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Pinometostat

Catalog No. T3099   CAS 1380288-87-8
Synonyms: EPZ-5676

Pinometostat (EPZ-5676) has been used in trials studying the treatment of Leukemia, Acute Leukemias, Acute Myeloid Leukemia, Myelodysplastic Syndrome, and Acute Lymphocytic Leukemia, among others.

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Pinometostat Chemical Structure
Pinometostat, CAS 1380288-87-8
Pack Size Availability Price/USD Quantity
2 mg In stock $ 34.00
5 mg In stock $ 55.00
10 mg In stock $ 81.00
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1 mL * 10 mM (in DMSO) In stock $ 68.00
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Purity: 99.83%
Purity: 99.29%
Purity: 99.19%
Purity: 97.56%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Pinometostat (EPZ-5676) has been used in trials studying the treatment of Leukemia, Acute Leukemias, Acute Myeloid Leukemia, Myelodysplastic Syndrome, and Acute Lymphocytic Leukemia, among others.
Targets&IC50 DOT1L:80 pM(Ki)
Cell Research EPZ-5676 is dissolved in DMSO. To analyse inhibition of histone methylation in MV4-11 cells following EPZ-5676 treatment, extracted histones (400 ng) are fractionated on a 10-20% Tris HCl gels with Tris-Glycine SDS running buffer under denaturing conditions and transferred to nitrocellulose filters. Filters are cut into strips and incubated for 1 hour in blocking buffer at room temperature (RT) and then incubated overnight at 4°C in blocking buffer. Filters are washed 3 times for 5 minutes with wash buffer (Phosphate buffered saline (PBS) including 0.01% Tween 20 (PBST)) and incubated with infrared tagged secondary antibody at RT for 1 hour. Filters are washed in PBST and reprobed for 1 hour at RT with the appropriate total histone antibody control (mouse anti-histone H3 (1:20,000), CST 3638, or mouse anti-histone H4 (1:10,000), CST 2935). Filters are washed again in PBST and incubated with infrared tagged secondary antibody (IRDye 800Cw donkey-anti-mouse IgG (1:20,000), Li-Cor 926-32212) at RT for 1 hour. After a final ish in PBST, filters are scanned using the Odyssey infared imager (Li-cor). To analyse inhibition of H3K79 methylation in peripheral blood mononuclear cells (PBMCs) from rats dosed with EPZ-5676, 20 μL of PBMC whole cell lysate is fractionated on denaturing gels and analysed by immunoblotting with antibodies to H3K79me2 or total H3. Signal intensities specific for the H3K79me2 antibody and total histone H3 control antibody are quantified using Odyssey software. The H3K79me2 signal intensity is normalized by dividing it by the total histone H3 control signal intensity in the same lane.
Synonyms EPZ-5676
Molecular Weight 562.71
Formula C30H42N8O3
CAS No. 1380288-87-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 85 mg/mL (151.1 mM)

DMSO: 93 mg/mL (165.3 mM)

TargetMolReferences and Literature

1. Robert A. Protein methyltransferases in cancer. AACR Annual Meeting, 2013. 2. Pollock RM, 54th ASH Annual Meeting and Exposition, 2012, Abst 2379 3. Chen R, Xie W, Cai B, et al. Establishment and Identification of a CiPSC Lineage Reprogrammed from FSP-tdTomato Mouse Embryonic Fibroblasts (MEFs)[J]. Stem cells international. 2018 Dec 25;2018:5965727.

TargetMolCitations

1. Yu S, Zhou C, He J, et al. BMP4 drives primed to naïve transition through PGC-like state. Nature Communications. 2022, 13(1): 1-15 2. Chen R, Xie W, Cai B, et al. Establishment and Identification of a CiPSC Lineage Reprogrammed from FSP-tdTomato Mouse Embryonic Fibroblasts (MEFs). Stem Cells International. 2018 Dec 25;2018:5965727 3. Zhao X, Li X, Sun H, et al.Dot1l cooperates with Npm1 to repress endogenous retrovirus MERVL in embryonic stem cells.Nucleic Acids Research.2023: gkad640.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Clinical Compound Library Anti-Cancer Active Compound Library Highly Selective Inhibitor Library Anti-Cancer Drug Library Human Metabolite Library Chromatin Modification Compound Library Anti-COVID-19 Compound Library Bioactive Compound Library Bioactive Compounds Library Max Hematonosis Compound Library

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PRMT4-IN-3 EPZ020411 EEDi-5285 CARM1 degrader-1 WM-586 CPI-169 racemate MS049 UNC1215

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Keywords

Pinometostat 1380288-87-8 Chromatin/Epigenetic Histone Methyltransferase EPZ5676 Inhibitor EPZ-5676 inhibit EPZ 5676 inhibitor

 

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