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Pinometostat

(Synonyms: EPZ-5676)

33 Cited Publications

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Based on 33 publication(s) in Google Scholar

Pinometostat (EPZ-5676) is a potent DOT1L histone methyltransferase inhibitor with a K_i of 80 pM.

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Pureza: 99.93%
No. CAS: 1380288-87-8
Fòrmula: C₃₀H₄₂N₈O₃
Peso molecular:562.71

Almacenamiento:

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

Pinometostat Chemical Structure

No. CAS: 1380288-87-8

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Top Publications Citing

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
Protocolo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

Pinometostat (EPZ-5676) is a potent DOT1L histone methyltransferase inhibitor with a K_i of 80 pM.

IC₅₀ & Target

DOT1L

Ver todos los productos específicos de isoformas Histone Methyltransferase :

Cellular Effect

Cell Line	Type	Value	Description	References
HeLa	IC₅₀	7 nM Compound: EPZ-5676	Inhibition of DOT1L in human HeLa cells assessed as reduction in H3K79me2 level after 72 hrs by ELISA Inhibition of DOT1L in human HeLa cells assessed as reduction in H3K79me2 level after 72 hrs by ELISA	[PMID: 28337327]
K562	IC₅₀	31 μM Compound: EPZ5676	Anticancer activity against human K562 cells assessed as inhibition of cell growth treated for 8 days measured by CCK-8 kit method Anticancer activity against human K562 cells assessed as inhibition of cell growth treated for 8 days measured by CCK-8 kit method	[PMID: 35612819]
KOPN-8	IC₅₀	0.06 μM Compound: EPZ5676	Anticancer activity against human KOPN-8 cells harbouring MLL-ENL assessed as inhibition of cell growth treated for 8 days measured by CCK-8 kit method Anticancer activity against human KOPN-8 cells harbouring MLL-ENL assessed as inhibition of cell growth treated for 8 days measured by CCK-8 kit method	[PMID: 35612819]
MOLM-13	EC₅₀	0.004 μM Compound: 23, EPZ-5676	Antiproliferative activity against human MOLM13 cells containing MLL-AF9 Antiproliferative activity against human MOLM13 cells containing MLL-AF9	[PMID: 23879463]
MOLM-13	IC₅₀	0.03 μM Compound: EPZ5676	Anticancer activity against human MOLM-13 cells harbouring MLL-AF9 assessed as inhibition of cell growth treated for 8 days measured by CCK-8 kit method Anticancer activity against human MOLM-13 cells harbouring MLL-AF9 assessed as inhibition of cell growth treated for 8 days measured by CCK-8 kit method	[PMID: 35612819]
MOLM-13	IC₅₀	21 nM Compound: EPZ5676	Anticancer activity against human MOLM-13 cells harbouring MLL-AF9 assessed as inhibition of cell growth treated for 9 days measured by CCK-8 kit method Anticancer activity against human MOLM-13 cells harbouring MLL-AF9 assessed as inhibition of cell growth treated for 9 days measured by CCK-8 kit method	[PMID: 35612819]
MOLM-13	IC₅₀	227 nM Compound: EPZ5676	Anticancer activity against human MOLM-13 cells harbouring MLL-AF9 assessed as inhibition of cell growth treated for 4 days measured by CCK-8 kit method Anticancer activity against human MOLM-13 cells harbouring MLL-AF9 assessed as inhibition of cell growth treated for 4 days measured by CCK-8 kit method	[PMID: 35612819]
MOLM-13	IC₅₀	59 nM Compound: EPZ5676	Anticancer activity against human MOLM-13 cells harbouring MLL-AF9 assessed as inhibition of cell growth treated for 7 days measured by CCK-8 kit method Anticancer activity against human MOLM-13 cells harbouring MLL-AF9 assessed as inhibition of cell growth treated for 7 days measured by CCK-8 kit method	[PMID: 35612819]
MOLM-13	IC₅₀	73 nM Compound: EPZ5676	Anticancer activity against human MOLM-13 cells harbouring MLL-AF9 assessed as inhibition of cell growth treated for 6 days measured by CCK-8 kit method Anticancer activity against human MOLM-13 cells harbouring MLL-AF9 assessed as inhibition of cell growth treated for 6 days measured by CCK-8 kit method	[PMID: 35612819]
MOLM-13	IC₅₀	97 nM Compound: EPZ5676	Anticancer activity against human MOLM-13 cells harbouring MLL-AF9 assessed as inhibition of cell growth treated for 5 days measured by CCK-8 kit method Anticancer activity against human MOLM-13 cells harbouring MLL-AF9 assessed as inhibition of cell growth treated for 5 days measured by CCK-8 kit method	[PMID: 35612819]
MV4-11	EC₅₀	0.004 μM Compound: 23, EPZ-5676	Antiproliferative activity against human MV4-11 cells containing MLL-AF4 Antiproliferative activity against human MV4-11 cells containing MLL-AF4	[PMID: 23879463]
MV4-11	IC₅₀	0.05 μM Compound: EPZ5676	Anticancer activity against human MV4-11 cells assessed as inhibition of cell growth treated for 8 days measured by CCK-8 kit method Anticancer activity against human MV4-11 cells assessed as inhibition of cell growth treated for 8 days measured by CCK-8 kit method	[PMID: 35612819]
MV4-11	IC₅₀	15 nM Compound: EPZ-5676	Antiproliferative activity against human MV4-11 cells harboring MLL-AF4 treated for 6 hrs measured after 8 days by Celltiter-Glo reagent based assay Antiproliferative activity against human MV4-11 cells harboring MLL-AF4 treated for 6 hrs measured after 8 days by Celltiter-Glo reagent based assay	[PMID: 28337327]
MV4-11	IC₅₀	3 nM Compound: 38, EPZ-5676	Inhibition of DOT1L in human MV4-11 cells expressing MLL-AF4 assessed as reduction of H3K79me2 level after 4 days by ELISA method Inhibition of DOT1L in human MV4-11 cells expressing MLL-AF4 assessed as reduction of H3K79me2 level after 4 days by ELISA method	[PMID: 25406853]
MV4-11	IC₅₀	3.5 nM Compound: 38, EPZ-5676	Inhibition of DOT1L in human MV4-11 cells expressing MLL-AF4 assessed as cell growth inhibition after 14 days by Guava Viacount assay Inhibition of DOT1L in human MV4-11 cells expressing MLL-AF4 assessed as cell growth inhibition after 14 days by Guava Viacount assay	[PMID: 25406853]
RS4-11	IC₅₀	0.07 μM Compound: EPZ5676	Anticancer activity against human RS4-11 cells assessed as inhibition of cell growth treated for 8 days measured by CCK-8 kit method Anticancer activity against human RS4-11 cells assessed as inhibition of cell growth treated for 8 days measured by CCK-8 kit method	[PMID: 35612819]
THP-1	EC₅₀	0.004 μM Compound: 23, EPZ-5676	Antiproliferative activity against human THP1 cells containing MLL-AF9 Antiproliferative activity against human THP1 cells containing MLL-AF9	[PMID: 23879463]

In Vitro

Pinometostat (EPZ-5676) inhibits H3K79me2 with IC₅₀ values of 3 nM and 5 nM in MV4-11 and HL60 cells, respectively. Pinometostat (EPZ-5676) is a potent inhibitor of MV4-11 proliferation with an IC₅₀ value of 3.5 nM^[1]. Pinometostat (EPZ-5676) induces a synergistic and durable antiproliferative effect, increases expression of differentiation markers and apoptosis as single agent, and demonstrates combination benefit in combination with AML standard of care drugs in MLL-r cells^[2].

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

In Vivo

Pinometostat (EPZ-5676) (70 mg/kg, i.p.) causes complete and sustained regression in a rat xenograft model of MLL-rearranged leukemia. Pinometostat (EPZ-5676) (70, 35 mg/kg, i.v.) reduces HOXA9 and MEIS1 mRNA levels of tumors taken from rats, and reduces MLL-fusion target gene expression in vivo^[1].

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

Ensayo clínico

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

Chemical Information

No. CAS 1380288-87-8
Appearance Solid
Peso molecular 562.71
Fòrmula C₃₀H₄₂N₈O₃
Color White to light yellow
SMILES

NC1=NC=NC2=C1N=CN2[C@H]3[C@H](O)[C@H](O)[C@@H](CN([C@@H]4C[C@H](CCC5=NC6=C(C=CC(C(C)(C)C)=C6)N5)C4)C(C)C)O3
Synonyms

EPZ-5676
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 Assay2D/3D Cell Culture and DifferentiationWBRT-PCR

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Journal Impact Factor

Cell

p53 safeguards chemical reprogramming of human somatic cells toward pluripotency. [Abstract]

2026 Jun 11;189(12):3541-3552.e18. PMID: 41999746
Cancer Discov

KAT6A and ENL Form an Epigenetic Transcriptional Control Module to Drive Critical Leukemogenic Gene-Expression Programs. [Abstract]

2022 Mar 1;12(3):792-811. PMID: 34853079
Blood

DOT1L Shapes ncPRC1-Target Gene Repression to Maintain Germinal Center B Cell Identity of Diffuse Large B cell Lymphoma. [Abstract]

2026 May 29:blood.2025031615. PMID: 42213647
Cell Stem Cell

Highly efficient and rapid generation of human pluripotent stem cells by chemical reprogramming. [Abstract]

2023 Apr 6;30(4):450-459.e9. PMID: 36944335

Pinometostat purchased from MedChemExpress. Usage Cited in: Cell Stem Cell. 2023 Apr 6;30(4):450-459.e9. [Abstract]

Number of hCiPSC colonies induced from hADSCs (hADSCs-0618) with stage II condition (SII, 12 days treatment) or SII plus EPZ5676 (E; 2 μM) and DZNep (Z) using the four-stage protocol.
Nat Cell Biol

KDM6A epigenetically regulates subtype plasticity in small cell lung cancer. [Abstract]

2023 Sep;25(9):1346-1358. PMID: 37591951

Pinometostat purchased from MedChemExpress. Usage Cited in: Nat Cell Biol. 2023 Sep;25(9):1346-1358. [Abstract]

Immunoblot analysis of 1014 Kdm6a isogenic cells treated with inhibitors that block the function of epigenetic modifiers that normally maintain gene expression including VTP50469 (500 nM), EPZ-5676 (1 μM), PF-9363 (100 nM), JQAD1 or DMSO for 6 days.
Nat Commun

Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]

2026 Feb 12;17(1):1214. PMID: 41680175
Nat Commun

TET2 deficiency increases the competitive advantage of hematopoietic stem and progenitor cells through upregulation of thrombopoietin receptor signaling. [Abstract]

2025 Mar 10;16(1):2384. PMID: 40064887

Pinometostat purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Mar 10;16(1):2384. [Abstract]

Count of Annexin V negative Tet2^KO or Tet2^WT HPC^HOXB4 cells treated with Pinometostat (1μM; 0-20 days) over time normalized to the corresponding untreated sample.
Sci Adv

Gain-of-function mutations in the catalytic domain of DOT1L promote lung cancer malignant phenotypes via the MAPK/ERK signaling pathway. [Abstract]

2023 Jun 2;9(22):eadc9273. PMID: 37256945

Pinometostat purchased from MedChemExpress. Usage Cited in: Sci Adv. 2023 Jun 2;9(22):eadc9273. [Abstract]

H3K79me2 levels in HCI-H460 cells expressing WT or R231Q DOT1L after treatment with different concentrations (0, 0.5, and 5 μM, 9 days) of DOT1Lis (SGC0946, EPZ004777, and EPZ5676).
Hum Reprod Open

Human iPSCs derived from cryopreserved testicular somatic cells enable germline regeneration in childhood cancer survivors. [Abstract]

2026 Jun 3;2026(3):hoag054. PMID: 42389191
Cell Death Dis

Targeting EHMT2 reverses EGFR-TKI resistance in NSCLC by epigenetically regulating the PTEN/AKT signaling pathway. [Abstract]

2018 Jan 26;9(2):129. PMID: 29374157
Int J Biol Macromol

Multi omics analysis reveals senescence associated genes in metabolic dysfunction associated steatohepatitis related liver cancer and their functional validation. [Abstract]

2026 Apr:358:151713. PMID: 41933769
Acta Pharmacol Sin

P300/CBP inhibition sensitizes mantle cell lymphoma to PI3Kδ inhibitor idelalisib. [Abstract]

2022 Feb;43(2):457-469. PMID: 33850273
Phytomedicine

Hesperetin promotes DOT1L degradation and reduces histone H3K79 methylation to inhibit gastric cancer metastasis. [Abstract]

2021 Apr:84:153499. PMID: 33667841
Cell Syst

A Library of Phosphoproteomic and Chromatin Signatures for Characterizing Cellular Responses to Drug Perturbations. [Abstract]

2018 Apr 25;6(4):424-443.e7. PMID: 29655704
Oncogene

Dual function of DOT1L suppresses tumor cell-intrinsic immunogenicity in hepatocellular carcinoma. [Abstract]

2026 May;45(16):1484-1500. PMID: 41912776
Cell Rep

Chemical-induced epigenome resetting for regeneration program activation in human cells. [Abstract]

2023 May 23;42(6):112547. PMID: 37224020
Cell Rep

Oxidized mC modulates synthetic lethality to PARP inhibitors for the treatment of leukemia. [Abstract]

2023 Jan 31;42(1):112027. PMID: 36848231
Cell Rep

DOT1L O-GlcNAcylation promotes its protein stability and MLL-fusion leukemia cell proliferation. [Abstract]

2021 Sep 21;36(12):109739. PMID: 34551297
Oncogenesis

Disruptor of telomeric silencing 1-like promotes ovarian cancer tumor growth by stimulating pro-tumorigenic metabolic pathways and blocking apoptosis. [Abstract]

2021 Jul 12;10(7):48. PMID: 34253709
Transl Psychiatry

Non-gene-edited neural stem cells reverse neuroinflammation and microbiota dysbiosis in a sprague-dawley rat model of autism spectrum disorder. [Abstract]

2026 Apr 1;16(1):275. PMID: 41922322
BMC Cancer

Identification of epigenetic factors regulating the mesenchyme to epithelium transition by RNA interference screening in breast cancer cells. [Abstract]

2016 Aug 31;16(1):700. PMID: 27581651

Pinometostat purchased from MedChemExpress. Usage Cited in: BMC Cancer. 2016 Aug 31;16(1):700. [Abstract]

Pharmacological inhibition of DOT1L induces E-cadherin and CD24 expression in MDA-MB-231 in vitro. Cells are treated with dose effects of EPZ-5676 (0.1 μM, 1 μM, 10 μM) or 0.1 % DMSO for the indicated days, followed by mRNA extraction and RT-qPCR with specific primers.
Genes (Basel)

CHIR99021 and Brdu Are Critical in Chicken iPSC Reprogramming via Small-Molecule Screening. [Abstract]

2024 Sep 13;15(9):1206. PMID: 39336797
bioRxiv

2026 Jan 17.
University of Groningen

2025 Jul 4.
bioRxiv

2025 May 02.
Patent

US20240335438A1.
biorxiv

2024 Jun 08.
Research Square Preprint

2023 May 26.
Research Square Preprint

2022 May.
University of Pennsylvania

2022 Jan 1.
bioRxiv

2020 Jun.
bioRxiv

2019 Nov.
Patent

US20180263995A1.

Solvente y solubilidad

In Vitro:

DMSO : 100 mg/mL (177.71 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : 100 mg/mL (177.71 mM; Need ultrasonic)

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

1.7771 mL

8.8856 mL

17.7711 mL

5 mM

0.3554 mL

1.7771 mL

3.5542 mL

10 mM

0.1777 mL

0.8886 mL

1.7771 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: 10% DMSO 40% PEG300 5% Tween-80 45% Saline