2. Epigenetics
  3. METTL3
  4. EP652

EP652 is a METTL3 inhibitor and antitumor agent with IC50 values of 2 nM, <10 nM, and 37 nM in SPA, intracellular, and ATPlite assays, respectively. EP652 exhibits high selectivity against 40 other methyltransferases and FTO, and possesses favorable pharmacokinetic parameters. EP652 reduces intracellular N6-methyladenosine (m6A) levels in mRNA. EP652 inhibits tumor growth and progression of both hematologic malignancies and solid tumors. EP652 can be used for the research of acute myeloid leukemia, ovarian cancer, non-small cell lung cancer, and hypopharyngeal squamous cell carcinoma.

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EP652

EP652 Chemical Structure

CAS No. : 3050819-22-9

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Description

EP652 is a METTL3 inhibitor and antitumor agent with IC50 values of 2 nM, <10 nM, and 37 nM in SPA, intracellular, and ATPlite assays, respectively. EP652 exhibits high selectivity against 40 other methyltransferases and FTO, and possesses favorable pharmacokinetic parameters. EP652 reduces intracellular N6-methyladenosine (m6A) levels in mRNA. EP652 inhibits tumor growth and progression of both hematologic malignancies and solid tumors. EP652 can be used for the research of acute myeloid leukemia, ovarian cancer, non-small cell lung cancer, and hypopharyngeal squamous cell carcinoma[1].

In Vitro

EP652 (range; 24 h for Calu-6) potently reduces intracellular m6A levels across multiple liquid and solid tumor cell lines, with IC50 values ranging from 3 nM to 9 nM, including an IC50 of 8.6 nM in Calu-6 cells after 24-hour treatment[1].
EP652 inhibits 3D spheroid proliferation of NCI-H1650 lung cancer cells with an IC50 of 99 nM[1].
EP652 (respective IC50 concentrations; 72 h) modulates key oncogenic and pro-apoptotic biomarkers in solid tumor cell lines after 72-hour treatment at their respective IC50 concentrations, reducing Bcl-2 levels and increasing Bax levels[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

EP652 Related Antibodies

Cell Viability Assay[1]

Cell Line: Kasumi-1, MV-4-11, Caov-3, Calu-6, A549, FaDu, SK-OV-3
Concentration: Range (to determine IC50 values)
Incubation Time: 72 h
Result: Demonstrated dose-dependent antiproliferative activity with IC50 values of 37 nM (Kasumi-1), 234 nM (MV-4-11), 20 nM (Caov-3), 18 nM (Calu-6), 169 nM (A549), 50 nM (FaDu), and 11 nM (SK-OV-3).

Western Blot Analysis[1]

Cell Line: SK-OV-3, FaDu, A549
Concentration: IC50 concentration (respective cell lines)
Incubation Time: 72 h
Result: Downregulated the oncogenic biomarker Bcl-2 (relative expression: 0.9 in SK-OV-3, 0.6 in FaDu, 0.3 in A549) compared to DMSO-treated controls.
Upregulated the pro-apoptotic biomarker Bax (relative expression: 1.6 in SK-OV-3, 1.9 in FaDu, 1.6 in A549) compared to DMSO-treated controls.
Parmacokinetics
Species Dose Route AUC CLunbound
Rat[1] 1 mg/kg i.v. 5.1 μM·min 358 mL/min/kg
Mice[1] 30 mg/kg i.p. 175.8 μM·min /
In Vivo

EP652 (0.3-3 mg/kg, intraperitoneal injection, once daily for 2 consecutive days) reduces the maximum cellular m6A level (by up to 75%) in peripheral blood mononuclear cells of rats[1].
EP652 (30 mg/kg; intraperitoneal injection; once daily; for 91 consecutive days) significantly prolongs the survival of patient-derived xenograft models of acute myeloid leukemia, with a 100% survival rate on day 112[1].
EP652 (10-30 mg/kg; i.p.; once daily; days 19 to 31) inhibits the progression of acute myeloid leukemia, reduces the human cancer cell burden in the blood, bone marrow and spleen, and a dose-dependent response is observed at the doses of 10 mg/kg and 30 mg/kg[1].
EP652 (30 mg/kg; i.p.; once daily) prolongs the survival time of mice in orthotopic xenograft models of non-small cell lung cancer and subcutaneous xenograft models of pharyngeal squamous cell carcinoma, respectively[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Sprague-Dawley rats (male)[1]
Dosage: 0.3 mg/kg; 1 mg/kg; 3 mg/kg
Administration: i.p.; daily; 2 days
Result: Induced a maximum ~75% reduction in cellular m6A levels in peripheral blood mononuclear cells at the 0.3 mg/kg dose.
Animal Model: NSG mice with Acute myeloid leukemia (female; orthotopic patient-derived xenograft model via intratibial implantation of LEXFAM 4128 cells)[1]
Dosage: 30 mg/kg
Administration: i.p.; daily; 91 days
Result: Resulted in 100% survival of mice up to study conclusion on day 112, compared to vehicle control mice which had 0% survival by day 60.
Animal Model: NSG mice with Acute myeloid leukemia (female; disseminated cell line-derived xenograft model via intravenous implantation of 2×106 MV-4-11-Luc-mCh-Puro cells)[1]
Dosage: 10 mg/kg (day 19 bioluminescence assessment); 30 mg/kg (31-day treatment)
Administration: i.p.; daily; 19 days (10 mg/kg); daily; 31 days (30 mg/kg)
Result: Inhibited AML progression as measured by bioluminescence imaging at 30 mg/kg.
Showed selective decreases in hCD45+ human cancer cells in bone marrow, blood, and spleen (reaching near-undetectable levels in bone marrow and spleen) at 30 mg/kg.
Induced a dose-dependent reduction in bioluminescence signal on day 19 post-implant at 10 mg/kg and 30 mg/kg.
Animal Model: NSG mcie with Ovarian cancer (female; orthotopic cell line-derived xenograft model via implantation of SK-OV-3 cells)[1]
Dosage: 30 mg/kg
Administration: i.p.; daily
Result: Inhibited tumor growth as measured by bioluminescence imaging, with sustained low signal levels compared to vehicle control.
Significantly improved survival (p < 0.01) relative to vehicle control.
Caused minimal body weight loss and no macroscopic adverse events.
Animal Model: Subcutaneous cell line-derived xenograft mice model via implantation of FaDu cells[1]
Dosage: 30 mg/kg
Administration: i.p.; daily
Result: Significantly prolonged survival.
Inhibited tumor growth as measured by direct tumor volume assessment.
Caused minimal body weight loss and no macroscopic adverse events.
Animal Model: Orthotopic cell line-derived xenograft mice model via implantation of A549 cells[1]
Dosage: 30 mg/kg
Administration: i.p.; daily
Result: Significantly prolonged survival relative to vehicle control.
Caused minimal body weight loss and no macroscopic adverse events.
Molecular Weight

462.59

Formula

C25H34N8O
CAS No.
SMILES

C[C@H](N1C=CC(N2CCC[C@H](C2)NCC3CC3)=CC1=O)N4C=C(N=N4)C5=CC(N(C)C)=CN=C5
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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EP652 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

EP6523050819-22-9EP 652EP-652METTL3Methyltransferase-like 3methyltransferasesacute myeloid leukemiaantineoplastic agentovarian cancerm6Anon-small cell lung cancerhypopharyngeal squamous cell carcinomaN6-methyladenosineFTOInhibitorinhibitorinhibit

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