Identification | Back Directory | [Name]
Morpholine, 4-(4-phenyl-2-thiazolyl)- | [CAS]
19983-28-9 | [Synonyms]
VPC-14228 VPC-14228 >=98% (HPLC) Morpholine, 4-(4-phenyl-2-thiazolyl)- | [Molecular Formula]
C13H14N2OS | [MDL Number]
MFCD00628805 | [MOL File]
19983-28-9.mol | [Molecular Weight]
246.33 |
Chemical Properties | Back Directory | [Melting point ]
76.0-78.5 °C(Solv: hexane (110-54-3); benzene (71-43-2)) | [Boiling point ]
422.0±55.0 °C(Predicted) | [density ]
1.227±0.06 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO: 20mg/mL, clear | [form ]
Solid | [pka]
4.47±0.50(Predicted) | [color ]
White to light yellow |
Hazard Information | Back Directory | [Description]
VPC-14228 is a specific inhibitor of AR-DBD. It acts by inhibiting both Y594A and Q592A mutants, blocking the interaction of the AR with androgen response elements in the nucleus.. | [Uses]
VPC-14228 is an inhibitor that selectively targets androgen receptor DNA binding domain (AR-DBD). VPC-14228 inhibits the interaction between AR and DNA, thereby blocking AR-mediated transcriptional activation. VPC-14228 does not rely on nuclear localization inhibition, but rather inhibits the activity of full-length AR and splice variant AR-V7 by interfering with AR binding to chromatin. And VPC-14228 has high selectivity for other nuclear receptors such as ER and PR. VPC-14228 can be used in the study of prostate cancer[1][2]. | [References]
[1] Kush Dalal, et al. Selectively targeting the DNA-binding domain of the androgen receptor as a prospective therapy for prostate cancer. J Biol Chem. 2014 Sep 19;289(38):26417-26429. DOI:10.1074/jbc.M114.553818 [2] Bhumireddy A, et al. Design, synthesis, and biological evaluation of phenyl thiazole-based AR-V7 degraders. Bioorg Med Chem Lett. 2022 Jan 1;55:128448. DOI:10.1016/j.bmcl.2021.128448 |
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Company Name: |
Energy Chemical
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Tel: |
021-58432009 400-005-6266 |
Website: |
http://www.energy-chemical.com |
Company Name: |
Merck KGaA
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Tel: |
21-20338288 |
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www.sigmaaldrich.cn |
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