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ChemicalBook Product Catalog Biochemical Engineering Biochemical Reagents Agonist Inhibitors APTO-253

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APTO-253 NEW

$36.00 1mg

$50.00 2mg

$73.00 5mg

Min. Order
Purity99.43%
Cas No916151-99-0
Supply Ability10g
Update time2025-05-01

TargetMol Chemicals Inc.

TargetMol Chemicals Inc.

VIP2Y

United States

United States

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Chemical Properties

Product Name	APTO-253
CAS No	916151-99-0
EC-No
Min. Order
Purity	99.43%
Supply Ability	10g
Release date	2025/05/01

Product Introduction

Bioactivity

Name	APTO-253
Description	APTO-253 (LOR-253) inhibits c-Myc expression, stabilizes G-quadruplex DNA, and induces cell cycle arrest and apoptosis in acute myeloid leukemia cells. APTO-253 mediates anticancer activity through the induction of the KLF4 tumor suppressor.
In vitro	APTO-253 (5 μM) induces KLF4 expression and enhances apoptosis induced by NSC 119875 in both SKOV3 and OVCAR3 cells. APTO-253 (5 μM) also leads to G1 phase arrest and reduces S and G2/M phase cells in SKOV3 and OVCAR3 cells [1]. APTO-253 is cytotoxic to Raji and Raji/253R cell lines (IC50s: 105 nM and 1387 nM). APTO-253 (0.5 μM) also causes DNA damage in Raji cells. BRCA1/2 deficient cells are hypersensitive to APTO-253. ABCG2 overexpressed HEK-293 cells are resistant to APTO-253 and inhibition of ABCG2 reverses resistance to APTO-253 in Raji/253R [2]. APTO-253 suppresses the proliferation of acute myeloid leukemia (AML) cell lines and various forms of lymphoma cell lines (IC50s: 57 nM to 1.75 μM). APTO-253 (500 nM) also causes G0/G1 cell cycle arrest, induces apoptosis, and down-regulates MYC RNA and protein expression in AML lines. APTO-253 (500 nM) leads to DNA damage response pathways in MV4-11 cells. Furthermore, APTO-253 is a potent stabilizer of G-quadruplex (G4) motifs and demonstrates the greatest propensity for stabilizing the MYC G4 sequences.
Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
Solubility Information	DMSO : 32.33 mg/mL (88 mM), Sonication is recommended.
Keywords	Myc \| LT253 \| LT 253 \| LOR253 \| LOR 253 \| Krüppel-like factor \| KLF \| Inhibitor \| inhibit \| c-Myc \| cMyc \| APTO-253 \| APTO253 \| APTO 253 \| Apoptosis
Inhibitors Related	Stavudine \| 5-Fluorouracil \| Acetylcysteine \| Myricetin \| Sodium 4-phenylbutyrate \| L-Ascorbic acid \| Dextran sulfate sodium salt (MW 4500-5500) \| L-Glutamic acid \| Metronidazole \| Tributyrin \| L-Ascorbic acid sodium salt \| Salicylic acid
Related Compound Libraries	Failed Clinical Trials Compound Library \| Bioactive Compound Library \| Pain-Related Compound Library \| Anti-Obesity Compound Library \| Anti-Cancer Clinical Compound Library \| Drug Repurposing Compound Library \| Inhibitor Library \| Immunology/Inflammation Compound Library \| Bioactive Compounds Library Max \| Wnt/Hedgehog/Notch Compound Library \| Anti-Cancer Drug Library \| Anti-Cancer Active Compound Library

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