6-Dimethylpyrimido[5,6-e][1,2,4]triazine-5,7-dione, Wnt Pathway Inhibitor X
A synthetic cell-permeable actinobacteria pyrimidotriazine-dione that selectively disrupts β-catenin-Tcf4 interaction (IC50 = 0.8 µM in cell-free binding assays) and inhibits β-catenin-regulated cellular transcription activity (IC50 = 0.3 µM in HCT116-based reporter assays). PKF118-310 is demonstrated to reverse β-catenin, but not siamois, mRNA-induced ventral body axis formation in Xenopus embryos, while direct tumor site injection (1 mg/kg/0.5 wk) in HepG2 xenograph mice is shown to increase the number of apoptotic cells and decrease the expression of β-catenin target genes (cyclin D1, c-Myc, survivin) in the tumor mass, resulting in an effective tumor growth retardation (by ~60% after a 4-wk treatment period) in vivo.
产品信息
Form  Dark yellow solid
Molar mass  193.2
Protect from Light  是的
Packaged under inert gas  是的
Purity  ≥95% by HPLC
Solubility  DMSO
Chemical formula  C7H7N5O2
商店和运输信息
Storage  +2°C to +8°C
Ship  Ambient Temperature Only
Standard Handling

2°C – 8°C

b-Catenin/Tcf Inhibitor V, BC21

货号： 219334-10MG      产品名称： b-Catenin/Tcf Inhibitor V, BC21   品牌： Merck 规格： *** 3周到货 生化实验

β-Catenin/Tcf Inhibitor V, BC21
Copper, di-µ-chlorobis[1-[(1-piperidinyl-κN)methyl]-2-naphthalenolato-κO]di-(9Cl), Wnt Pathway Inhibitor XV
A cell-permeable dimeric copper complex that competitively binds β-catenin and disrupts β-catenin/Tcf4 interaction reversibly (IC50 = 5.0 µM), and acts as a Wnt signaling inhibitor. Shown to induce preferential growth arrest in β-catenin overexpressing HCT116 colon cancer and HEK293 cells (≤ 10 µM), and downregulate mRNA expressions of c-Myc and cyclin D1. Reported to inhibit PP2C and proteasomal activities at higher concentrations (~50 µM).
产品信息
Form  Dark brown solid
Molar mass  678.6
Protect from Light  是的
Packaged under inert gas  是的
Purity  ≥95% by HPLC
Solubility  DMSO
Chemical formula  C32H36Cl2Cu2N2O2
CAS number  691005-38-6
商店和运输信息
Storage  +2°C to +8°C
Ship  Ambient Temperature Only
Standard Handling

2°C – 8°C