PRMT5-IN-33
PRMT5-IN-33 (compound A8) is a selective, SAM-competitve PRMT5 inhibitors with IC50 of 10.9 nM. PRMT5-IN-33 induces apoptosis and inhibits proliferation of cells Z-138 and MOLM-13. PRMT5-IN-33 exhibits an antitumor activity.
For research use only. We do not sell to patients.
- CAS No.: 3054228-62-2
- Formula: C25H24BrN5O3S
- Molecular Weight:554.46
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Histone Methyltransferase Isoforms
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Biological Activity
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PRMT5 10.9 nM (IC50) |
PRMT1 6.89 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MOLM-13 | IC50 |
123.2 nM
Compound: A8
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Antiproliferation activity against human MOLM-13 cells assessed as cell viability incubated for 6 days by CCK-8 assay
Antiproliferation activity against human MOLM-13 cells assessed as cell viability incubated for 6 days by CCK-8 assay
|
[PMID: 38301329] |
| Z-138 | IC50 |
248.6 nM
Compound: A8
|
Antiproliferation activity against human Z138 cells assessed as cell viability incubated for 6 days by CCK-8 assay
Antiproliferation activity against human Z138 cells assessed as cell viability incubated for 6 days by CCK-8 assay
|
[PMID: 38301329] |
PRMT5-IN-33 inhibits proliferation of cells Z-138 and MOLM-13, with IC50s of 123.2 nM and 248.6 nM, respectively[1].
PRMT5-IN-33 decreases levels of arginine symmetrical dimethylation (sDMA) in a dose-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Z-138 and MOLM-13
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Concentration:50-500 nM
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Incubation Time:48 h
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Result:Inhibited expression of sDMA.
PRMT5-IN-33 (p.o., 10 mg/kg, single dosage) reveals a pharmacokinetic profils in ICR mice[1]:
.
Pharmacokinetic Analysis of PRMT5-IN-33 in ICR mice[1]
| route | Dose (mg/kg) | Tmax (h) | Cmax (ng/mL) | AUC0-t (ng·h/mL) | AUC0-inf (ng·h/mL) | T1/2 (h) |
| po | 10 | 0.25 | 6870 | 6730 | 6760 | 1.17 |