TCRS-417

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].

Product Specifications

CAS Number

[2032123-28-5]

Product Name Alternative

T417

UNSPSC

12352005

Target

DNA/RNA Synthesis; HOXA; NEKs

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage

Applications

COVID-19-immunoregulation

Field of Research

Cancer; Inflammation/Immunology; Neurological Disease

Assay Protocol

https://www.medchemexpress.com/tcrs-417.html

Concentration

10mM

Purity

99.13

Solubility

DMSO : 100 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C(C1=CC(F)=CC=C1)NC2=CC=C(C3=C2C=CC=C3)OCC(NC4=CC=C(C(O)=C4)O)=O

Molecular Formula

C25H19FN2O5

Molecular Weight

446.43

References & Citations

[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.|[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.