Réactifs et instruments pour l'immunologie, la biologie cellulaire et la biologie moléculaire.
 
> RSM3 (TFA)

RSM3 (TFA)

Imprimer Imprimer
Identifiez-vous

Référence HY-P10387A-10mg

Conditionnement : 10mg

Marque : MedChemExpress


Description

RSM3 TFA is a METTL3-METTL14 complex inhibitor with a Kd of 3.10 μM for the METTL3-METTL14 complex. RSM3 TFA reduces the m6A modification level of SLC31A1 and the global RNA methylation level. RSM3 TFA upregulates programmed cell death-related genes, enhances cell apoptosis, inhibits pro-cancer signals and suppresses tumor growth. RSM3 TFA is applicable to the research of preeclampsia and cancer[1][2].

In Vitro

RSM3 TFA inhibits the methyltransferase activity of the purified METTL3-METTL14 complex by 45.5%[1].
RSM3 TFA inhibits the viability of CCRF-CEM leukemia cells with an IC50 of 4.6 μM[1].
RSM3 TFA inhibits the viability of DU145 prostate cancer cells with an IC50 of 25.8 μM[1].
RSM3 TFA inhibits the viability of ASPC-1 pancreatic cancer cells with an IC50 of 33.8 μM[1].
RSM3 TFA inhibits the viability of PC3 prostate cancer cells with an IC50 of 26.5 μM[1].
RSM3 (15 μM; 24 h) TFA reduces the migratory capacity of PC3 and DU145 prostate cancer cells[1].
RSM3 (15 μM) TFA induces G1 phase cell cycle arrest and apoptosis in PC3 and DU145 prostate cancer cells[1].
RSM3 (25 μM; 12 h) TFA reduces the protein levels of METTL3 and METTL14 in PC3 prostate cancer cells[1].
RSM3 (25 μM; 12 h) TFA inhibits the activity of the ERK/MAPK signaling pathway in PC3 prostate cancer cells by reducing the phosphorylation level of p42/44[1].
RSM3 (12 h) TFA reduces the global RNA m6A modification level in PC3 and DU145 prostate cancer cells[1].
RSM3 (25 μM; 12 h) TFA induces a specific transcriptomic response in PC3 prostate cancer cells, upregulating programmed cell death, p53 signaling pathway, differentiation and immune pathways, while downregulating cancer proliferation and cell cycle pathways, and enriching gene signatures of apoptosis, p53 and AR pathways[1].
RSM3 (25 μM; 12 h) TFA upregulates NF-κB, inflammation, apoptosis and luminal differentiation-related genes, and downregulates cell cycle, proliferation and stemness-related genes in PC3 prostate cancer cells[1].

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

RSM3 TFA Related Antibodies

Cell Migration Assay [1]

Cell Line: PC3 and DU145 (prostate cancer) cells
Concentration: 15 μM
Incubation Time: 24 h
Result: Resulted in approximately a 2-3 fold reduction in cell migration in PC3 and DU145 cells.

Western Blot Analysis[1]

Cell Line: PC3 (prostate cancer) cells
Concentration: 25 μM
Incubation Time: 12 h
Result: Reduced the protein levels of METTL3 and METTL14 in PC3 cells.\n
Reduced phosphorylation levels of p42/44 (ERK1/2).

Real Time qPCR[1]

Cell Line: PC3 (prostate cancer) cells
Concentration: 25 μM
Incubation Time: 12 h
Result: Upregulated NF-kB responsive, inflammatory, apoptosis, and luminal differentiation (AR, PSA, NKX3.1, CK18) genes, and downregulated cell cycle, proliferation, and stemness genes.
In Vivo

RSM3 (50 mg/kg; i.p.; single administration) TFA shows no obvious acute toxicity in C57BL/6 mice[1].
RSM3 (20 mg/kg; peritumoral injection; once every 2 days; for 14 consecutive days) TFA inhibits the growth of PC3/ASPC-1 xenografts in mice[1].
RSM3 (50 mg/kg; intraperitoneal injection; daily; 11 days) TFA significantly improves preeclampsia (PE)-related symptoms in rats[2].

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

Animal Model: Immunocompromised mice treated PC3 cells (xenograft model)[1]
Dosage: 20 mg/kg
Administration: peri-tumoral injection; every 2 days; 14 days
Result: Reduced tumor volumes, average tumor mass.
Decreased METTL3 expression and global m6A levels in tumor tissue.
Increased Caspase-3 expression, decreased Ki67 expression in tumor tissue.
Showed no significant changes in body weight.
Detected no histopathological abnormalities in heart, liver, spleen, lung, or kidney tissue.
Animal Model: Immunocompromised mice treated ASPC-1 cells (xenograft model)[1]
Dosage: 20 mg/kg
Administration: peri-tumoral injection; every 2 days; 14 days
Result: Reduced tumor volume.
Lowered average tumor mass.
Animal Model: Sprague-Dawley (SD) (female, 7-week-old, 200-220 g, PE model)[2]
Dosage: 50 mg/kg
Administration: i.p.; daily; GD 10 to GD 20
Result: Significantly reduced systolic blood pressure.
Significantly reduced 24-hour urine protein concentration.
Significantly reduced urine albumin to creatinine ratio.
Significantly lowered placental METTL3 protein expression.
Significantly increased placental SLC31A1 protein expression.
Significantly reduced m6A modification level of SLC31A1 in placental tissue.
Masse moléculaire

3049.66 (free base)

Formule

C130H218N54O26S3.xC2HF3O2
Appearance

Solid

Color

White to off-white

Sequence

Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Cys-Met-Glu-Leu-Gly-Arg-Glu-Cys-Leu-Asn-Leu-Trp-NH2 (Stapled between two Cys via bhp)
Sequence Shortening

RRRRRRRRRCMELGRECLNLW-NH2 (Stapled between two Cys via bhp)
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

Sealed storage, away from moisture

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvant et solubilité
In Vitro: 

DMSO : 66.67 mg/mL (Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

  • Calculateur de molarité

  • Calculateur de dilution

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Pureté et documentation
Références