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Art. -Nr.: HY-126256

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PRMT5-IN-1

PRMT5 IN-1, a hemiaminal, is a potent, selective protein arginine methyltransferase 5 (PRMT5) inhibitor with an IC₅₀ of 11 nM for PRMT5/MEP50. PRMT5 IN-1 can be converted to aldehydes and react with C449 to form covalent adducts under physiological conditions.

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CAS. Nr.: 2366149-83-7
Formel: C₁₉H₁₉ClN₄O₅
Molecular Weight:418.83

Speicherung:

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

Data Sheet (273 KB)

PRMT5-IN-1 Chemical Structure

CAS. Nr.: 2366149-83-7

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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
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

PRMT5

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
Granta-519	IC₅₀	0.012 μM Compound: 9	Inhibition of PRMT5 in human Granta-519 assessed as reduction in sDMA production incubated for 3 days by Western blotting analysis Inhibition of PRMT5 in human Granta-519 assessed as reduction in sDMA production incubated for 3 days by Western blotting analysis	[PMID: 31312404]
Granta-519	IC₅₀	0.06 μM Compound: 9	Antiproliferative activity against human GRANTA-519 cells assessed as reduction in cell viability supplemented with fresh medium containing compound every 3 days incubated for 10 days by CCK-8 assay Antiproliferative activity against human GRANTA-519 cells assessed as reduction in cell viability supplemented with fresh medium containing compound every 3 days incubated for 10 days by CCK-8 assay	[PMID: 31312404]

In Vitro

PRMT5 IN-1 (0-500 nM) inhibits the PRMT5/MEP50 complex [K_inact/K_I=1.2×10⁵ M^-1 min^-1] very rapidly with a K_inact of 0.068 min^-1 and a good binding affinity (K_I=55 nM)^[1].
PRMT5 IN-1 (0-1000 nM; 3 d; Granta-519 cells) inhibits the expression of cellular sDMA with an IC₅₀ value of 0.012 μM^[1].
PRMT5 IN-1 (0-1 μM; 10 d; Granta-519 cells) inhibits cell proliferation in a dose-dependent manner with an IC₅₀ value of 0.06 μM^[1].

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

Cell Viability Assay^[1]

Cell Line:

Granta-519 cells
Concentration:

0, 0.0001524, 0.000457, 0.001372, 0.004115, 0.012346, 0.037037, 0.111111, 0.333333 and 1 μM
Incubation Time:

10 days
Result:

Inhibited cell proliferative, in which cells died on day 10 at high concentrations (0.3 and 1 μM).

Western Blot Analysis^[1]

Cell Line:

Granta-519 cells
Concentration:

0, 0.05, 0.15, 0.46, 1.37, 4, 12, 37, 111, 333, 1000 nM
Incubation Time:

3 days
Result:

Inhibited cellular sDMA in Granta-519 cells in a dose-dependent manner.

Chemical Information

CAS. Nr. 2366149-83-7
Molecular Weight 418.83
Formel C₁₉H₁₉ClN₄O₅
SMILES

O[C@@H]1[C@@H]([C@@H](C2=CC=C(Cl)C=C2)O)O[C@@H](N3C=CC4=C3N=CN5C4=NCC5O)[C@@H]1O
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 (273 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]. Lin H, et, al. Discovery of Potent and Selective Covalent Protein Arginine Methyltransferase 5 (PRMT5) Inhibitors. ACS Med Chem Lett. 2019 May 22;10(7):1033-1038. [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.

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MOQ

Minimum order quantity

100 mg

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

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PRMT5-IN-1

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

PRMT5-IN-1 Related Classifications

HY-126256 Related Classifications