APTO-253 (hydrochloride)

APTO-253 (LOR-253) hydrochloride is a small molecule that inhibits c-Myc expression, stabilizes G-quadruplex DNA and induces cell cycle arrest and apoptosis in acute myeloid leukemia cells. APTO-253 hydrochloride mediates anticancer activity via induction of Kruppel-like factor 4 (KLF4) tumor suppressor. APTO-253 hydrochloride exhibits antiarthritic activity[1].

Product Specifications

CAS Number

[1691221-67-6]

Product Name Alternative

LOR-253 (hydrochloride) ; LT-253 (hydrochloride)

UNSPSC

12352005

Target

C-Myc

Type

Reference compound

Related Pathways

Apoptosis

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/apto-253-hydrochloride.html

Smiles

CC(NC1=C2C=C(F)C=C1)=C2C3=NC4=C5C=CC=NC5=C6N=CC=CC6=C4N3

Molecular Formula

C22H14FN5

Molecular Weight

367.38

References & Citations

[1]Local A, et al. APTO-253 Stabilizes G-quadruplex DNA, Inhibits MYC Expression, and Induces DNA Damage in Acute Myeloid Leukemia Cells. Mol Cancer Ther. 2018 Jun;17 (6) :1177-1186. [Content Brief]|[2]Haruka Tsuchiya, et al. Parsing multiomics landscape of activated synovial fibroblasts highlights drug targets linked to genetic risk of rheumatoid arthritis. Ann Rheum Dis. 2020 Nov2; annrheumdis-2020-218189.|[3]Hongying Zhang, et al. Inhibition of c-Myc By Apto-253 As an Innovative Therapeutic Approach to Induce Cell Cycle Arrest and Apoptosis in Acute Myeloid Leukemia. Blood 2016 128:1716.