2032123-28-5
Chemical Structure
TCRS-417
Synonym(s): T417
- CAS No.: 2032123-28-5
- Formula:C25H19FN2O5
- Molecular Weight:446.43
InChIKey: FAUNPVFPOMPBQA-UHFFFAOYSA-N
SMILES: O=C(C1=CC(F)=CC=C1)NC2=CC=C(C3=C2C=CC=C3)OCC(NC4=CC=C(C(O)=C4)O)=O
Biological Activity: TCRS-417 (T417) is a small-molecular inhibitor for PBX1. TCRS-417 can directly block PBX1-binding to DNA (IC50 = 6.58 μM), and affects PBX1 transcription. TCRS-417 is able to hammer out the stemness traits of Carboplatin (HY-17393)-resistant (CR) cells to revert to a differentiated status through tacking PBX1 signaling cascade. TCRS-417 significantly suppresses self-renewal and proliferation of cancer cells expressing high levels of PBX1. TCRS-417 can decrease the mRNA levels of FOXM1, NEK2, and E2F2 in cancer cell lines. TCRS-417 is selectively toxic against chr1q-amp myeloma and solid tumor cells[1][2][3][4].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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TCRS-417 | 99.13% | TCRS-417 (T417) is a small-molecular inhibitor for PBX1. TCRS-417 can directly block PBX1-binding to DNA (IC50 = 6.58 μM), and affects PBX1 transcription. TCRS-417 is able to hammer out the stemness traits of Carboplatin (HY-17393)-resistant (CR) cells to revert to a differentiated status through tacking PBX1 signaling cascade. TCRS-417 significantly suppresses self-renewal and proliferation of cancer cells expressing high levels of PBX1. TCRS-417 can decrease the mRNA levels of FOXM1, NEK2, and E2F2 in cancer cell lines. TCRS-417 is selectively toxic against chr1q-amp myeloma and solid tumor cells. | ||||||||||||||||||||
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- [1]. Small molecule compounds targeting pbx1 transcriptional complex.WO2016172437.
- [2]. Yao-An Shen, et al., Abstract 1966: A novel small-molecule compound targeting PBX1-DNA interaction impedes cancer cell survival and carboplatin resistance. Cancer Res 1 July 2018; 78 (13_Supplement): 1966.
- [3]. Trasanidis, N., et al., (2022). Systems medicine dissection of chr1q-amp reveals a novel PBX1-FOXM1 axis for targeted therapy in multiple myeloma. Blood, 139(13), 1939–1953. [Content Brief]
- [4]. Shen, Y. A., et al., (2021). Development of small molecule inhibitors targeting PBX1 transcription signaling as a novel cancer therapeutic strategy. iScience, 24(11), 103297. [Content Brief]
Keywords
