UNC6852
Based on 5 publication(s) in Google Scholar
UNC6852 is a PRC2 PROTAC degrader, with a DC50 value of 0.79 μM for EED (HeLa), 0.3 μM for EZH2 (HeLa), and 0.59 μM for SUZ12 (DLBCL). UNC6852 binds to the WD40 aromatic cage of EED and CRL2-VHL, inducing proteasomal degradation of EED, EZH2 and SUZ12. UNC6852 reduces the level of H3K27me3 and exerts antiproliferative effects in cancer cells. UNC6852 can be used in studies related to diffuse large B-cell lymphoma, triple-negative breast cancer and prostate cancer.
(Pink: PRC2 ligand (HY-130979); Blue: VHL ligand (HY-125845); Black: linker (HY-N0067)).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.49%
- CAS 番号: 2688842-08-0
- 分子式: C43H48N10O6S
- 分子量:832.97
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 UNC6852
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Customer Validation & Images
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Bio/Physico-chemical Assay
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In Vivo Efficacy Study
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RT-PCR
PROTACs アイソフォーム固有の製品をすべて表示
MoreHistone Methyltransferase アイソフォーム固有の製品をすべて表示
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生物活性
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EZH2 0.3 μM (DC50) |
EZH2 Y641N 0.67 μM (DC50) |
EED 0.79 μM (DC50) |
SUZ12 0.59 μM (DC50) |
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Cell Line
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Type | Value | Description | References |
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| DB | EC50 |
3.4 μM
Compound: 71; UNC6852
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Antiproliferative activity against human DB cells assessed as viable cells with replenishment of medium with compound for every three days upto 9 days by trypan blue staining based automated bio-rad TC20 cell counter method
Antiproliferative activity against human DB cells assessed as viable cells with replenishment of medium with compound for every three days upto 9 days by trypan blue staining based automated bio-rad TC20 cell counter method
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[PMID: 35093670] |
| DB | EC50 |
3.4 μM
Compound: 71; UNC6852
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Antiproliferative activity against human DB cells measured after 9 days by tryphan blue staining
Antiproliferative activity against human DB cells measured after 9 days by tryphan blue staining
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[PMID: 35093670] |
| Pfeiffer | EC50 |
0.41 μM
Compound: 71; UNC6852
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Antiproliferative activity against human Pfeiffer cells assessed as viable cells with replenishment of medium with compound for every three days upto 6 days by trypan blue staining based automated bio-rad TC20 cell counter method
Antiproliferative activity against human Pfeiffer cells assessed as viable cells with replenishment of medium with compound for every three days upto 6 days by trypan blue staining based automated bio-rad TC20 cell counter method
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[PMID: 35093670] |
| Pfeiffer | IC50 |
0.41 μM
Compound: 71; UNC6852
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Antiproliferative activity against human Pfeiffer cells measured after 3 days by tryphan blue staining
Antiproliferative activity against human Pfeiffer cells measured after 3 days by tryphan blue staining
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[PMID: 35093670] |
UNC6852 potently binds to the WD40 domain of recombinant EED, with an IC50 of 247 nM[1].
UNC6852 (0.1-30 μM; 2-72 h) degrades PRC2 components EED, EZH2 and SUZ12 in a dose- and time-dependent manner in HeLa cells via the VHL-dependent proteasome-mediated pathway, with a DC50 value of 0.79 μM for EED and 0.3 μM for EZH2[1].
UNC6852 (10 μM; 72 h) reduces the level of H3K27me3 by 51% in HeLa cells, accompanied by the degradation of EED and EZH2[1].
UNC6852 degrades core PRC2 components in Pfeiffer diffuse large B-cell lymphoma (DLBCL) cells harboring the gain-of-function EZH2A677G mutation[1].
UNC6852 (0.1-30 μM; 24-72 h) dose-dependently degrades EED, EZH2/EZH2Y641N and SUZ12 in double-hit diffuse large B-cell lymphoma (DLBCL) cells (with DC50 values of 0.61 μM, 0.67 μM and 0.59 μM, respectively), and reduces H3K27me3 levels by 71% after 72 h[1].
UNC6852 (0.1-10 μM; 6-12 days) potently inhibits the proliferation of DB DLBCL cells (EC50 = 3.4 μM at day 9) and Pfeiffer DLBCL cells (EC50 = 0.41 μM at day 6)[1].
UNC6852 (6.25 μM; 48 h) degrades EZH2 and EED in MDA-MB-231 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HeLa cells
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Concentration:0.1, 0.5, 1, 3, 5, 10, 20, 30 μM
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Incubation Time:2, 4, 8, 10, 16, 20, 24, 48, 72 h
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Result:Induced 80% degradation of EED and 76% degradation of EZH2 at 5 μM for 24 h.
Achieved half-maximal degradation (DC50) of EED at 0.79 μM (maximal degradation [Dₘₐₓ] = 92%) and of EZH2 at 0.3 μM (Dₘₐₓ = 75%) in dose-response testing at 24 h.
Resulted in an apparent half-life (t1/2) of 0.81 hours for EED and 1.92 hours for EZH2 in time-course testing at 10 μM.
Degraded SUZ12 to a lesser extent, with a Dₘₐₓ of 22% (no DC50 or t1/2 calculable).
Showed no cellular toxicity at concentrations up to 30 μM.
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Cell Line:HeLa cells
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Concentration:10 μM
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Incubation Time:24, 72, 96 h
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Result:Reduced H3K27me3 levels by 51% after 72 h, with a further decrease observed at 96 h.
Showed a reduction comparable to that induced by EED226 and UNC1999, while only UNC6852 reduced EED and EZH2 protein levels.
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Cell Line:MDA-MB-231 triple negative breast cancer cells
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Concentration:0.1, 0.5, 1, 2.5, 5 μM
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Incubation Time:48 h
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Result:Reduces EZH2 and EED protein levels in a dose-dependent manner.
Fails to reduce protein levels of NF-κB factors RelA and RelB at any tested concentration.
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Cell Line:22Rv1 castration-resistant prostate cancer cells
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Concentration:2.5 μM
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Incubation Time:24 h
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Result:Did not significantly reduce the expression of EZH2:AR:AR-V7-co-activated oncogenes (including PRC1, CDK2, TMPRSS2, HMGB1, PDIA4, LBR, TRRG1L, MYBL2, CORO1C, ITPR3, EGFR) relative to DMSO-treated controls.
化学情報
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CAS 番号 2688842-08-0
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性状 Solid
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分子量 832.97
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分子式 C43H48N10O6S
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Color Light yellow to yellow
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SMILES
O=C(C1=CC=C(C=C1)C2=CN=C(N3C2=NN=C3)NCC4=CC=CO4)NCCCC(N[C@H](C(N5[C@@H](C[C@H](C5)O)C(NCC6=CC=C(C=C6)C7=C(N=CS7)C)=O)=O)C(C)(C)C)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (5)
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Journal Impact Factor
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Most Recent
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Cell
2026 Jun 11;189(12):3541-3552.e18. PMID: 41999746 -
Sci Rep
Knockdown screening of chromatin binding and regulatory proteins in zebrafish identified Suz12b as a regulator of tfpia and an antithrombotic drug target. [Abstract]2021 Jul 27;11(1):15238. PMID: 34315984
UNC6852 purchased from MedChemExpress. Usage Cited in: Sci Rep. 2021 Jul 27;11(1):15238. [Abstract]
Comparison of time to occlusion of the caudal vein after laser injury between wild-type control 5 dpf larvae and UNC6852-injected larvae by one-way ANOVA. The x-axis represents four different concentrations of the UNC6852 (0.075 mM, 0.15 mM, 0.3 mM and 0.6 mM) (2 h) used for larval injections. The dot plots represent wild-type larvae (closed circles) and the knockdown larvae (closed triangles).
UNC6852 purchased from MedChemExpress. Usage Cited in: Sci Rep. 2021 Jul 27;11(1):15238. [Abstract]
Quantitative real-time PCR showing the fold change of tfpia gene expression in liver and spleen for UNC6852 (6 h)-injected adult zebrafish with wild-type control by Student’ s t test. The concentration of UNC6852 used for adult injections (0.6 mM) was indicated beneath the bar graph.
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bioRxiv
Dual EZH1/2 inhibition enhances DNMT inhibitor efficacy in colon cancer through targeting H3K27me1. [Abstract]2025 Sep 18:2025.09.16.676613. PMID: 41000734
UNC6852 purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 Sep 18:2025.09.16.676613. [Abstract]
NLuc reporter activity measurements following 72-hour treatment with the indicated SAM-competitive EZH inhibitors or other PRC2 inhibitors, including EED inhibitors and EZH2 or EED PROTACs (UNC6852) (5-10 μM; 72 h).
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溶剤 & 溶解度
DMSO : 100 mg/mL (120.05 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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: ≥ 5 mg/mL (6.00 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (6.00 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
純度とドキュメンテーション
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データシート (282 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
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- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Potjewyd F, et al. Degradation of Polycomb Repressive Complex 2 with an EED-Targeted Bivalent Chemical Degrader. Cell chemical biology. 2020 Jan 16;27(1):47-56.e15. [Content Brief]
[2]. Dardis GJ, et al. An EZH2-NF-κB regulatory axis drives expression of pro-oncogenic gene signatures in triple negative breast cancer. iScience. 2023 Jul 21;26(7):107115. [Content Brief]
[3]. Wang J, et al. A cryptic transactivation domain of EZH2 binds AR and AR's splice variant, promoting oncogene activation and tumorous transformation. Nucleic acids research. 2022 Oct 28;50(19):10929-10946. [Content Brief]
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 | 1.2005 mL | 6.0026 mL | 12.0052 mL | 30.0131 mL |
| 5 mM | 0.2401 mL | 1.2005 mL | 2.4010 mL | 6.0026 mL | |
| 10 mM | 0.1201 mL | 0.6003 mL | 1.2005 mL | 3.0013 mL | |
| 15 mM | 0.0800 mL | 0.4002 mL | 0.8003 mL | 2.0009 mL | |
| 20 mM | 0.0600 mL | 0.3001 mL | 0.6003 mL | 1.5007 mL | |
| 25 mM | 0.0480 mL | 0.2401 mL | 0.4802 mL | 1.2005 mL | |
| 30 mM | 0.0400 mL | 0.2001 mL | 0.4002 mL | 1.0004 mL | |
| 40 mM | 0.0300 mL | 0.1501 mL | 0.3001 mL | 0.7503 mL | |
| 50 mM | 0.0240 mL | 0.1201 mL | 0.2401 mL | 0.6003 mL | |
| 60 mM | 0.0200 mL | 0.1000 mL | 0.2001 mL | 0.5002 mL | |
| 80 mM | 0.0150 mL | 0.0750 mL | 0.1501 mL | 0.3752 mL | |
| 100 mM | 0.0120 mL | 0.0600 mL | 0.1201 mL | 0.3001 mL |
UNC6852 関連分類
HY-130708 関連分類
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