APTO-253 hydrochloride
Based on 21 publication(s) in Google Scholar
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.
For research use only. We do not sell to patients.
- CAS No.: 1691221-67-6
- Formula: C22H14FN5
- Molecular Weight:367.38
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications Citing Use of MedChemExpress (MCE) APTO-253 hydrochloride
More- Blood. 2024 Aug 16:blood.2023023644. [Abstract]
- Ann Rheum Dis. 2021 Apr;80(4):440-450. [Abstract]
- Nat Commun. 2023 Sep 2;14(1):5360. [Abstract]
- Nat Commun. 2019 Sep 25;10(1):4369. [Abstract]
- Adv Sci (Weinh). 2025 Mar 24:e2408992. [Abstract]
- Leukemia. 2025 Sep;39(9):2163-2173. [Abstract]
- J Transl Med. 2024 Oct 10;22(1):922. [Abstract]
- Cell Rep. 2026 Mar 24;45(4):117201. [Abstract]
- J Environ Sci. 2025 Nov 28.
- JCI Insight. 2022 Aug 22;7(16):e160688. [Abstract]
- PLoS Pathog. 2025 May 12;21(5):e1013166. [Abstract]
- Int Immunopharmacol. 2023 Jul:120:110425. [Abstract]
- FASEB J. 2025 May 31;39(10):e70613. [Abstract]
- Mol Cell Biochem. 2021 Apr;476(4):1741-1749. [Abstract]
- J Immunol. 2025 Aug 7:vkaf170. [Abstract]
- J Diabetes Res. 2021 Sep 15:2021:7945117. [Abstract]
- Neurotox Res. 2020 Dec;38(4):967-978. [Abstract]
- Genes (Basel). 2021 Apr 8;12(4):539. [Abstract]
- Research Square Preprint. 2023 Jun 29.
- Research Square Preprint. 2023 Apr 18.
- Patent. US20220332841A1.
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Cell Proliferation/Viability Assay
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WB
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WB
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RT-PCR
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In Vivo Efficacy Study
Biological Activity
Chemical Information
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CAS No. 1691221-67-6
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Molecular Weight 367.38
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Formula C22H14FN5
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SMILES
CC(NC1=C2C=C(F)C=C1)=C2C3=NC4=C5C=CC=NC5=C6N=CC=CC6=C4N3
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Synonyms
LOR-253 hydrochloride; LT-253 hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (21)
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Journal Impact Factor
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Most Recent
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Blood
Epigenetic Regulation of Non-canonical Menin Targets Modulates Menin Inhibitor Response in Acute Myeloid Leukemia. [Abstract]2024 Aug 16:blood.2023023644. PMID: 39158067
APTO-253 hydrochloride purchased from MedChemExpress. Usage Cited in: Blood. 2024 Aug 16:blood.2023023644. [Abstract]
Cell viability of OCI-AML2 cells expressing either sgLuc or sgPCGF1 was assessed under the treatment of APTO-253 (100 nM; 9 d).
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Ann Rheum Dis
Parsing multiomics landscape of activated synovial fibroblasts highlights drug targets linked to genetic risk of rheumatoid arthritis. [Abstract]2021 Apr;80(4):440-450. PMID: 33139312
APTO-253 hydrochloride purchased from MedChemExpress. Usage Cited in: Ann Rheum Dis. 2021 Apr;80(4):440-450. [Abstract]
APTO-253 (1-4 μM) reduced mRNA levels of 8-mix SE-contacted genes (IL-6, CCL5) in stimulated RASFs.
APTO-253 hydrochloride purchased from MedChemExpress. Usage Cited in: Ann Rheum Dis. 2021 Apr;80(4):440-450. [Abstract]
APTO-253 (15 mg/kg; i.v.; twice per day for two consecutive days per week) demonstrated significant therapeutic activity in collagen-induced arthritis (CIA) mice.
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Nat Commun
FAM3A reshapes VSMC fate specification in abdominal aortic aneurysm by regulating KLF4 ubiquitination. [Abstract]2023 Sep 2;14(1):5360. PMID: 37660071
APTO-253 hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Sep 2;14(1):5360. [Abstract]
APTO-253 (10 μM) reversed the effects of FAM3A on suppressing the expression of the markers for macrophages (CD68) and osteoblasts (OPN, RUNX2) in VSMCs.
APTO-253 hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Sep 2;14(1):5360. [Abstract]
KLF4 inducer APTO-253 (1 μg/g; i.p.; once daily for 4 weeks) significantly abrogated the effects of FAM3A on maintaining the contractile phenotype of VSMCs in aortas from AngII-ApoE−/− murine AAA models.
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Nat Commun
Chromatin-informed inference of transcriptional programs in gynecologic and basal breast cancers. [Abstract]2019 Sep 25;10(1):4369. PMID: 31554806 -
Adv Sci (Weinh)
Artesunate Inhibits Neointimal Hyperplasia by Promoting IRF4 Associated Macrophage Polarization. [Abstract]2025 Mar 24:e2408992. PMID: 40126336 -
Leukemia
Targeting of IRAK4 and GSPT1 enhances therapeutic efficacy in AML via c-Myc destabilization. [Abstract]2025 Sep;39(9):2163-2173. PMID: 40670672 -
J Transl Med
KLF4 regulates trophoblast function and associates with unexplained recurrent spontaneous abortion. [Abstract]2024 Oct 10;22(1):922. PMID: 39390495 -
Cell Rep
SETDB2-mediated transcriptional repression of IDE in sensory neurons promotes migraine-like pain behaviors in mice. [Abstract]2026 Mar 24;45(4):117201. PMID: 41880325 -
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JCI Insight
KLF4 is a therapeutically tractable brake on fibroblast activation that promotes resolution of pulmonary fibrosis. [Abstract]2022 Aug 22;7(16):e160688. PMID: 35852857 -
PLoS Pathog
STAT3, MYC, and EBNA1 cooperate through a ZC3H18 transcriptional network to regulate survival and proliferation of EBV-positive lymphomas. [Abstract]2025 May 12;21(5):e1013166. PMID: 40354417 -
Int Immunopharmacol
Succinate pretreatment attenuates intestinal ischemia-reperfusion injury by inhibiting necroptosis and inflammation via upregulating Klf4. [Abstract]2023 Jul:120:110425. PMID: 37285681 -
FASEB J
Induction of T-Cell Differentiation by KLF4 in T-Cell Acute Lymphoblastic Leukemia Cells Harboring Activating Mutation in NOTCH3. [Abstract]2025 May 31;39(10):e70613. PMID: 40354086 -
Mol Cell Biochem
2021 Apr;476(4):1741-1749. PMID: 33428060 -
J Immunol
TLR7-mediated immune response of renal myeloid-derived suppressor cells via RUNX1-KLF4 in systemic candidiasis. [Abstract]2025 Aug 7:vkaf170. PMID: 40795213 -
J Diabetes Res
KLF4 Promotes Diabetic Chronic Wound Healing by Suppressing Th17 Cell Differentiation in an MDSC-Dependent Manner. [Abstract]2021 Sep 15:2021:7945117. PMID: 34568499 -
Neurotox Res
2020 Dec;38(4):967-978. PMID: 32870474 -
Genes (Basel)
Krüppel-Like Factor 4 and Its Activator APTO-253 Induce NOXA-Mediated, p53-Independent Apoptosis in Triple-Negative Breast Cancer Cells. [Abstract]2021 Apr 8;12(4):539. PMID: 33918002 -
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Purity & Documentation
References
[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] [Content Brief]
[3]. 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. [Content Brief]
Calculators
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