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Art. -Nr.: HY-162230

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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.

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CAS. Nr.: 3054228-62-2
Formel: C₂₅H₂₄BrN₅O₃S
Molecular Weight:554.46

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (274 KB)

PRMT5-IN-33 Chemical Structure

CAS. Nr.: 3054228-62-2

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

PRMT5

10.9 nM (IC₅₀)

PRMT1

6.89 μM (IC₅₀)

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
MOLM-13	IC₅₀	123.2 nM Compound: A8	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]

In Vitro

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.

Western Blot Analysis^[1]

Cell Line:

Z-138 and MOLM-13
Concentration:

50-500 nM
Incubation Time:

48 h
Result:

Inhibited expression of sDMA.

In Vivo

PRMT5-IN-33 (60-120 mg/kg, i.g.,twice a day for 13 days) inhibits the MOLM-13 xenograft tumor growth in a dose-dependent manner in BALB/c mice without a body weight loss^[1].
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]

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

Animal Model:

MOLM-13 xenograft tumor in nude BALB/c mice^[1]
Dosage:

60-120 mg/kg
Administration:

intragastrical administration (i.g.), twice a day for 13 days
Result:

Exhibited a tumor growth inhibition rate (TGI) of 33% (60 mg/kg) and 52% (120 mg/kg)

Chemical Information

CAS. Nr. 3054228-62-2
Molecular Weight 554.46
Formel C₂₅H₂₄BrN₅O₃S
SMILES

BrC1=CC2=CC=C(C=C2N=C1N)CC[C@@H]3[C@H]([C@H]([C@@H](C3)NC4=C(C=NC=N4)C(C5=CSC=C5)=O)O)O
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Chen Y, et al., Structure-based discovery of a new series of nucleoside-derived ring-opening PRMT5 inhibitors. Eur J Med Chem. 2024 Jan 28;267:116171. [Content Brief]

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise

route	Dose (mg/kg)	T_max (h)	C_max (ng/mL)	AUC_0-t (ng·h/mL)	AUC_0-inf (ng·h/mL)	T_1/2 (h)
po	10	0.25	6870	6730	6760	1.17

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PRMT5-IN-33

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

PRMT5-IN-33 Related Classifications

HY-162230 Related Classifications