| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
| Targets |
Mad1 (6-21) targets the PAH2 (paired amphipathic helix 2) domain of the mammalian Sin3A protein. The peptide binds directly to the Sin3A PAH2 domain with high affinity (Kd approximately 29 nM). This interaction is mediated by an amphipathic alpha-helical structure formed by Mad1 (6-21) upon binding. The PAH2 domain of mSin3A consists of a left-handed four-helix bundle, with helices alpha1 and alpha2 creating a deep hydrophobic pocket that serves as the main contact surface for the Mad1 peptide. This binding is critical for Mad1's function in transcriptional regulation and cell cycle control.
|
|---|---|
| ln Vitro |
The residues in the turn regions and all four helices of the left-handed, up-and-down four-helix bundle structure that the PAH2 domain of mSin3A adopts define a tight structural domain with a large hydrophobic core. A deep hydrophobic pocket formed by helices α1 and α2 serves as the main contact surface for the Mad1 (6-21) peptide. Within the complex, Mad1 (6-21) forms an amphipathic α helix, mostly interacting with PAH2 via the helix's apolar surface[1].
In vitro, Mad1 (6-21) exhibits strong binding affinity to the mammalian Sin3A PAH2 domain, with a dissociation constant (Kd) of approximately 29 nM. The peptide adopts an amphipathic alpha-helical structure upon binding, engaging with the PAH2 domain primarily through its nonpolar surface. This high-affinity interaction makes the peptide an excellent tool for studying Mad1-Sin3A binding and for mapping the interaction interface between the Mad1 protein and the Sin3A transcriptional corepressor complex. No direct enzymatic activity has been reported. |
| ln Vivo |
In vivo studies using the Mad1 (6-21) peptide are not typically performed, as the peptide is used as a binding probe in structural and biochemical studies rather than as a therapeutic agent. The full-length Mad1 protein is essential for spindle assembly checkpoint function in vivo, but the peptide fragment alone does not substitute for the full-length protein. In vivo relevance is studied through mutagenesis of the full-length Mad1 protein based on structural information derived from peptide-binding studies.
|
| Enzyme Assay |
Cell-free binding assay protocol for Sin3A PAH2-Mad1 interaction: Recombinant Sin3A PAH2 domain protein is immobilized on a biosensor chip (SPR) or in a 96-well plate. Varying concentrations of synthetic Mad1 (6-21) peptide (e.g., 1-500 nM) are flowed over the immobilized protein, and binding is measured as response units (SPR) or fluorescence polarization (if fluorescently labeled). Association and dissociation rates are calculated, and Kd is determined by nonlinear curve fitting. Isothermal titration calorimetry (ITC) may also be used to measure binding thermodynamics.
|
| Cell Assay |
Cell-based binding studies: Cells expressing fluorescently tagged Sin3A are used to assess the ability of Mad1 (6-21) peptide to compete with full-length Mad1 for Sin3A binding. However, the peptide is not cell-permeable under standard conditions. For pulldown experiments, biotinylated Mad1 (6-21) peptide is immobilized on streptavidin beads and incubated with cell lysates expressing Sin3A. Bound proteins are eluted and detected by Western blotting to confirm specific interaction and to identify additional binding partners of the Mad1 sequence.
|
| Animal Protocol |
In vivo animal studies with Mad1 (6-21) peptide are not standardly performed due to the peptide's lack of membrane permeability and its use as a biochemical tool. Transgenic mouse models may be used to study the effects of mutations in the corresponding region of the full-length Mad1 protein. These mutations disrupt Mad1-Sin3A binding and are expected to affect cell cycle progression and mitotic checkpoint function, but the peptide itself is not administered to animals.
|
| ADME/Pharmacokinetics |
Pharmacokinetic studies of Mad1 (6-21) have not been performed because the peptide is not a drug candidate. As a 16-amino acid peptide (molecular weight ~1966 Da), it would not be orally bioavailable and would be rapidly degraded by proteases in the gastrointestinal tract and bloodstream if administered in vivo. The peptide is designed exclusively for in vitro biochemical and structural studies of protein-protein interactions and is not intended for systemic administration.
|
| Toxicity/Toxicokinetics |
No toxicity studies have been conducted for Mad1 (6-21) as it is a research peptide used at low concentrations (nanomolar to low micromolar) in cell-free and cell-based binding assays. The peptide is not administered to animals for toxicological evaluation. Standard laboratory safety precautions for handling synthetic peptides (avoiding inhalation, skin contact, and injection) should be followed, as the toxicological profile has not been characterized.
|
| References |
[1]. K Brubaker, et al. Solution structure of the interacting domains of the Mad-Sin3 complex: implications for recruitment of a chromatin-modifying complex. Cell. 2000 Nov 10;103(4):655-65.
|
| Additional Infomation |
Mad1 (6-21) is not a drug and has no clinical applications or regulatory approval. It is a research-grade peptide used to investigate the molecular interactions between the Mad1 spindle checkpoint protein and the Sin3A transcriptional corepressor complex. The high-affinity binding (Kd ~29 nM) makes it a valuable tool for structural biology studies (including NMR and X-ray crystallography), protein interaction mapping, and cell cycle research. The peptide sequence is H-Arg-Met-Asn-Ile-Gln-Met-Leu-Leu-Glu-Ala-Ala-Asp-Tyr-Leu-Glu-Arg-OH. Not for therapeutic use.
|
| Molecular Formula |
C84H140N24O26S2
|
|---|---|
| Molecular Weight |
1966.28561687469
|
| Exact Mass |
1964.981
|
| CAS # |
880150-82-3
|
| Related CAS # |
Mad1 (6-21) (TFA)
|
| PubChem CID |
168013263
|
| Appearance |
White to off-white solid powder
|
| LogP |
-5.2
|
| Hydrogen Bond Donor Count |
29
|
| Hydrogen Bond Acceptor Count |
31
|
| Rotatable Bond Count |
70
|
| Heavy Atom Count |
136
|
| Complexity |
4070
|
| Defined Atom Stereocenter Count |
17
|
| SMILES |
[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CC(=O)N)NC(=O)[C@H](CCSC)NC(=O)[C@@H](N)CCCNC(N)=N)(C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](C(=O)O)CCCNC(N)=N)CC1C=CC(O)=CC=1
|
| InChi Key |
ZBAJHFNGYUVVPZ-ZJZZMTSFSA-N
|
| InChi Code |
InChI=1S/C84H140N24O26S2/c1-13-43(8)66(108-80(131)59(38-62(87)111)107-73(124)52(28-32-135-11)96-69(120)48(85)16-14-30-92-83(88)89)81(132)100-49(22-25-61(86)110)71(122)99-53(29-33-136-12)74(125)103-57(36-42(6)7)77(128)104-55(34-40(2)3)75(126)97-50(23-26-63(112)113)70(121)95-44(9)67(118)94-45(10)68(119)102-60(39-65(116)117)79(130)106-58(37-46-18-20-47(109)21-19-46)78(129)105-56(35-41(4)5)76(127)98-51(24-27-64(114)115)72(123)101-54(82(133)134)17-15-31-93-84(90)91/h18-21,40-45,48-60,66,109H,13-17,22-39,85H2,1-12H3,(H2,86,110)(H2,87,111)(H,94,118)(H,95,121)(H,96,120)(H,97,126)(H,98,127)(H,99,122)(H,100,132)(H,101,123)(H,102,119)(H,103,125)(H,104,128)(H,105,129)(H,106,130)(H,107,124)(H,108,131)(H,112,113)(H,114,115)(H,116,117)(H,133,134)(H4,88,89,92)(H4,90,91,93)/t43-,44-,45-,48-,49-,50-,51-,52-,53-,54-,55-,56-,57-,58-,59-,60-,66-/m0/s1
|
| Chemical Name |
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S,3S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-amino-5-carbamimidamidopentanoyl]amino]-4-methylsulfanylbutanoyl]amino]-4-oxobutanoyl]amino]-3-methylpentanoyl]amino]-5-oxopentanoyl]amino]-4-methylsulfanylbutanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-5-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(1S)-4-carbamimidamido-1-carboxybutyl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-oxopentanoic acid
|
| 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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| 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
|
|---|---|
| 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
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *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 : PEG300 ：Tween 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). View More
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)] 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). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.5086 mL | 2.5429 mL | 5.0857 mL | |
| 5 mM | 0.1017 mL | 0.5086 mL | 1.0171 mL | |
| 10 mM | 0.0509 mL | 0.2543 mL | 0.5086 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
