685141-23-5
Chemical Structure
BXL0124
- CAS No.: 685141-23-5
- Formula:C32H44F6O4
- Molecular Weight:606.68
InChIKey: VSOWXEHVBCDXAY-GEJQTTJQSA-N
SMILES: C[C@@]12[C@](CC[C@]2([H])[C@H](CCCC(C)(O)C)CC#CC(C(F)(F)F)(O)C(F)(F)F)([H])/C(CCC1)=C/C=C3C([C@H](C[C@@H](C\3)O)O)=C
Biological Activity: BXL0124 is an orally effective CD44 inhibitor and Notch signaling pathway inhibitor. BXL0124 has a vitamin D receptor-dependent mechanism and can downregulate the expression of CD44, Notch1/2/3, HES1, OCT4, LAMA5, JAG1, JAG2, NF-κB and DLL1. BXL0124 inhibits c-Myc expression and the levels of phosphorylated ERK, AKT, ErbB2, reduces the level of activated Notch1 receptor and its nuclear localization, decreases the mRNA and protein levels of Jagged-1 and Jagged-2, and inhibits the STAT3 signaling pathway by reducing the formation of the CD44-STAT3-JAK2 complex, while also inhibiting the transcriptional activity of the CD44 promoter in a p53-dependent manner. BXL0124 can induce myoepithelial differentiation and inhibit the self-renewal of cancer stem cell-like cells, cancer cell proliferation, invasion, and growth. BXL0124 can be used in research related to triple-negative breast cancer, basal-like breast cancer, ErbB2-overexpressing mammary tumorigenesis, and breast cancer[1][2][3][4][5].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
|
|
BXL0124 | BXL0124 is an orally effective CD44 inhibitor and Notch signaling pathway inhibitor. BXL0124 has a vitamin D receptor-dependent mechanism and can downregulate the expression of CD44, Notch1/2/3, HES1, OCT4, LAMA5, JAG1, JAG2, NF-κB and DLL1. BXL0124 inhibits c-Myc expression and the levels of phosphorylated ERK, AKT, ErbB2, reduces the level of activated Notch1 receptor and its nuclear localization, decreases the mRNA and protein levels of Jagged-1 and Jagged-2, and inhibits the STAT3 signaling pathway by reducing the formation of the CD44-STAT3-JAK2 complex, while also inhibiting the transcriptional activity of the CD44 promoter in a p53-dependent manner. BXL0124 can induce myoepithelial differentiation and inhibit the self-renewal of cancer stem cell-like cells, cancer cell proliferation, invasion, and growth. BXL0124 can be used in research related to triple-negative breast cancer, basal-like breast cancer, ErbB2-overexpressing mammary tumorigenesis, and breast cancer. | |||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
References
- [1]. Shan NL, et al. Vitamin D compounds inhibit cancer stem-like cells and induce differentiation in triple negative breast cancer. The Journal of steroid biochemistry and molecular biology. 2017 Oct;173:122-129.
- [2]. So JY, et al. HES1-mediated inhibition of Notch1 signaling by a Gemini vitamin D analog leads to decreased CD44(+)/CD24(-/low) tumor-initiating subpopulation in basal-like breast cancer. The Journal of steroid biochemistry and molecular biology. 2015 Apr;148:111-21.
- [3]. Lee HJ, et al. Gemini vitamin D analog suppresses ErbB2-positive mammary tumor growth via inhibition of ErbB2/AKT/ERK signaling. The Journal of steroid biochemistry and molecular biology. 2010 Jul;121(1-2):408-12.
- [4]. So JY, et al. Targeting CD44-STAT3 signaling by Gemini vitamin D analog leads to inhibition of invasion in basal-like breast cancer. PloS one. 2013;8(1):e54020.
- [5]. So JY, et al. A novel Gemini vitamin D analog represses the expression of a stem cell marker CD44 in breast cancer. Molecular pharmacology. 2011 Mar;79(3):360-7.
