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Referencia número: HY-189289

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PRMT5-IN-58

PRMT5-IN-58 is an MTA-cooperative PRMT5 inhibitor and PRMT5-MTA complex binder (IC₅₀ = 11.7 nM) that inhibits methyltransferase activity and SDMA (HY-101410) production by stabilizing the MTA-bound conformation, and induces apoptosis via sub-G1 phase accumulation, exhibiting selective antiproliferative activity against MTAP-deleted cancer cells over MTAP wild-type cells. PRMT5-IN-58 can be used for research on MTAP-deleted cancers.

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No. CAS: 3107304-24-2
Fòrmula: C₃₁H₃₇N₇O₃S
Peso molecular:587.74

Almacenamiento:

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

Data Sheet (290 KB)

PRMT5-IN-58 Chemical Structure

No. CAS: 3107304-24-2

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Use of MCE Products

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

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Pureza y Documentación
Referencias
Calculators
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

IC₅₀ & Target

^[1]

PRMT5

11.7 nM (IC₅₀)

Ver todos los productos específicos de isoformas Histone Methyltransferase :

Cellular Effect

Cell Line	Type	Value	Description	References
HCT116 MTAP-de	IC50	13 nM	Antiproliferative activity against MTAP-deleted HCT116 cells assessed as reduction in cell viability incubated for 10 days by CellTiter-Glo Luminescent Cell Viability Assay. Antiproliferative activity against MTAP-deleted HCT116 cells assessed as reduction in cell viability incubated for 10 days by CellTiter-Glo Luminescent Cell Viability Assay.	42531724
HCT-116	IC50	0.913 μM	Antiproliferative activity against MTAP-wild type HCT116 cells assessed as reduction in cell viability incubated for 10 days by CellTiter-Glo Luminescent Cell Viability Assay. Antiproliferative activity against MTAP-wild type HCT116 cells assessed as reduction in cell viability incubated for 10 days by CellTiter-Glo Luminescent Cell Viability Assay.	42531724
NCI-H1650	IC50	9 nM	Antiproliferative activity against MTAP-deleted H1650 cells assessed as reduction in cell viability. Antiproliferative activity against MTAP-deleted H1650 cells assessed as reduction in cell viability.	42531724
Lu-99 cell line	IC50	23 nM	Antiproliferative activity against MTAP-deleted LU99 cells assessed as reduction in cell viability. Antiproliferative activity against MTAP-deleted LU99 cells assessed as reduction in cell viability.	42531724
LN-18	IC50	< 1.5 nM	Antiproliferative activity against MTAP-deleted LN18 cells assessed as reduction in cell viability. Antiproliferative activity against MTAP-deleted LN18 cells assessed as reduction in cell viability.	42531724
MIA PaCa-2	IC50	51 nM	Antiproliferative activity against MTAP-deleted MIA PaCa-2 cells assessed as reduction in cell viability. Antiproliferative activity against MTAP-deleted MIA PaCa-2 cells assessed as reduction in cell viability.	42531724
NCI-H358	IC50	1234 nM	Antiproliferative activity against MTAP-wild type H358 cells assessed as reduction in cell viability. Antiproliferative activity against MTAP-wild type H358 cells assessed as reduction in cell viability.	42531724
HCT116 MTAP-de	IC50	6.9 nM	Inhibition of symmetric dimethylarginine production in MTAP-deleted HCT116 cells incubated for 4 days by Western blotting assay. Inhibition of symmetric dimethylarginine production in MTAP-deleted HCT116 cells incubated for 4 days by Western blotting assay.	42531724
HCT-116	IC50	55.5 nM	Inhibition of symmetric dimethylarginine production in MTAP-wild type HCT116 cells incubated for 4 days by Western blotting assay. Inhibition of symmetric dimethylarginine production in MTAP-wild type HCT116 cells incubated for 4 days by Western blotting assay.	42531724

In Vitro

Anti-cancerApoptosisCell Cycle RegulationOthers

Anti-cancer

PRMT5-IN-58 (compound 9u) (10 days) exhibits potent antiproliferative activity against HCT116 MTAP-deleted cells with an IC₅₀ of 13 nM and 70-fold selectivity over HCT116 MTAP wild-type cells^[1].
PRMT5-IN-58 exhibits potent and selective antiproliferative activity in multiple MTAP-deleted cancer cell lines (H1650, LU99, LN18, MIA PaCa-2), with IC₅₀ values ranging from < 1.5 to 51 nM, while showing minimal effect on MTAP wild-type H358 cells^[1].
PRMT5-IN-58 (4 days) selectively inhibits SDMA production in HCT116 MTAP-deleted cells with an IC₅₀ of 6.9 nM and exhibits 8-fold selectivity over HCT116 MTAP wild-type cells (IC₅₀ = 55.5 nM)^[1].

Anti-cancer

Apoptosis

Cell Cycle Regulation

PRMT5-IN-58 (10-100 nM; 7 days) selectively triggers apoptosis in MTAP-deleted Miapaca-2 and PSN-1 cells in a concentration-dependent manner, without affecting the cell cycle of MTAP wild-type HCT116 cells^[1].

Others

PRMT5-IN-58 significantly inhibits the PRMT5⋅MTA complex with an IC₅₀ of 11.7 nM^[1].
PRMT5-IN-58 binds to the PRMT5-MTA complex and forms key interactions with residues such as Phe327, Trp579, Glu444, Glu435, Phe580, and Thr323^[1].

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

Western Blot Analysis^[1]

Cell Line:

HCT116 MTAP-deleted and HCT116 MTAP-wt cell lines
Concentration:

0.15, 0.45, 1.37, 4, 12, 37, 111, 333, 1000 nM
Incubation Time:

4 days
Result:

Inhibited SDMA production in MTAP-deleted HCT116 cells with an IC₅₀ value of 6.9 nM and complete inhibition at 111 nM.
Inhibited SDMA production in MTAP-wt HCT116 cells with an IC₅₀ value of 55.5 nM and full suppression at 333 nM.

Cell Cycle Analysis^[1]

Cell Line:

Miapaca-2, PSN-1, HCT116
Concentration:

10, 100 nM
Incubation Time:

7 days
Result:

Induced concentration-dependent accumulation of sub-G1 cells in MTAP-deleted Miapaca-2 and PSN-1 cell lines.
Did not affect the cell cycle profile of MTAP wild-type HCT116 cells.

Related Protocols :

Chemical Information

No. CAS 3107304-24-2
Peso molecular 587.74
Fòrmula C₃₁H₃₇N₇O₃S
SMILES

C[C@@H](CC1)CN(C(C(NC2=CC(CC)=C(N)N=C2)=O)=O)[C@H]1C3=CC=C4C(N5C(S4)=NC(CN6CCCCC6)=CC5=O)=C3
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (290 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)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Liu B, et al. Design, synthesis and evaluation of benzo[4,5]thiazolo[3,2-a]pyrimidin-4-one derivatives as novel MTA cooperative PRMT5 inhibitors for the treatment of MTAP-deleted cancers. Bioorganic chemistry. 2026 Oct 05;181:110285.

Calculators

Calculadora de molaridad

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Calculadora de dilución

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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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