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T417

Chemical Structure : T417

CAS No.: 2032123-28-5

T417 (PBX1 inhibitor T417, TCRS-417)

Catalog No.: PC-72727Not For Human Use, Lab Use Only.

T417 (PBX1 inhibitor T417, TCRS-417) is a novel small molecule compound capable of docking to the interface between PBX1 and its cognate DNA target sequence, potently interferes with the PBX1-DNA interaction with IC50 of 6.58 uM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

T417 (PBX1 inhibitor T417, TCRS-417) is a novel small molecule compound capable of docking to the interface between PBX1 and its cognate DNA target sequence, potently interferes with the PBX1-DNA interaction with IC50 of 6.58 uM.
T417 destabilizes the PBX1-DNA complex, T417 competition of PBX1 protein binding to immobilized PBX1 consensus DNA with IC50 of 5 uM.
T417 selectively suppresses the formation of the PBX1/MEIS2 transcriptional complex, inhibits PBX1 transcriptional activity by hindering its binding to the promoter regions of PBX1 downstream target genes.
T417 (PBX1 inhibitor T417) selectively inhibits carboplatin-resistant tumor cells, and suppresses tumor growth in xenograft models of carboplatin-resistant cancer models.
T417 also is selectively toxic against chr1q-amplified myeloma and solid tumour cells.

Physicochemical Properties

M.Wt 446.434
Formula C25H19FN2O5
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-(4-(2-((3,4-dihydroxyphenyl)amino)-2-oxoethoxy)naphthalen-1-yl)-3-fluorobenzamide

References

1. Shen YA, et al. iScience. 2021 Oct 15;24(11):103297. 

2. Trasanidis N, et al. Blood. 2022 Jan 11:blood.2021014391.

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