UNC1999
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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- Pureza: 99.87%
- No. CAS: 1431612-23-5
- Fòrmula: C33H43N7O2
- Peso molecular:569.74
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
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Publications Citing Use of MedChemExpress (MCE) UNC1999
More- Nat Commun. 2026 Feb 12;17(1):1214. [Abstract]
- Protein Cell. 2025 Jun 20;16(6):439-457. [Abstract]
- Carbohydr Polym. 2024 Dec 15:346:122645. [Abstract]
- Proc Natl Acad Sci U S A. 2019 Feb 19;116(8):2961-2966. [Abstract]
- Commun Biol. 2025 Dec 10;8(1):1772. [Abstract]
- Int J Mol Sci. 2022 Apr 1;23(7):3911. [Abstract]
- Biol Res. 2024 Nov 8;57(1):83. [Abstract]
- Transl Oncol. 2020 Oct;13(10):100819. [Abstract]
- Cytotherapy. 2024 Feb;26(2):136-144. [Abstract]
- 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.
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Ver todos los productos específicos de isoformas Histone Methyltransferase
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Actividad biológica
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EZH2 |
EZH1 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| DB | EC50 |
633 nM
Compound: Chemical Probe: UNC1999, 4
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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
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[PMID: 23614352] |
| MCF-10A | EC50 |
19.2 μM
Compound: 9; UNC1999
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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
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[PMID: 34378389] |
| MCF-10A | EC50 |
19200 nM
Compound: 21, UNC1999
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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
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[PMID: 25406853] |
| MCF-10A | EC50 |
19200 nM
Compound: Chemical Probe: UNC1999, 4
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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
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[PMID: 23614352] |
| MCF-10A | IC50 |
124 nM
Compound: 21, UNC1999
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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
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[PMID: 25406853] |
| MDA-MB-231 | IC50 |
14.69 μM
Compound: UNC1999
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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
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[PMID: 35623249] |
| MDA-MB-468 | IC50 |
7.67 μM
Compound: UNC1999
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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
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[PMID: 35623249] |
| Medulloblastoma cell | IC50 |
2.09 μM
Compound: Chemical Probe: UNC1999
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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
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[PMID: 32579914] |
| MV4-11 | EC50 |
524.8 nM
Compound: UNC1999
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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
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[PMID: 28741798] |
| RS4-11 | EC50 |
1956 nM
Compound: UNC1999
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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
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[PMID: 28741798] |
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 Ki 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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1431612-23-5
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Appearance Solid
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Peso molecular 569.74
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Fòrmula C33H43N7O2
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Color Off-white to light yellow
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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
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
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
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Most Recent
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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
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
2019 Feb 19;116(8):2961-2966. PMID: 30718431 -
Commun Biol
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.
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Biol Res
2024 Nov 8;57(1):83. PMID: 39511641 -
Transl Oncol
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 -
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Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocolo
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.
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.
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.
Pureza y Documentación
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Ficha de datos (281 KB)
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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)
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Instrucciones de manejo (2659 KB)
Referencias
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.
| 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 |
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