FzM1 is a negative allosteric modulator (NAM) of Frizzled receptor FZD4. FzM1 reduces WNT5A-dependent WNT responsive element (WRE) activity (log EC50inh=−6.2). FzM1 binds to an allosteric binding site located in intracellular loop 3 (ICL3) of FZD4 and alters the conformation of the receptor, ultimately inhibiting the WNT/β-catenin cascade[1].
分子量
360.43
Formula
C21H16N2O2S
CAS 号
1680196-54-6
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Gennaro Riccio, et al. A Negative Allosteric Modulator of WNT Receptor Frizzled 4 Switches into an Allosteric Agonist. Biochemistry. 2018 Feb 6;57(5):839-851.
FzM1 is a negative allosteric modulator (NAM) of Frizzled receptor FZD4. FzM1 reduces WNT5A-dependent WNT responsive element (WRE) activity (log EC50inh=−6.2). FzM1 binds to an allosteric binding site located in intracellular loop 3 (ICL3) of FZD4 and alters the conformation of the receptor, ultimately inhibiting the WNT/β-catenin cascade[1].
分子量
360.43
Formula
C21H16N2O2S
CAS 号
1680196-54-6
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Gennaro Riccio, et al. A Negative Allosteric Modulator of WNT Receptor Frizzled 4 Switches into an Allosteric Agonist. Biochemistry. 2018 Feb 6;57(5):839-851.
FzM1 is a negative allosteric modulator (NAM) of Frizzled receptor FZD4. FzM1 reduces WNT5A-dependent WNT responsive element (WRE) activity (log EC50inh=−6.2). FzM1 binds to an allosteric binding site located in intracellular loop 3 (ICL3) of FZD4 and alters the conformation of the receptor, ultimately inhibiting the WNT/β-catenin cascade[1].
分子量
360.43
Formula
C21H16N2O2S
CAS 号
1680196-54-6
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Gennaro Riccio, et al. A Negative Allosteric Modulator of WNT Receptor Frizzled 4 Switches into an Allosteric Agonist. Biochemistry. 2018 Feb 6;57(5):839-851.
Hematein is a oxidation product of hematoxylin acted as a dye[1]. Hematein is an allosteric casein kinase II inhibitor with an IC50 of 0.74 μM. Hematein inhibits Akt/PKB Ser129 phosphorylation, the Wnt/TCF pathway and increases apoptosis in lung cancer cells[2].
IC50 & Target[2]
CKII
0.74 μM (IC50)
Akt
Wnt
体外研究 (In Vitro)
Hematein (10-100 μM; 14 days) inhibits cells growth in A427 lung cancer cells[1]. Hematein (50 and 100 μM; 48 hours) induces apoptosis in A427 lung cancer cells[1]. Hematein (50 and 100 μM; 48 hours) inhibits CK2-specific Akt phosphorylation[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay[1]
Cell Line:
A427 (HTB-53) cell line
Concentration:
10-100 μM
Incubation Time:
14 days
Result:
Inhibited cells growth.
Apoptosis Analysis[1]
Cell Line:
A427 (HTB-53) cell line
Concentration:
50 and 100 μM
Incubation Time:
48 hours
Result:
Induced apoptosis in A427 lung cancer cells.
Western Blot Analysis[1]
Cell Line:
A427 (HTB-53) cell line
Concentration:
50 and 100 μM
Incubation Time:
48 hours
Result:
Inhibited CK2-specific Akt phosphorylation.
体内研究 (In Vivo)
Hematein (intraperitoneal injections; 50 mg/kg; twice a week for 6 weeks) inhibits tumor growth in A427 lung cancer cell xenografts[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
Female athymic BALB/c nude mice (6-week-old) [1]
Dosage:
50 mg/kg
Administration:
Intraperitoneal injections; twice a week for 6 weeks
Result:
Inhibited tumor growth in A427 lung cancer cell xenografts.
分子量
300.26
Formula
C16H12O6
CAS 号
475-25-2
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Shirai, K., & Matsuoka, M. (1996). Structure and properties of hematein derivatives. Dyes and Pigments, 32(3), 159–169.
[2]. Hung MS, et al. Hematein, a casein kinase II inhibitor, inhibits lung cancer tumor growth in a murine xenograftmodel.Int J Oncol. 2013 Nov;43(5):1517-22.