Art. -Nr.: HY-15646

UNC1999

16 Cited Publications

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Based on 16 publication(s) in Google Scholar

UNC1999, a chemical probe, is a SAM-competitive, potent and selective inhibitor of EZH2/1 with IC₅₀s of <10 nM and 45 nM, repectively.

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Reinheit: 99.87%
CAS. Nr.: 1431612-23-5
Formel: C₃₃H₄₃N₇O₂
Molecular Weight:569.74

Speicherung:

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

UNC1999 Chemical Structure

CAS. Nr.: 1431612-23-5

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Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (16)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

UNC1999, a chemical probe, is a SAM-competitive, potent and selective inhibitor of EZH2/1 with IC₅₀s of <10 nM and 45 nM, repectively.

IC₅₀ & Target

EZH2

EZH1

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
DB	EC₅₀	633 nM Compound: Chemical Probe: UNC1999, 4	Antiproliferative activity against human DB cells assessed as reduction in cell viability measured after 8 days by cell proliferation assay Antiproliferative activity against human DB cells assessed as reduction in cell viability measured after 8 days by cell proliferation assay	[PMID: 23614352]
MCF-10A	EC₅₀	19.2 μM Compound: 9; UNC1999	Cytotoxicity in human MCF-10A cells assessed as reduction in cell viability incubated for 72 hrs by resazurin assay Cytotoxicity in human MCF-10A cells assessed as reduction in cell viability incubated for 72 hrs by resazurin assay	[PMID: 34378389]
MCF-10A	EC₅₀	19200 nM Compound: 21, UNC1999	Cytotoxicity against human MCF10A cells assessed as cell viability by Alamar Blue assay Cytotoxicity against human MCF10A cells assessed as cell viability by Alamar Blue assay	[PMID: 25406853]
MCF-10A	EC₅₀	19200 nM Compound: Chemical Probe: UNC1999, 4	Cytotoxicity against human MCF-10A cells assessed as reduction in cell viability by alamar blue assay Cytotoxicity against human MCF-10A cells assessed as reduction in cell viability by alamar blue assay	[PMID: 23614352]
MCF-10A	IC₅₀	124 nM Compound: 21, UNC1999	Inhibition of EZH2 in human MCF10A cells assessed as reduction of H3K27me3 level after 72 hrs by Western blot analysis Inhibition of EZH2 in human MCF10A cells assessed as reduction of H3K27me3 level after 72 hrs by Western blot analysis	[PMID: 25406853]
MDA-MB-231	IC₅₀	14.69 μM Compound: UNC1999	Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 35623249]
MDA-MB-468	IC₅₀	7.67 μM Compound: UNC1999	Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 35623249]
Medulloblastoma cell	IC₅₀	2.09 μM Compound: Chemical Probe: UNC1999	Antiproliferative activity in Ptch1-deficient mouse medulloblastoma cell after 48 hrs by CCK-8 assay Antiproliferative activity in Ptch1-deficient mouse medulloblastoma cell after 48 hrs by CCK-8 assay	[PMID: 32579914]
MV4-11	EC₅₀	524.8 nM Compound: UNC1999	Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth	[PMID: 28741798]
RS4-11	EC₅₀	1956 nM Compound: UNC1999	Antiproliferative activity against human RS4-11 cells assessed as inhibition of cell growth Antiproliferative activity against human RS4-11 cells assessed as inhibition of cell growth	[PMID: 28741798]

In Vitro

UNC1999, the first orally bioavailable inhibitor that has high in vitro potency for wild-type and mutant EZH2 as well as EZH1, a closely related H3K27 methyltransferase that shares 96% sequence identity with EZH2 in their respective catalytic domains. UNC1999 is highly selective for EZH2 and EZH1 over a broad range of epigenetic and non-epigenetic targets, competitive with the cofactor SAM, and non-competitive with the peptide substrate. UNC1999 has K_i values of 4,700 nM, 65 nM, 300 nM, and 1,500 nM for sigma1, sigma2, histamine H₃, and NET, respectively. NC1999 selectively kills DB cells, a DLBCL cell line with the EZH2 Y641N mutation. UNC1999 displays a concentration- and time-dependent inhibition of DB cell proliferation (EC₅₀=633±101 nM (n=3))^[1].

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

In Vivo

A single intraperitoneal (IP) injection of UNC1999 at 15, 50, or 150 mg/kg achieved high C_max (9,700-11,800 nM) and exhibited dose linearity in male Swiss albino mice. Both the 150 and 50 mg/kg IP doses resulted in the plasma concentrations of UNC1999 above its cellular IC₅₀ over the entire 24 h period while the 15 mg/kg IP dose led to the plasma concentrations of UNC1999 above its cellular IC₅₀ for approximately 12 h. We next examined whether UNC1999 is orally bioavailable and are pleased to find that a single 50 mg/kg oral dose of UNC1999 achieved high C_max (4,700 nM) and good exposure levels in male Swiss albino mice. The plasma concentrations of UNC1999 are maintained above its cellular IC₅₀ for approximately 20 h following this single oral dose. It is worth noting that all doses including the 150 mg/kg IP dose are well tolerated by all test mice, and no adverse effects are observed^[1].

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

Chemical Information

CAS. Nr. 1431612-23-5
Appearance Solid
Molecular Weight 569.74
Formel C₃₃H₄₃N₇O₂
Color Off-white to light yellow
SMILES

O=C1C(CNC(C2=C(C=NN3C(C)C)C3=CC(C4=CN=C(N5CCN(C(C)C)CC5)C=C4)=C2)=O)=C(CCC)C=C(C)N1
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Publications (16)

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Journal Impact Factor

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
Protein Cell

Setd2 overexpression rescues bivalent gene expression during SCNT-mediated ZGA. [Abstract]

2025 Jun 20;16(6):439-457. PMID: 39945726
Carbohydr Polym

Chitosan/dextran-based organohydrogel delivers EZH2 inhibitor to epigenetically reprogram chemo/immuno-resistance in unresectable metastatic melanoma. [Abstract]

2024 Dec 15:346:122645. PMID: 39245506
Proc Natl Acad Sci U S A

MGMT-activated DUB3 stabilizes MCL1 and drives chemoresistance in ovarian cancer. [Abstract]

2019 Feb 19;116(8):2961-2966. PMID: 30718431
Commun Biol

Therapeutic targeting SPI1 in combination with erastin promotes ferroptosis in ccRCC. [Abstract]

2025 Dec 10;8(1):1772. PMID: 41372608
Int J Mol Sci

Dual Inhibition of H3K9me2 and H3K27me3 Promotes Tumor Cell Senescence without Triggering the Secretion of SASP. [Abstract]

2022 Apr 1;23(7):3911. PMID: 35409271

UNC1999 purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2022 Apr 1;23(7):3911. [Abstract]

Cell cycle analysis in MDA-MB-231 cell treated with UNC1999 (5 μM), UNC0642, and UNC1999+ UNC0642.

UNC1999 purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2022 Apr 1;23(7):3911. [Abstract]

Western blot analysis of expression of CyclinA2, H3K9me2, and H3K27me3 in MDA-MB-231 cells treated with UNC1999 (5 μM), UNC0642, and UNC1999+ UNC0642.

UNC1999 purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2022 Apr 1;23(7):3911. [Abstract]

qRT-PCR analysis of the expression of CyclinA2 in MDA-MB-231 cells treated with UNC1999 (5 μM), UNC0642, and UNC1999+ UNC0642.

UNC1999 purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2022 Apr 1;23(7):3911. [Abstract]

SA-β-Gal staining in MDA-MB-231 cells treated with UNC1999 (5 μM), UNC0642, and UNC1999+ UNC0642.

UNC1999 purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2022 Apr 1;23(7):3911. [Abstract]

Immunofluorescence analysis of Ki67 in MDA-MB-231 cells with UNC1999 (5 μM), UNC0642, and UNC1999+ UNC0642.
Biol Res

EZH1/2 plays critical roles in oocyte meiosis prophase I in mice. [Abstract]

2024 Nov 8;57(1):83. PMID: 39511641
Transl Oncol

The neural stem-cell marker CD24 is specifically upregulated in IDH-mutant glioma. [Abstract]

2020 Oct;13(10):100819. PMID: 32622311
Cytotherapy

Generation of human ILC3 from allogeneic and autologous CD34+ hematopoietic progenitors toward adoptive transfer. [Abstract]

2024 Feb;26(2):136-144. PMID: 38149947
bioRxiv

2026 May 1.
SSRN

2024 Mar 20.
McGill University

2023 Jul.
bioRxiv

2023 Nov 9.
Research Square Print

September 20th, 2022.
bioRxiv

May 10, 2022.
Patent

US20180263995A1.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (175.52 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

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

1.7552 mL

8.7759 mL

17.5519 mL

5 mM

0.3510 mL

1.7552 mL

3.5104 mL

10 mM

0.1755 mL

0.8776 mL

1.7552 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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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

Solubility: ≥ 2.25 mg/mL (3.95 mM); Clear solution

This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 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 2

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

Solubility: 2.25 mg/mL (3.95 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.25 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 (22.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

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

Solubility: 2.25 mg/mL (3.95 mM); Clear solution; Need warming

This protocol yields a clear solution of 2.25 mg/mL. 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 (22.5 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

Protokoll

Kinase Assay^[1]

EZH2 Y641N mutant is generated and assayed by BPS Bioscience. A series of dilutions of UNC1999 are prepared with 10% DMSO in HMT assay buffer and 5 μL of the dilution is added to a 50 μL reaction so that the final concentration of DMSO is 1% in all of reactions. All of the enzymatic reactions are conducted in duplicate at room temperature for 60 minutes (EZH2) and 180 minutes (EZH2 Y641N) in a 50 μL mixture containing HMT assay buffer, S-adenoslymethionine, enzyme, and UNC1999. These 50 μL reactions are carried out in wells of a HMT substrate pre-coated plate. After enzymatic reactions, the reaction mixtures are discarded and each of the wells is washed three times with TBST buffer, and slowly shaken with Blocking Buffer for 10 minutes. Wells are emptied, and 100 μL of diluted 1°antibody is added. The plate is then slowly shaken for 60 minutes at room temperature. As before, the plate is emptied and washed three times, and shaken with Blocking Buffer for 10 minutes at room temperature. After discarding the Blocking Buffer, 100 μL of diluted 2°antibody is added. The plate is then slowly shaken for 30 minutes at room temperature. As before, the plate is emptied and washed three times, and shaken with Blocking Buffer for 10 minutes at room temperature. Blocking Buffer is discarded and a mixture of the HRP chemiluminescent substrates is freshly prepared. 100 μL of this mixture is added to each empty well. Immediately, the luminescence of the samples is measured in a BioTek SynergyTM 2 microplate reader^[1].

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

Cell Assay^[1]

DB cells, a diffuse-large B-cell lymphoma cell line harboring the EZH2 Y641N mutation, are obtained from ATCC and cultured in RPMI 1640 supplemented with 10% fetal bovine serum, antibiotics, and various concentration of UNC1999 (0.1, 0.2, 0.3, 0.4, 0.5, 1, 2, 3, and 5 μM) or UNC2400 and DMSO control. The medium containing the test compound or control is refreshed every three days. The numbers of viable cells from at least three independent experiments are measured using TC20 automated cell counter system. Total histones are prepared from cell nuclei using an acidic extraction protocol. About 1 microgram of total histones is separated using 15% of SDS-PAGE, transferred to PVDF membranes, and probed with histone antibodies. Antibodies used in this study are those against EZH2, general H3, and H3K27me3^[1].

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

Animal Administration^[1]

Mice^[1]
Standard PK studies are conducted using male Swiss albino mice at Sai Life Sciences. Four doses (15, 50, and 150 mg/kg IP, and 50 mg/kg PO) of UNC1999 are evaluated. Each study lasted 24 h. Plasma concentrations of UNC1999 reported at each of the eight time points (0.08, 0.25, 0.5, 1, 2, 4, 8, and 24 h post dosing) are the average values from 3 test animals.

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 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)
Handling Instructions (2659 KB)

Verweise

[1]. Konze KD, et al. An Orally Bioavailable Chemical Probe of the Lysine Methyltransferases EZH2 and EZH1. ACS Chem Biol. 2013;8(6):1324-34. [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	1.7552 mL	8.7759 mL	17.5519 mL	43.8797 mL
	5 mM	0.3510 mL	1.7552 mL	3.5104 mL	8.7759 mL
	10 mM	0.1755 mL	0.8776 mL	1.7552 mL	4.3880 mL
	15 mM	0.1170 mL	0.5851 mL	1.1701 mL	2.9253 mL
	20 mM	0.0878 mL	0.4388 mL	0.8776 mL	2.1940 mL
	25 mM	0.0702 mL	0.3510 mL	0.7021 mL	1.7552 mL
	30 mM	0.0585 mL	0.2925 mL	0.5851 mL	1.4627 mL
	40 mM	0.0439 mL	0.2194 mL	0.4388 mL	1.0970 mL
	50 mM	0.0351 mL	0.1755 mL	0.3510 mL	0.8776 mL
	60 mM	0.0293 mL	0.1463 mL	0.2925 mL	0.7313 mL
	80 mM	0.0219 mL	0.1097 mL	0.2194 mL	0.5485 mL
	100 mM	0.0176 mL	0.0878 mL	0.1755 mL	0.4388 mL

Keywords

UNC1999

16 Cited Publications

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UNC1999

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Autophagy Compound Library

Reprogramming Compound Library

Chemical Probe Library

Anti-Blood Cancer Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

Epigenetics Compound Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Methylation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) UNC1999

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (16)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

UNC1999

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Autophagy Compound Library

Reprogramming Compound Library

Chemical Probe Library

Anti-Blood Cancer Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

Epigenetics Compound Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Methylation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) UNC1999

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (16)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

UNC1999 Related Classifications

HY-15646 Related Classifications