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MMH1-NR

Cat No.:V83896 Purity: ≥98%
MMH1-NR
MMH1-NR Chemical Structure Product category: Others 14
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
1mg
5mg
10mg
Other Sizes
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Product Description
MMH1-NR contains a non-reactive (ethyl) group and is a negative control for MMH1, a CUL4-associated factor 16 (DCAF16)-based bromodomain protein 4 (BRD4) degrader.
MMH1-NR is a negative control compound specifically paired with the covalent molecular glue degrader MMH1. MMH1 is a CUL4-associated factor (DCAF16)-based bromodomain protein 4 (BRD4) degrader. MMH1-NR contains a non-reactive (ethyl) group in place of the reactive acrylamide warhead, preserving the complete non-covalent binding scaffold of MMH1 while eliminating DCAF16 Cys58 alkylation. The compound has a molecular weight of 493.62 and a molecular formula of C26H31N5O3S. It is intended for research use only.
Biological Activity I Assay Protocols (From Reference)
Targets
MMH1-NR targets the same non-covalent binding scaffold as MMH1 but lacks the reactive electrophilic warhead required for covalent engagement with DCAF16. As a negative control, it does not degrade BRD4, as it cannot form the covalent bond with Cys58 of DCAF16 that is essential for the degradation mechanism. The compound serves as a structurally matched control to differentiate between effects mediated by MMH1's target engagement and those arising from the covalent warhead or off-target effects.
ln Vitro
In vitro studies demonstrate that MMH1-NR functions as a negative control for the BRD4 degrader MMH1. Unlike MMH1, MMH1-NR contains a non-reactive ethyl group instead of the reactive acrylamide warhead and therefore 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 MMH1-mediated BRD4 degradation.
ln Vivo
In vivo activity of MMH1-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 MMH1 scaffold in animal studies. Any in vivo effects observed with MMH1-NR would indicate off-target activities not related to BRD4 degradation. Detailed in vivo data for MMH1-NR are not extensively documented in the available literature.
Enzyme Assay
The in vitro enzyme/receptor binding assay for MMH1-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 MMH1-NR retains the non-covalent binding properties of MMH1 without covalent engagement. Surface plasmon resonance or isothermal titration calorimetry may be used to assess binding to target proteins. Standard protocols include MMH1 as a positive control for binding and degradation.
Cell Assay
In vitro cell-based assays for MMH1-NR are conducted using cell lines to evaluate its function as a negative control for BRD4 degradation. Cells are treated with MMH1-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 MMH1 as a positive control for BRD4 degradation and appropriate vehicle controls.
Animal Protocol
In vivo animal studies for MMH1-NR would typically be conducted alongside MMH1 to control for non-specific effects in mouse models. Animals would be administered MMH1-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.
ADME/Pharmacokinetics
Pharmacokinetic properties of MMH1-NR include a molecular weight of 493.62 and a molecular formula of C26H31N5O3S. The compound appears as a white to light yellow solid. Solubility includes DMSO at 100 mg/mL (202.58 mM). Storage recommendations include powder at -20°C for 3 years or 4°C for 2 years, and in solvent at -80°C for 6 months or -20°C for 1 month. The compound is hygroscopic and requires careful handling.
Toxicity/Toxicokinetics
Toxicity information for MMH1-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. The compound is a controlled substance and not for sale in certain territories.
References

[1].Template-assisted covalent modification of DCAF16 underlies activity of BRD4 molecular glue degraders. bioRxiv. 2023 Feb 15:2023.02.14.528208.

Additional Infomation
MMH1-NR is a negative control for the covalent molecular glue degrader MMH1, which is a DCAF16-based BRD4 degrader. MMH1-NR contains a non-reactive ethyl group instead of the reactive acrylamide warhead, preserving the complete non-covalent binding scaffold while eliminating DCAF16 Cys58 alkylation. It is used to distinguish specific BRD4 degradation effects from non-specific effects. It has a molecular weight of 493.62 and formula C26H31N5O3S.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C26H31N5O3S
Molecular Weight
493.62
Appearance
White to light yellow solid powder
HS Tariff Code
2934.99.9001
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)
Solubility Data
Solubility (In Vitro)
DMSO :~100 mg/mL (~202.58 mM; with sonication)
Solubility (In Vivo)
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

Injection Formulations
(e.g. IP/IV/IM/SC)
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution 50 μL Tween 80 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO 400 μLPEG300 50 μL Tween 80 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).
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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO 900 μL (20% SBE-β-CD in saline)]
*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.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO 100 μLPEG300 200 μL castor oil 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10: 10 : 80 (i.e. 100 μL Ethanol 100 μL Cremophor 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH 400 μLPEG300 50 μL Tween 80 450 μL Saline)


Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).
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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders


Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.0258 mL 10.1292 mL 20.2585 mL
5 mM 0.4052 mL 2.0258 mL 4.0517 mL
10 mM 0.2026 mL 1.0129 mL 2.0258 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.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

  • Calculate the Mass of a compound required to prepare a solution of known volume and concentration
  • Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume
An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
  • To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
  • Click the “Calculate” button
  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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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