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Chemical Structure| 2499663-01-1 Chemical Structure| 2499663-01-1

Structure of STM2457
CAS No.: 2499663-01-1

Chemical Structure| 2499663-01-1

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STM2457 is an inhibitor of methyltransferase-like 3 (METTL3) and METTL14 complex with IC50 value of 16.9 µM.

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Product Details of STM2457

CAS No. :2499663-01-1
Formula : C25H28N6O2
M.W : 444.53
SMILES Code : O=C(C(N=C1N2C=CC=C1)=CC2=O)NCC3=CN4C=C(CNCC5CCCCC5)C=CC4=N3
MDL No. :MFCD34368521
InChI Key :OBERVORNENYOLE-UHFFFAOYSA-N
Pubchem ID :155167581

Safety of STM2457

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P280-P301+P312-P302+P352-P305+P351+P338

Related Pathways of STM2457

epigenetics

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
TM4 cells 20 μM 24 h To verify the m6A-dependent reduction of Wt1 stability under environmental stress PMC10866985
BMDMs 10 μM 7 days STM2457 inhibited TGF-β1-induced MMT, reducing the expression of Smad3, α-SMA, and Col-I PMC11923867
THP-1 0.04-50 μM 72 h To study the anti-leukaemic potential of STM2457 in the AML cell line THP-1, results showed that STM2457 significantly reduced cell proliferation. PMC7613134
MOLM-13 1 μM 24 h To study the anti-leukaemic potential of STM2457 in the AML cell line MOLM-13, results showed that STM2457 significantly reduced cell proliferation and decreased m6A levels. PMC7613134
H446DDP 6.25 μM 24 h STM2457 significantly reduced the IC50 values of CDDP and VP16 in H446DDP cells and increased the proportion of apoptotic cells. PMC10022264
H69AR 6.25 μM 24 h STM2457 significantly reduced the IC50 values of CDDP and VP16 in H69AR cells and increased the proportion of apoptotic cells. PMC10022264
Human lymphatic endothelial cells (HLECs) 1 μM 24 h To evaluate the effects of STM2457 on HLEC proliferation, migration, and tube formation, results showed that STM2457 significantly inhibited these functions PMC11450254
Human lymphatic endothelial cells (HLECs) 1 μM 24 h To evaluate the cytotoxicity of STM2457 on HLECs, results showed no obvious cytotoxicity at 1 μM PMC11450254
HL-1 cardiomyocytes 5 μM 24 h To evaluate the effect of STM2457 on DOX-induced cardiomyocyte ferroptosis, results showed that STM2457 significantly inhibited DOX-induced cell death and LDH release, reduced lipid peroxidation and MDA production, and improved GSH/GSSG ratio. PMC11033199

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice AML PDX models Intraperitoneal injection 50 mg/kg Once daily for two weeks To study the anti-leukaemic effect of STM2457 in AML PDX models, results showed that STM2457 significantly prolonged the lifespan of mice and reduced AML engraftment and expansion. PMC7613134
Mice Orthotopic colorectal cancer model Intratumoral injection 50 mg/kg Single injection To evaluate the effect of GOSM-gel on NK cell infiltration in the orthotopic colorectal cancer model PMC11532749
Mice High-fat diet-induced obesity model Local testicular injection 50.0 mg/kg Once a week for 5 weeks To restore the sperm count and Wt1 levels reduced by high-fat diet PMC10866985
Mice NAFLD-HCC model Intraperitoneal injection 50mg/mice Every other day, ongoing treatment To evaluate the efficacy of STM2457 in combination with anti-PD-1 therapy for NAFLD-HCC. Single STM2457 significantly inhibited tumor growth, while the combination of STM2457 and anti-PD-1 showed stronger tumor suppression and significantly increased intratumoral infiltration of IFN-γ+ and GZMB+ CD8+ T cells. PMC10439254
Nude mice H69AR xenograft model Subcutaneous injection 6.25 μM Single dose, continuous observation of tumor growth STM2457 significantly inhibited the growth of H69AR xenografts and reduced the tumor volume after chemotherapy. PMC10022264
Mice Neuroblastoma xenograft model Intraperitoneal injection 50 mg/kg Once daily for 12 days To evaluate the efficacy of STM2457 in NB treatment, the results showed that STM2457 combined with VCR significantly inhibited tumor growth. PMC11092262
C57BL/6 mice Corneal suture model Subconjunctival injection 1 μM 7 days To evaluate the effects of STM2457 on pathological lymphangiogenesis, results showed that STM2457 significantly inhibited lymphangiogenesis in the corneal suture model PMC11450254
Mice Chronic DOX-induced cardiomyopathy model Intraperitoneal injection 50 mg/kg Once daily for 4 weeks To evaluate the effect of STM2457 on DOX-induced cardiomyopathy, results showed that STM2457 significantly improved DOX-induced cardiac dysfunction, fibrosis, and iron accumulation, and alleviated cardiomyocyte ferroptosis. PMC11033199

Protocol

Bio Calculators
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1 mM

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10 mM

2.25mL

0.45mL

0.23mL

11.25mL

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1.12mL

22.50mL

4.50mL

2.25mL

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