GSK3326595 (Synonyms: EPZ015938)

Name: GSK3326595
Brand: MedChemExpress
SKU: HY-101563
Rating: 5.0 (31 reviews)

Cat. No.: HY-101563 Purity: 99.82%: Data Sheet
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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.

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CAS No. : 1616392-22-3

사이즈	재고	수량

무료 샘플 (0.1 - 0.2 mg)	지금 신청하기
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	해외재고보유	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	해외재고보유	Estimated Time of Arrival: December 31
Solid
5 mg	해외재고보유	Estimated Time of Arrival: December 31
10 mg	해외재고보유	Estimated Time of Arrival: December 31
25 mg	해외재고보유	Estimated Time of Arrival: December 31
50 mg	해외재고보유	Estimated Time of Arrival: December 31
100 mg	해외재고보유	Estimated Time of Arrival: December 31
200 mg	해외재고보유	Estimated Time of Arrival: December 31
1 g	해외재고보유	Estimated Time of Arrival: December 31
5 g	견적 받기
10 g	견적 받기

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고객리뷰

Based on 31 publication(s) in Google Scholar

Other Forms of GSK3326595:

GSK3326595 (Standard) 견적 받기

31 Publications Citing Use of MCE GSK3326595

Cell Proliferation/Viability Assay

IHC

: GSK3326595 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

: GSK3326595 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.

: GSK3326595 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.

: GSK3326595 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.

: GSK3326595 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.

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms

EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 NSD3/WHSC1L1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

View All CDK Isoform Specific Products:

View All Isoforms

CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

Biological Activity
순도&문서
References
고객리뷰

제품 설명

IC₅₀ & Target

PRMT5

CDK4

CDK6

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	IC₅₀	189 1 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	189 1 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]
5637	GI₅₀	0.069 3 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]
HCT-116	IC₅₀	237 1 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]
HCT-116	IC₅₀	237 1 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]
A 172	GI₅₀	1.167 3 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 3 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 3 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 3 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 3 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 3 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 1 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 1 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 3 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 3 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]
JM1	GI₅₀	0.079 3 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 3 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]
JeKo-1	GI₅₀	5.402 3 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]
KMS-11	GI₅₀	0.066 3 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 3 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 3 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]
MCF7	GI₅₀	0.062 3 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 3 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 3 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 3 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]
Maver1	GI₅₀	0.085 3 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]
NCI-H526	GI₅₀	0.275 3 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 3 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 3 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 3 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]
RL	GI₅₀	0.014 3 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]
Rec1	GI₅₀	2.108 3 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]
SCaBER	GI₅₀	0.198 3 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 3 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 3 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 3 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]
SU-DHL-16	GI₅₀	0.099 3 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 3 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 3 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 3 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 3 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]
SU-DHL10	GI₅₀	0.054 3 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]
SUD4	GI₅₀	0.492 3 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]
SW780	GI₅₀	0.29 3 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 3 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 3 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]
U-2940	GI₅₀	10.176 3 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 3 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 3 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]
U2932	GI₅₀	0.053 3 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]
UMUC3	GI₅₀	29.326 3 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]
WSU-NHL	GI₅₀	0.008 3 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]
WSUDLCL2	GI₅₀	0.082 3 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]
Z-138	GI₅₀	0.004 3 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 3 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.

Clinical Trial

분자량

452.55

화학식

C₂₄H₃₂N₆O₃

CAS No.

1616392-22-3

Appearance

Solid

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

선적

Room temperature in continental US; may vary elsewhere.

보관

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

용액&용해도

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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.

몰농도 계산기
농도 희석 계산기

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

순도&문서

Purity: 99.83%

Select Batch:

Data Sheet (277 KB) SDS (393 KB)

COA (244 KB) LCMS (93 KB) Elemental Analysis Report (102 KB)

Handling Instructions (2659 KB)

References

[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]

Complete Stock Solution Preparation Table

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

GSK3326595 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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GSK3326595 (Synonyms: EPZ015938)

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Other Forms of GSK3326595:

31 Publications Citing Use of MCE GSK3326595

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GSK3326595 Related Classifications

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GSK3326595 (Synonyms: EPZ015938)

고객리뷰

Other Forms of GSK3326595:

GSK3326595 Related Antibodies

31 Publications Citing Use of MCE GSK3326595

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Histone Methyltransferase Isoform Specific Products:

View All CDK Isoform Specific Products:

Biological Activity

순도&문서

References

고객리뷰

GSK3326595 Related Antibodies

몰농도 계산기

농도 희석 계산기

Complete Stock Solution Preparation Table

GSK3326595 Related Classifications

Keywords:

최근 본 상품:

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