2. Epigenetics Apoptosis
  3. Histone Methyltransferase Apoptosis
  4. PRMT1-IN-3

PRMT1-IN-3 is a potent protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 4.11 μM. PRMT1-IN-3 inhibits PRMT6 and PRMT8 with IC50s of 23.3 and 30.1 μM. PRMT1-IN-3 suppresses asymmetric dimethylarginine (ADMA) levels and histone H4R3me2a modification in triple-negative breast cancer (TNBC) cells. PRMT1-IN-3 induces cell cycle arrest, apoptosis, and inhibits migration and colony formation in MDA-MB-231 cells. PRMT1-IN-3 acts as chemotherapeutic sensitizers for Paclitaxel (HY-B0015). PRMT1-IN-3 can be used for the study of TNBC.

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PRMT1-IN-3

PRMT1-IN-3 Chemical Structure

CAS No. : 892570-48-8

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PRMT1-IN-3 Related Antibodies

Top Publications Citing Use of Products

View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms
EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

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Description

PRMT1-IN-3 is a potent protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 4.11 μM. PRMT1-IN-3 inhibits PRMT6 and PRMT8 with IC50s of 23.3 and 30.1 μM. PRMT1-IN-3 suppresses asymmetric dimethylarginine (ADMA) levels and histone H4R3me2a modification in triple-negative breast cancer (TNBC) cells. PRMT1-IN-3 induces cell cycle arrest, apoptosis, and inhibits migration and colony formation in MDA-MB-231 cells. PRMT1-IN-3 acts as chemotherapeutic sensitizers for Paclitaxel (HY-B0015). PRMT1-IN-3 can be used for the study of TNBC[1].

IC50 & Target[1]

PRMT1

4.11 μM (IC50)

PRMT3

> 100 μM (IC50)

PRMT4

> 100 μM (IC50)

PRMT6

23.3 μM (IC50)

PRMT5

> 100 μM (IC50)

PRMT8

30.1 μM (IC50)

PRMT7

> 100 μM (IC50)

In Vitro

PRMT1-IN-3 (Compound YH-4) (10 μM, 37-65°C) significantly enhances the thermal stability of PRMT1 (ΔTm = +5.2°C) and has no significant effect on other PRMT subtypes[1].
PRMT1-IN-3 (0.01-100 μM, 48 h) inhibits MDA-MB-231, HCT116, HeLa, and A549 cells growth with IC50s of 6.38 μM, 15.29 μM, 12.97 μM, and 9.187 μM, respectively[1].
PRMT1-IN-3 (1.25-10 μM, 48 h) dose-dependently inhibits ADMA levels and H4R3me2a modification in MDA-MB-231 cells[1].
PRMT1-IN-3 (0-20 μM, 72 h) (resistance ratio: 9.0) shows synergistic effect with Paclitaxel (PTX) (resistance ratio: 92.7) in MDA-MB-231 cells and MDA-MB-231/Taxol cells[1].
PRMT1-IN-3 (0-40 μM, 0-48 h) induces G0/G1 phase arrest and cell apoptosis, and inhibits cell migration in MDA-MB-231 cells[1].
PRMT1-IN-3 (0-20 μM, 10 days) almost completely inhibits MDA-MB-231 cells colony formation at 20 μM[1].

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

PRMT1-IN-3 Related Antibodies

Apoptosis Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 0, 5, 20 and 40 μM
Incubation Time: 48 h
Result: Resulted in an increase in early apoptosis from 2.34 % to 34.3 % from 2.5 μM to 40 μM.

Cell Cycle Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 0, 2.5, 5, 10, 20 μM
Incubation Time: 48 h
Result: Observed that the proportion of cells in the G0/G1 phase increased in a dose-dependent manner from 41.8 % to 60.9 %, while the proportions of cells in the S phase and G2/M phase decreased in a dose-dependent manner from 33.2 % to 23.6 % and from 24.9 % to 15.2 %, respectively.

Cell Migration Assay [1]

Cell Line: MDA-MB-231 cells
Concentration: 1.25, 2.5, 5, 10 and 20 μM
Incubation Time: 0, 12, 36, and 48 h
Result: Decreased the healing rate to 18.52% after 48 h at 20 μM.
In Vivo

PRMT1-IN-3 (Compound YH-4) (30 mg/kg, i.p., for one week, then discontinue for three days, for a total of 21 days) is a chemotherapeutic sensitizer for PTX, enhancing its therapeutic efficacy while significantly reducing the required dosage and mitigating it toxic side effects in TNBC mice model[1].

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

Animal Model: MDA-MB-23-YFP-Luc cells induced xenograft model established in female nude mice 4-5 weeks old weighing 16-18 g[1]
Dosage: 30 mg/kg with or without PTX
Administration: Intraperitoneal injection (i.p.), for one week, then discontinue for three days, for a total of 21 days
Result: Demonstrated significant inhibitory effects on tumor volume, with the combination of PTX showing a markedly superior antitumor efficacy compared to the monotherapies.
Molecular Weight

302.39

Formula

C18H23FN2O
CAS No.
SMILES

FC1=CC=C(COC2=C(C=CC=C2)CNCCCNC)C=C1
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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PRMT1-IN-3 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:

PRMT1-IN-3892570-48-8Histone MethyltransferaseApoptosisPRMT1 inhibitorTriple-negative breast cancerVirtual screeningChemotherapeutic sensitizersInhibitorinhibitorinhibit

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