| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg | |||
| 250mg | |||
| Other Sizes |
| Targets |
UNC6852 targets the polycomb repressive complex 2 (PRC2), specifically the EED subunit. By recruiting VHL E3 ubiquitin ligase to EED, it induces the ubiquitination and proteasomal degradation of EED, EZH2, and SUZ12. This eliminates both the catalytic (EZH2) and scaffolding (EED, SUZ12) functions of PRC2, unlike EZH2 inhibitors or EED inhibitors that only block enzymatic activity.
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| ln Vitro |
UNC6852 facilitates PRC2 degradation [1]. UNC6852 is not harmful to HeLa cells at doses of up to 30 μM [1]. UNC6852 (10 μM; 1-72 hours) reduces EED and EZH2 levels [1]. UNC6852 induces PRC2 degradation via VHL recruitment [1]. UNC6852 preferentially destroys both EED and EZH2[1]. UNC6852 lowers H3K27me3 levels and DLBCL cell growth [1].
In vitro, UNC6852 is a potent degrader of PRC2 components. It degrades EED, EZH2, and SUZ12 via recruitment of VHL. The compound's activity is assessed by measuring the degradation of these proteins by Western blot. Its anti-proliferative effects are evaluated in cancer cell lines dependent on PRC2 function. UNC6852 has an IC50 for degradation of PRC2 components. |
| ln Vivo |
In vivo, UNC6852 is used in research to study the role of PRC2 in cancer and other diseases. As a first-in-class PROTAC degrader, it provides a unique tool to investigate the effects of complete PRC2 loss. Its ability to degrade both catalytic and scaffolding functions makes it a valuable tool for studying PRC2 biology. Further in vivo studies are needed to evaluate its therapeutic potential.
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| Enzyme Assay |
In vitro binding assays for UNC6852 measure its affinity for the EED subunit of PRC2 and for VHL. Surface plasmon resonance (SPR) or isothermal titration calorimetry (ITC) can be used to determine binding affinities. The compound's ability to induce the formation of a ternary complex between EED and VHL is assessed. Degradation assays measure the reduction of EED, EZH2, and SUZ12 protein levels by Western blot.
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| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: DLBCL Cells Tested Concentrations: 3 μM Incubation Duration: 0 -10 days Experimental Results: demonstrated anti-proliferative effects. Western Blot Analysis[1] Cell Types: HeLa Cells Tested Concentrations: 10 μM Incubation Duration: 1 hour, 4 hrs (hours), 8 hrs (hours), 10 hrs (hours), 16 hrs (hours), 20 hrs (hours), 24 hrs (hours), 48 hrs (hours), 72 hrs (hours) Experimental Results: Resulted in a decrease in the levels of both EED and EZH2. In vitro cellular studies are conducted using cancer cell lines dependent on PRC2 function. Cells are treated with UNC6852 at various concentrations. Protein levels of EED, EZH2, and SUZ12 are measured by Western blot to confirm degradation. Cell viability is assessed using MTT or CellTiter-Glo assays. Changes in gene expression (e.g., H3K27me3 levels, PRC2 target gene expression) are analyzed to evaluate the functional consequences of PRC2 degradation. |
| Animal Protocol |
In vivo animal experiments are performed in xenograft models of PRC2-dependent cancers. Tumor-bearing mice are administered UNC6852 via various routes. Tumor volume is measured over time, and endpoints include tumor growth inhibition and survival. Pharmacodynamic studies evaluate PRC2 degradation and H3K27me3 levels in tumor tissues.
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| ADME/Pharmacokinetics |
UNC6852 is a research compound with specific molecular properties. It is a bivalent degrader targeting the EED and EZH2 subunits of PRC2. The compound is soluble in DMSO and should be stored at -20°C. It is supplied with ≥98% purity (HPLC). For in vivo administration, appropriate formulations should be used. It is a potent degrader with an IC50 for PRC2 degradation.
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| Toxicity/Toxicokinetics |
As a research chemical with potent biological activity, UNC6852 is not intended for human use. Its toxicological profile is not fully characterized. Standard laboratory safety precautions should be followed when handling it. Its effects are related to its mechanism as a PRC2 degrader, which could have significant biological consequences.
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| References | |
| Additional Infomation |
UNC6852 is a first-in-class PROTAC degrader of PRC2 components. Unlike EZH2 inhibitors (tazemetostat, GSK126) or EED inhibitors (EED226) that only block enzymatic activity, UNC6852 eliminates both catalytic and scaffolding functions of PRC2. It is used in research on cancer, development, and epigenetics. It is a valuable tool for studying the role of PRC2 in various biological processes.
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| Exact Mass |
832.35
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|---|---|
| Elemental Analysis |
C, 62.00; H, 5.81; N, 16.82; O, 11.52; S, 3.85
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| Appearance |
Light yellow to yellow solid powder
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| Synonyms |
UNC6852 UNC-6852
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (6.00 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 5 mg/mL (6.00 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 5 mg/mL (6.00 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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