PRMT/HKMT-IN-1
PRMT/HKMT-IN-1 is an epigenetic multi-target protein arginine methyltransferases (PRMTs) and histone lysine methyltransferases (HKMTs) inhibitor. PRMT/HKMT-IN-1 inhibits Aspergillus nidulans RmtA with an IC50 of 29 μM. PRMT/HKMT-IN-1 inhibits human PRMT1, p300/CBP HAT, CARM1, SET7, SIRT1 and SIRT2. PRMT/HKMT-IN-1 inhibits methylation of histone H3K4, H4R3, and H3R17 residues. CBP/p300-IN-23 induces apoptosis, arrests cell cycle in S phase, and triggers granulocytic differentiation in leukemia cells. PRMT/HKMT-IN-1 can be used for the research of leukemia.
For research use only. We do not sell to patients.
- CAS No.: 1020399-52-3
- Formula: C19H12Br4O4
- Molecular Weight:623.92
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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CBP/p300 |
SIRT1 |
SIRT2 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| U-937 | Inhibition |
61 %
Compound: 4j
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Inhibition of human p300/CBP in U937 cells at 50 uM assessed as histone H3 acetylation
Inhibition of human p300/CBP in U937 cells at 50 uM assessed as histone H3 acetylation
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[PMID: 18348515] |
PRMT/HKMT-IN-1 (Compound 4j) inhibits fungal RmtA with an IC50 of 29 μM[1].
PRMT/HKMT-IN-1 (50 μM) inhibits human PRMT1 activity by 91.1% using histone H4 as substrate[1].
PRMT/HKMT-IN-1 (100 μM; 90 min) strongly inhibits human CARM1 and SET7[1].
PRMT/HKMT-IN-1 (50 μM; 24 h) reduces H3K4, H4R3, and H3R17 methylation in U937 cells[1].
CBP/p300-IN-23 (50 μM; 90 min) inhibits p300/CBP HAT activity by 61%[1].
PRMT/HKMT-IN-1 (25 μM; 2 h) inhibits SIRT1 and SIRT2[1].
PRMT/HKMT-IN-1 (25 μM; 30 h) induces 28% apoptosis in human leukemia U937 cells[1].
PRMT/HKMT-IN-1 (0.5-5 μM; 30 h) induces dose-dependent granulocytic differentiation in human leukemia U937 cells, with 96.1% CD11c-positive cells at 5 μM after 30 h of treatment[1].
CBP/p300-IN-23 (25 μM; 30 h) induces S phase cell cycle arrest in human leukemia U937 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human leukemia U937 cells
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Concentration:50 μM
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Incubation Time:24 h
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Result:Strongly inhibited H3K4 monomethylation.
Inhibited H4R3 monomethylation.
Inhibited H3R17 dimethylation.
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Cell Line:Human leukemia U937 cells
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Concentration:25 μM
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Incubation Time:30 h
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Result:Induced 28% apoptosis in U937 cells.
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Cell Line:Human leukemia U937 cells
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Concentration:0.5-5 μM
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Incubation Time:30 h
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Result:Induced 96.1% CD11c-positive/PI-negative cells at 5 μM.
Induced 67% CD11c-positive/PI-negative cells at 1 μM.
Induced 59% CD11c-positive/PI-negative cells at 0.5 μM, showing a dose-dependent differentiating effect.
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Cell Line:Human leukemia U937 cells
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Concentration:25 μM
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Incubation Time:30 h
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Result:Induced cell cycle arrest in S phase.
Chemical Information
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CAS No. 1020399-52-3
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Molecular Weight 623.92
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Formula C19H12Br4O4
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SMILES
O=C1C(=CC2=CC(Br)=C(O)C(Br)=C2)COCC1=CC3=CC(Br)=C(O)C(Br)=C3
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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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