Referencia número: HY-101563

Pemrametostat

Name: Pemrametostat
Brand: MedChemExpress
SKU: HY-101563
Price: 50.00 USD
Availability: InStock
Rating: 5 (33 reviews)

(Synonyms: GSK3326595; EPZ015938)

33 Cited Publications

Revisión del cliente

Based on 33 publication(s) in Google Scholar

GSK3326595 is a protein arginine methyltransferase 5 (PRMT5) inhibitor. GSK3326595 decreases SARS-CoV-2 infection, inhibits cancer cell proliferation and induces pro-inflammatory macrophage polarization and increases hepatic triglyceride levels without affecting atherosclerosis. GSK3326595 can be used for research of relapsed/refractory mantle cell lymphoma.

Para uso exclusivo en investigación. No vendemos a pacientes.

Pureza: 99.82%
No. CAS: 1616392-22-3
Fòrmula: C₂₄H₃₂N₆O₃
Peso molecular:452.55

Almacenamiento:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Pemrametostat Chemical Structure

No. CAS: 1616392-22-3

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Use of MCE Products

Fluorescent Dye

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

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Ensayo clínico
Chemical Information
Publications (33)
Solvente y solubilidad
- In Vitro
- In Vivo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

IC₅₀ & Target

PRMT5

CDK4

CDK6

Ver todos los productos específicos de isoformas Histone Methyltransferase :

Ver todos los productos específicos de isoformas CDK :

Cellular Effect

Cell Line	Type	Value	Description	References
5637	GI₅₀	0.069 μM Compound: GSK3326595	Antiproliferative activity against human 5637 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay Antiproliferative activity against human 5637 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay	[PMID: 29946150]
A 172	GI₅₀	1.167 μM Compound: GSK3326595	Antiproliferative activity against human A-172 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay Antiproliferative activity against human A-172 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay	[PMID: 29946150]
BJAB	GI₅₀	1.9 μM Compound: GSK3326595	Antiproliferative activity against human BJAB cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay Antiproliferative activity against human BJAB cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay	[PMID: 29946150]
DOHH-2	GI₅₀	0.213 μM Compound: GSK3326595	Antiproliferative activity against human DOHH-2 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay Antiproliferative activity against human DOHH-2 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay	[PMID: 29946150]
HCC1143	GI₅₀	0.246 μM Compound: GSK3326595	Antiproliferative activity against human HCC1143 cells assessed as cell growth inhibition viability incubated for 6 days by celltiter-glo assay Antiproliferative activity against human HCC1143 cells assessed as cell growth inhibition viability incubated for 6 days by celltiter-glo assay	[PMID: 29946150]
HCC1806	GI₅₀	0.098 μM Compound: GSK3326595	Antiproliferative activity against human HCC1806 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay Antiproliferative activity against human HCC1806 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay	[PMID: 29946150]
HCC70	GI₅₀	0.13 μM Compound: GSK3326595	Antiproliferative activity against human HCC70 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay Antiproliferative activity against human HCC70 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay	[PMID: 29946150]
HCT-116	IC₅₀	189 nM Compound: GSK3326595	Antiproliferative activity against MTAP knockout human HCT-116 cells assessed as reduction in cell viability incubated for 5 days followed by replacement with fresh medium containing compound and measured after 5 days by CTG assay Antiproliferative activity against MTAP knockout human HCT-116 cells assessed as reduction in cell viability incubated for 5 days followed by replacement with fresh medium containing compound and measured after 5 days by CTG assay	[PMID: 35041419]
HCT-116	IC₅₀	237 nM Compound: GSK3326595	Antiproliferative activity against human HCT-116 cells expressing wild type MTAP assessed as reduction in cell viability incubated for 5 days followed by replacement with fresh medium containing compound and measured after 5 days by CTG assay Antiproliferative activity against human HCT-116 cells expressing wild type MTAP assessed as reduction in cell viability incubated for 5 days followed by replacement with fresh medium containing compound and measured after 5 days by CTG assay	[PMID: 35041419]
HT-1376	GI₅₀	17.599 μM Compound: GSK3326595	Antiproliferative activity against human HT-1376 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay Antiproliferative activity against human HT-1376 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay	[PMID: 29946150]
J82	GI₅₀	29.326 μM Compound: GSK3326595	Antiproliferative activity against human J82 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay Antiproliferative activity against human J82 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay	[PMID: 29946150]
JeKo-1	GI₅₀	5.402 μM Compound: GSK3326595	Antiproliferative activity against human JeKo-1 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay Antiproliferative activity against human JeKo-1 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay	[PMID: 29946150]
JM1	GI₅₀	0.079 μM Compound: GSK3326595	Antiproliferative activity against human JM1 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay Antiproliferative activity against human JM1 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay	[PMID: 29946150]
JVM-2	GI₅₀	0.009 μM Compound: GSK3326595	Antiproliferative activity against human JVM-2 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay Antiproliferative activity against human JVM-2 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay	[PMID: 29946150]
KMS-11	GI₅₀	0.066 μM Compound: GSK3326595	Antiproliferative activity against human KMS-11 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay Antiproliferative activity against human KMS-11 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay	[PMID: 29946150]
LN-229	GI₅₀	0.254 μM Compound: GSK3326595	Antiproliferative activity against human LN-229 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay Antiproliferative activity against human LN-229 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay	[PMID: 29946150]
LP-1	GI₅₀	1.945 μM Compound: GSK3326595	Antiproliferative activity against human LP-1 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay Antiproliferative activity against human LP-1 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay	[PMID: 29946150]
Maver1	GI₅₀	0.085 μM Compound: GSK3326595	Antiproliferative activity against human MAVER-1 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay Antiproliferative activity against human MAVER-1 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay	[PMID: 29946150]
MCF7	GI₅₀	0.062 μM Compound: GSK3326595	Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay	[PMID: 29946150]
MDA-MB-231	GI₅₀	0.544 μM Compound: GSK3326595	Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay	[PMID: 29946150]
MDA-MB-453	GI₅₀	0.029 μM Compound: GSK3326595	Antiproliferative activity against human MDA-MB-453 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay Antiproliferative activity against human MDA-MB-453 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay	[PMID: 29946150]
MDA-MB-468	GI₅₀	0.057 μM Compound: GSK3326595	Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay	[PMID: 29946150]
NCI-H526	GI₅₀	0.275 μM Compound: GSK3326595	Antiproliferative activity against human NCI-H526 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay Antiproliferative activity against human NCI-H526 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay	[PMID: 29946150]
NU-DHL-1	GI₅₀	0.333 μM Compound: GSK3326595	Antiproliferative activity against human NU-DHL-1 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay Antiproliferative activity against human NU-DHL-1 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay	[PMID: 29946150]
Pfeiffer	GI₅₀	0.421 μM Compound: GSK3326595	Antiproliferative activity against human Pfeiffer cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay Antiproliferative activity against human Pfeiffer cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay	[PMID: 29946150]
RCK8	GI₅₀	0.529 μM Compound: GSK3326595	Antiproliferative activity against human RCK8 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay Antiproliferative activity against human RCK8 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay	[PMID: 29946150]
Rec1	GI₅₀	2.108 μM Compound: GSK3326595	Antiproliferative activity against human REC1 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay Antiproliferative activity against human REC1 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay	[PMID: 29946150]
RL	GI₅₀	0.014 μM Compound: GSK3326595	Antiproliferative activity against human RL cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay Antiproliferative activity against human RL cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay	[PMID: 29946150]
SCaBER	GI₅₀	0.198 μM Compound: GSK3326595	Antiproliferative activity against human SCaBER cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay Antiproliferative activity against human SCaBER cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay	[PMID: 29946150]
SF-295	GI₅₀	24.722 μM Compound: GSK3326595	Antiproliferative activity against human SF-295 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay Antiproliferative activity against human SF-295 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay	[PMID: 29946150]
SF-539	GI₅₀	0.061 μM Compound: GSK3326595	Antiproliferative activity against human SF-539 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay Antiproliferative activity against human SF-539 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay	[PMID: 29946150]
SK-BR-3	GI₅₀	0.073 μM Compound: GSK3326595	Antiproliferative activity against human SK-BR-3 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay Antiproliferative activity against human SK-BR-3 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay	[PMID: 29946150]
SUD4	GI₅₀	0.492 μM Compound: GSK3326595	Antiproliferative activity against human SU-DHL-4 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay Antiproliferative activity against human SU-DHL-4 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay	[PMID: 29946150]
SU-DHL10	GI₅₀	0.054 μM Compound: GSK3326595	Antiproliferative activity against human SU-DHL-10 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay Antiproliferative activity against human SU-DHL-10 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay	[PMID: 29946150]
SU-DHL-16	GI₅₀	0.099 μM Compound: GSK3326595	Antiproliferative activity against human SU-DHL-16 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay Antiproliferative activity against human SU-DHL-16 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay	[PMID: 29946150]
SU-DHL-2	GI₅₀	0.028 μM Compound: GSK3326595	Antiproliferative activity against human SUDHL2 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay Antiproliferative activity against human SUDHL2 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay	[PMID: 29946150]
SU-DHL-5	GI₅₀	0.028 μM Compound: GSK3326595	Antiproliferative activity against human SU-DHL-5 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay Antiproliferative activity against human SU-DHL-5 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay	[PMID: 29946150]
SU-DHL-6	GI₅₀	0.004 μM Compound: GSK3326595	Antiproliferative activity against human SU-DHL-6 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay Antiproliferative activity against human SU-DHL-6 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay	[PMID: 29946150]
SU-DHL-8	GI₅₀	0.053 μM Compound: GSK3326595	Antiproliferative activity against human SU-DHL-8 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay Antiproliferative activity against human SU-DHL-8 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay	[PMID: 29946150]
SW780	GI₅₀	0.29 μM Compound: GSK3326595	Antiproliferative activity against human SW780 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay Antiproliferative activity against human SW780 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay	[PMID: 29946150]
T-24	GI₅₀	0.765 μM Compound: GSK3326595	Antiproliferative activity against human T24 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay Antiproliferative activity against human T24 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay	[PMID: 29946150]
U-251	GI₅₀	1.798 μM Compound: GSK3326595	Antiproliferative activity against human U-251MG cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay Antiproliferative activity against human U-251MG cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay	[PMID: 29946150]
U2932	GI₅₀	0.053 μM Compound: GSK3326595	Antiproliferative activity against human U2932 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay Antiproliferative activity against human U2932 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay	[PMID: 29946150]
U-2940	GI₅₀	10.176 μM Compound: GSK3326595	Antiproliferative activity against human U-2940 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay Antiproliferative activity against human U-2940 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay	[PMID: 29946150]
U-87MG ATCC	GI₅₀	0.04 μM Compound: GSK3326595	Antiproliferative activity against human U-87 MG cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay Antiproliferative activity against human U-87 MG cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay	[PMID: 29946150]
U-937	GI₅₀	0.007 μM Compound: GSK3326595	Antiproliferative activity against human U-937 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay Antiproliferative activity against human U-937 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay	[PMID: 29946150]
UMUC3	GI₅₀	29.326 μM Compound: GSK3326595	Antiproliferative activity against human UMUC3 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay Antiproliferative activity against human UMUC3 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay	[PMID: 29946150]
WSUDLCL2	GI₅₀	0.082 μM Compound: GSK3326595	Antiproliferative activity against human WSUDLCL2 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay Antiproliferative activity against human WSUDLCL2 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay	[PMID: 29946150]
WSU-NHL	GI₅₀	0.008 μM Compound: GSK3326595	Antiproliferative activity against human WSU-NHL cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay Antiproliferative activity against human WSU-NHL cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay	[PMID: 29946150]
Z-138	GI₅₀	0.004 μM Compound: GSK3326595	Antiproliferative activity against human Z138 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay Antiproliferative activity against human Z138 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay	[PMID: 29946150]
ZR-75-1	GI₅₀	10.974 μM Compound: GSK3326595	Antiproliferative activity against human ZR-75-1 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay Antiproliferative activity against human ZR-75-1 cells assessed as cell growth inhibition incubated for 6 days by celltiter-glo assay	[PMID: 29946150]

In Vitro

GSK3326595 (10-100 nM, 24-72 h) inhibits SARS-CoV-2spike pseudovirus infection HEK-293 cells and A549 cells by attenuating ACE2-RBD interaction^[1].
GSK3326595 (100 nM, 12 h) primes peritoneal macrophages to IFN-gamma-induced M1 polarization^[3].
GSK3326595 (0.15-10 μM, 72 h) induces cell death in MCL cell^[4].

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

Western Blot Analysis^[4]

Cell Line:

HEK-293T cells, A549 cells
Concentration:

10 nM, 25 nM, 50 nM, 100 nM
Incubation Time:

48 h
Result:

Strongly inhibited ACE2-RBD interaction at low concentration.
Inhibited SARS-CoV-2 Omicron and other variants Spike1 binding with ACE2.
Inhibits SARS-CoV-2 spike pseudovirus infection host cells.

Cell Cytotoxicity Assay^[1]

Cell Line:

MCL cells
Concentration:

0.15 μM, 0.3 μM, 0.6 μM, 1.25 μM, 2.5 μM, 5 μM, 10 μM
Incubation Time:

72 h
Result:

Resulted in modest growth inhibition in MCL cells.

In Vivo

GSK3326595 (5 mg/kg, Intraperitoneal injection, three times a week for 9 weeks) increased hepatic triglyceride levels without affecting atherosclerosis in LDL receptor knockout mice^[3]. GSK3326595 (25-50 mg/kg, Oral, once a day for 2 weeks) enhances the efficacy of anti-programed cell death protein 1 (PD-1) immune checkpoint therapy (ICT) in hepatocellular carcinoma (HCC) in myelocytomatosis transgene turned on (MYC-ON) mice^[5].

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

Animal Model:

LDL receptor knockout mice^[3]
Dosage:

5 mg/kg
Administration:

Intraperitoneal injection (i.p.)
Result:

Did not alter atherosclerosis susceptibility.
Increased hepatic triglyceride levels without changing the hyperlipidemia extent.
Activated genes involved in fatty acid acquisition.

Animal Model:

myelocytomatosis transgene turned on mice^[5]
Dosage:

25 mg/kg, 50 mg/kg
Administration:

Oral
Result:

Significantly suppressed tumor growth at 50 mg/kg.
Showed better therapeutic efficacy at 25 mg/kg.

Ensayo clínico

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

No. CAS 1616392-22-3
Appearance Solid
Peso molecular 452.55
Fòrmula C₂₄H₃₂N₆O₃
Color White to light yellow
SMILES

O=C(C)N1CCC(NC2=NC=NC(C(NC[C@H](O)CN3CCC(C=CC=C4)=C4C3)=O)=C2)CC1
Synonyms

GSK3326595; EPZ015938
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (33)

All Cell Proliferation/Viability AssayWBIHC

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Journal Impact Factor

Gut

Identification of PRMT5 as a therapeutic target in cholangiocarcinoma. [Abstract]

2024 Sep 11:gutjnl-2024-332998. PMID: 39266051

Pemrametostat purchased from MedChemExpress. Usage Cited in: Gut. 2024 Sep 11:gutjnl-2024-332998. [Abstract]

GI₅₀ values for the PRMT5 inhibitors GSK3326595 and JNJ64619178 (Onametostat) in the indicated CCA cell lines.

Pemrametostat purchased from MedChemExpress. Usage Cited in: Gut. 2024 Sep 11:gutjnl-2024-332998. [Abstract]

Immunoblot analysis of PRMT5-dependent symmetric dimethylarginine (SMDA) protein marks in control and GSK3326595 or JNJ64619178 (Onametostat) treated HuCCT-1 and TFK-1 cells at the indicated doses for 5 days.

Pemrametostat purchased from MedChemExpress. Usage Cited in: Gut. 2024 Sep 11:gutjnl-2024-332998. [Abstract]

Immunohistochemical analysis of CK19 and H&E stainings showing the extent of CCA lesions in control Jnk^Δhepa+DEN+CCl4 and GSK3326595-treated mice. Representative images are shown.
Nat Commun

A BRET biosensor for measuring uncompetitive engagement of PRMT5 complexes in cells. [Abstract]

2025 Dec 3;16(1):10129. PMID: 41339334
Nat Commun

PRMT5-mediated arginine methylation activates AKT kinase to govern tumorigenesis. [Abstract]

2021 Jun 8;12(1):3444. PMID: 34103528

Pemrametostat purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Jun 8;12(1):3444. [Abstract]

Breast cancer cells are treated with DMSO, 0.5 μM GSK3326595 (GSK) for 4 days before examining cell viability.
J Adv Res

The aryl hydrocarbon receptor inhibits antigen presentation to promote progression of pancreatic ductal adenocarcinoma. [Abstract]

2025 Nov 5:S2090-1232(25)00874-4. PMID: 41203070
J Exp Clin Cancer Res

Flavokawain A is a natural inhibitor of PRMT5 in bladder cancer. [Abstract]

2022 Oct 5;41(1):293. PMID: 36199122
Adv Sci (Weinh)

Zinc Alleviates Gut Barrier Dysfunction by Promoting the Methylation of AKT. [Abstract]

2025 Sep;12(33):e08280. PMID: 40642900

Pemrametostat purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Sep;12(33):e08280. [Abstract]

HCT116 cells were treated with GSK3326595 (10 μM) for 6 h,HCT116 cells were starved in amino acid-free medium for 1 h, and then supplemented with ZnSO₄ for the indicated time. The level of pS473-AKT,binding
MedComm (2020)

SCR-7952, a highly selective MAT2A inhibitor, demonstrates synergistic antitumor activities in combination with the S-adenosylmethionine-competitive or the methylthioadenosine-cooperative protein arginine methyltransferase 5 inhibitors in methylthioadenosine phosphorylase-deleted tumors. [Abstract]

2024 Sep 20;5(10):e705. PMID: 39309689
Cell Death Dis

Reversible arginine methylation regulates mitochondrial IDH2 activity: coordinated control by CARM1 and KDM3A/4A. [Abstract]

2026 Feb 2;17(1):195. PMID: 41629283
Cancer Lett

DysUFMylation reprograms immunosuppressive neutrophils to potentiate anti-PD-1 therapy in hepatocellular carcinoma. [Abstract]

2026 May 1:645:218395. PMID: 41780840
Clin Cancer Res

MTA-Cooperative PRMT5 Inhibitors are Efficacious in MTAP-Deleted Malignant Peripheral Nerve Sheath Tumor Models. [Abstract]

2025 Jun 24. PMID: 40553452
Oncogene

BRD4 inhibition sensitizes cervical cancer to radiotherapy by attenuating DNA repair. [Abstract]

2021 Apr;40(15):2711-2724. PMID: 33712705
EMBO Mol Med

Nuclear PRMT5 is a biomarker of sensitivity to tamoxifen in ERα+ breast cancer. [Abstract]

2023 Aug 7;15(8):e17248. PMID: 37458145
Blood Adv

Loss of METTL3 attenuates blastic plasmacytoid dendritic cell neoplasm response to PRMT5 inhibition via IFN signaling. [Abstract]

2022 Apr 28;bloodadvances.2021006306. PMID: 35482445
Cell Mol Life Sci

Opposing USP19 splice variants in TGF-β signaling and TGF-β-induced epithelial-mesenchymal transition of breast cancer cells. [Abstract]

2023 Jan 17;80(2):43. PMID: 36646950
Biomed J

PRMT5-mediated methylation of LKB1 controls PD-L1 expression in NSCLC. [Abstract]

2026 Jun 10:101002. PMID: 42270077
EMBO Rep

Arginine methylation-dependent METTL14-SMN interaction regulates RNA m6A homeostasis. [Abstract]

2025 Oct 6. PMID: 41053315
Invest Ophthalmol Vis Sci

PRMT5 Regulates Senescence in Retinal Ganglion Cells by Targeting the Wnt/β-Catenin Signaling Cascade. [Abstract]

2025 Jun 2;66(6):8. PMID: 40459496
Transl Oncol

TNG908 is a brain-penetrant, MTA-cooperative PRMT5 inhibitor developed for the treatment of MTAP-deleted cancers. [Abstract]

2025 Feb:52:102264. PMID: 39756156
Sci Rep

Autophagy dictates sensitivity to PRMT5 inhibitor in breast cancer. [Abstract]

2023 Jul 3;13(1):10752. PMID: 37400460
Cancers (Basel)

TRAF6 Promotes PRMT5 Activity in a Ubiquitination-Dependent Manner. [Abstract]

2023 Apr 27;15(9):2501. PMID: 37173967
J Cell Mol Med

PRMT5 activates KLF5 by methylation to facilitate lung cancer. [Abstract]

2024 Mar;28(5):e17856. PMID: 37461162
J Biol Chem

Protein arginine methyltransferase 5 is essential for oncogene product EWSR1-ATF1-mediated gene transcription in clear cell sarcoma. [Abstract]

2022 Oct;298(10):102434. PMID: 36041632
Breast Cancer (Dove Med Press)

Therapeutic Advantage of Targeting PRMT5 in Combination with Chemotherapies or EGFR/HER2 Inhibitors in Triple-Negative Breast Cancers. [Abstract]

2023 Nov 6:15:785-799. PMID: 37954171
Mol Carcinog

PRMT1 inhibition promotes ferroptosis sensitivity via ACSL1 upregulation in acute myeloid leukemia. [Abstract]

2023 Aug;62(8):1119-1135. PMID: 37144835
Glycobiology

Compromised CDK12 activity causes dependency on the high activity of O-GlcNAc transferase. [Abstract]

2024 Dec 10;34(12):cwae081. PMID: 39361894
bioRxiv

2026 Apr 13.
bioRxiv

Radiation synergizes with BET inhibition to stimulate durable, systemic anti-tumor immunity in murine cancer models. [Abstract]

2026 Feb 18:2026.02.16.706212. PMID: 41757027
SSRN

2025 Dec 1.
Res Sq

2025 Jul 14.
bioRxiv

Ribosomal RNA transcription governs splicing through ribosomal protein RPL22. [Abstract]

2024 Aug 16:2024.08.15.608201. PMID: 39211199
Medical University of South Carolina

2023 Aug 12.
Research Square Print

November 11th, 2022.
Springer

2021 May 12.

Solvente y solubilidad

In Vitro:

DMSO : 62.5 mg/mL (138.11 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2097 mL

11.0485 mL

22.0970 mL

5 mM

0.4419 mL

2.2097 mL

4.4194 mL

10 mM

0.2210 mL

1.1049 mL

2.2097 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline

Solubility: ≥ 2.5 mg/mL (5.52 mM); Clear solution

Protocol 2

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (5.52 mM); Clear solution

Protocol 3

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: 2.08 mg/mL (4.60 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.08 mg/mL.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 4

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.08 mg/mL (4.60 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 5

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (4.60 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (283 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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]. Che Y, et al. Exploiting PRMT5 as a target for combination therapy in mantle cell lymphoma characterized by frequent ATM and TP53 mutations [J]. Blood cancer journal, 2023, 13(1): 27. [Content Brief]

[2]. Fedoriw A, et al. Anti-tumor activity of the type I PRMT inhibitor, GSK3368715, synergizes with PRMT5 inhibition through MTAP loss [J]. Cancer cell, 2019, 36(1): 100-114. e25.

[3]. Zhang Y, et al. PRMT5 inhibition induces pro‐inflammatory macrophage polarization and increased hepatic triglyceride levels without affecting atherosclerosis in mice [J]. Journal of Cellular and Molecular Medicine, 2023, 27(8): 1056-1068.

[4]. Li Z, et al. GSK3326595 is a promising drug to prevent SARS-CoV-2 Omicron and other variants infection by inhibiting ACE2-R671 di-methylation [J]. Journal of Medical Virology, 2023, 95(1): e28158.

[5]. Luo Y, et al. Myelocytomatosis-protein arginine N-methyltransferase 5 Axis defines the tumorigenesis and immune response in hepatocellular carcinoma [J]. Hepatology, 2021, 74(4): 1932-1951. [Content Brief]

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.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2097 mL	11.0485 mL	22.0970 mL	55.2425 mL
	5 mM	0.4419 mL	2.2097 mL	4.4194 mL	11.0485 mL
	10 mM	0.2210 mL	1.1049 mL	2.2097 mL	5.5243 mL
	15 mM	0.1473 mL	0.7366 mL	1.4731 mL	3.6828 mL
	20 mM	0.1105 mL	0.5524 mL	1.1049 mL	2.7621 mL
	25 mM	0.0884 mL	0.4419 mL	0.8839 mL	2.2097 mL
	30 mM	0.0737 mL	0.3683 mL	0.7366 mL	1.8414 mL
	40 mM	0.0552 mL	0.2762 mL	0.5524 mL	1.3811 mL
	50 mM	0.0442 mL	0.2210 mL	0.4419 mL	1.1049 mL
	60 mM	0.0368 mL	0.1841 mL	0.3683 mL	0.9207 mL
	80 mM	0.0276 mL	0.1381 mL	0.2762 mL	0.6905 mL
	100 mM	0.0221 mL	0.1105 mL	0.2210 mL	0.5524 mL

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