| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
MMH2-NR targets the same non-covalent binding scaffold as MMH2 but lacks the reactive electrophilic warhead required for covalent engagement with DCAF16. As a negative control, it does not degrade BRD4 because it cannot form the covalent bond with Cys58 of DCAF16 that is essential for the degradation mechanism. The compound serves as a structurally matched negative control to differentiate between effects mediated by MMH2's target engagement and those arising from off-target effects.
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| ln Vitro |
In vitro studies demonstrate that MMH2-NR functions as a negative control for the BRD4 degrader MMH2. Unlike MMH2, MMH2-NR is a non-reactive control probe that does not degrade BRD4. This allows researchers to distinguish between specific BRD4 degradation effects and non-specific effects of the compound scaffold. Detailed in vitro activity data, including cellular degradation assays, are used to validate the specificity of MMH2-mediated BRD4 degradation.
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| ln Vivo |
In vivo activity of MMH2-NR is not applicable in the traditional sense, as the compound is a negative control rather than a pharmacologically active agent. It is used in vivo to control for non-specific effects of the MMH2 scaffold in animal studies. Any in vivo effects observed with MMH2-NR would indicate off-target activities not related to BRD4 degradation. Detailed in vivo data for MMH2-NR are not extensively documented in the available literature.
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| Enzyme Assay |
The in vitro enzyme/receptor binding assay for MMH2-NR is not applicable in the traditional sense, as the compound is a negative control rather than an enzyme inhibitor or receptor ligand. However, binding studies may be performed to confirm that MMH2-NR retains the non-covalent binding properties of MMH2 without covalent engagement. Surface plasmon resonance or isothermal titration calorimetry may be used to assess binding to target proteins. Standard protocols include MMH2 as a positive control for binding and degradation.
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| Cell Assay |
In vitro cell-based assays for MMH2-NR are conducted using cell lines to evaluate its function as a negative control for BRD4 degradation. Cells are treated with MMH2-NR at various concentrations, and BRD4 protein levels are measured by Western blot to confirm that no degradation occurs. Cell viability and proliferation are assessed using MTT or CCK-8 assays to control for non-specific effects. Standard protocols include MMH2 as a positive control for BRD4 degradation and appropriate vehicle controls.
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| Animal Protocol |
In vivo animal studies for MMH2-NR would typically be conducted alongside MMH2 to control for non-specific effects in mouse models. Animals would be administered MMH2-NR via appropriate routes, and BRD4 degradation in tissues would be confirmed by Western blot. Tumor growth, body weight, and clinical signs would be monitored. However, detailed in vivo protocols and efficacy data are not available from the search results. The compound is intended for research use only.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of MMH2-NR are not extensively documented in the available literature. As a negative control compound for the BRD4 degrader MMH2, it is expected to have similar physicochemical properties to MMH2. Storage and handling recommendations would follow standard procedures for research compounds. Detailed pharmacokinetic parameters are not available from the search results.
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| Toxicity/Toxicokinetics |
Toxicity information for MMH2-NR is limited. As a research-use negative control, standard safety precautions for handling research chemicals should be followed. The compound is designated for research use only and is not for human therapeutic applications. No detailed toxicity data are available from the search results.
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| References | |
| Additional Infomation |
MMH2-NR is a chemically matched negative control for the BRD4 degrader MMH2. MMH2 is a DCAF16-based BRD4 degrader. MMH2-NR is a non-reactive control probe that preserves the complete non-covalent binding scaffold while eliminating covalent engagement. It is used to distinguish specific BRD4 degradation effects from non-specific effects. It is intended for research use only.
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| Molecular Formula |
C25H31N5O4S2
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|---|---|
| Molecular Weight |
529.67
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| Appearance |
White to light yellow solid powder
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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) |
DMSO :~100 mg/mL (~188.80 mM; with sonication)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (4.72 mM) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one),clear solution; with ultrasonication.
For example, if 1 mL of working solution is to be prepared,you can add 100 μL of 25.0 mg/mL clear DMSO stock solution and add it to 400 μL PEG300 and mix well. Then add 50 μL Tween-80 to the above system and mix well. Then continue to add 450 μL of physiological saline to make up 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: 2.5 mg/mL (4.72 mM) 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; with ultrasonication. For example, if 1 mL of working solution is to be prepared,you can add 100 μL of 25.0 mg/mL clear DMSO stock solution and add it to 900 μL of 20% SBE-β-CD saline solution and mix well. 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: 2.5 mg/mL (4.72 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one),clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8880 mL | 9.4398 mL | 18.8797 mL | |
| 5 mM | 0.3776 mL | 1.8880 mL | 3.7759 mL | |
| 10 mM | 0.1888 mL | 0.9440 mL | 1.8880 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
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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