| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg | |||
| Other Sizes |
| Targets |
The primary target of Histone H1-derived Peptide is cyclin-dependent kinase 1 (CDK1) in complex with cyclin B1, as the peptide contains the optimal recognition motif for this enzyme. It is designed as a substrate for CDK1-cyclin B1, enabling detection of its kinase activity. Additionally, the peptide interacts with Pin1 (peptidyl-prolyl cis-trans isomerase) as a phosphorylated substrate, allowing studies of Pin1 binding characteristics and phosphorylation-dependent protein interactions relevant to cell cycle regulation.
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| ln Vitro |
In vitro, Histone H1-derived Peptide functions as a direct substrate for CDK1-cyclin B1, undergoing phosphorylation that can be quantified to measure enzyme activity. It serves as a phosphopeptide substrate for studying CDK activity, substrate specificity, and phosphorylation dynamics in cell cycle research. The peptide is also utilized in binding assays to investigate interactions with Pin1, providing a model system for analyzing how phosphorylation affects protein-protein interactions and downstream signaling cascades in cellular proliferation.
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| ln Vivo |
In vivo studies using Histone H1-derived Peptide are generally not performed, as the peptide is designed as an in vitro research tool rather than a therapeutic agent. Instead, its applications focus on ex vivo analysis of CDK activity in cell lysates or tissue extracts. Researchers use the peptide to detect and quantify CDK1-cyclin B1 activity in samples derived from in vivo experiments, allowing correlation of kinase activity with cell cycle progression in animal models or disease states without administering the peptide itself to living animals.
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| Enzyme Assay |
Kinase activity assay protocol: Reaction mixture containing recombinant or immunoprecipitated CDK1-cyclin B1, Histone H1-derived Peptide substrate (typically 50-200 microM), ATP (including [gamma-32P]ATP or using non-radioactive detection), and kinase buffer is incubated at 30degC for 15-30 minutes. The reaction is stopped by adding SDS sample buffer or spotting onto phosphocellulose paper. Incorporation of phosphate into the peptide is measured by scintillation counting, phospho-specific antibody detection, or mass spectrometry.
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| Cell Assay |
Cell-based protocol: Cells (e.g., synchronized HeLa or other proliferating cell lines) are lysed in RIPA buffer with protease and phosphatase inhibitors. Cell lysates are normalized for protein concentration and used in in vitro kinase assays with Histone H1-derived Peptide as described above. Alternatively, the peptide can be used in pulldown assays by immobilizing it on agarose beads to capture interacting proteins from cell lysates, followed by Western blot analysis to identify CDK1 or other binding partners.
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| Animal Protocol |
In vivo pharmacokinetic and pharmacodynamic studies utilizing the peptide are not typical, as it is an in vitro substrate rather than a drug candidate. In research settings, the peptide may be used in ex vivo kinase activity assays following in vivo drug treatments. For example, animals treated with CDK inhibitors have their tumor tissues harvested and lysed, then the lysates are incubated with Histone H1-derived Peptide to assess residual CDK1 activity and treatment efficacy.
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| ADME/Pharmacokinetics |
Not applicable-Histone H1-derived Peptide is a research reagent for in vitro biochemical assays, not a therapeutic compound. Therefore, pharmacokinetic properties such as absorption, distribution, metabolism, and excretion have not been characterized in living organisms. The peptide is not intended for in vivo administration, and its stability in biological matrices is only relevant in the context of cell lysates or reaction buffers for enzyme activity measurements.
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| Toxicity/Toxicokinetics |
Toxicity studies are not performed for Histone H1-derived Peptide because it is a research-grade peptide used exclusively in in vitro biochemical and cellular assays. The peptide is not administered to animals or humans for therapeutic purposes, and no systemic toxicity data exist. Standard laboratory safety precautions for handling synthetic peptides (avoiding inhalation, skin contact, and ingestion) are recommended due to lack of comprehensive toxicological evaluation.
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| References |
[1]. Roderick G Walker, et al. High throughput screens yield small molecule inhibitors of Leishmania CRK3:CYC6 cyclin-dependent kinase. PLoS Negl Trop Dis. 2011 Apr 5;5(4):e1033.
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| Additional Infomation |
Histone H1-derived Peptide is not a drug and has not been approved for clinical use. It is a chemical tool for biomedical research, specifically for studying CDK1-cyclin B1 activity in cell cycle regulation. The peptide contains the CDK optimal recognition motif and is widely used in kinase assays to screen inhibitors, characterize enzyme kinetics, and investigate phosphorylation-dependent signaling. It is supplied as a lyophilized powder and reconstituted in aqueous buffers. Not intended for therapeutic applications.
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| Molecular Formula |
C56H101N17O15
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|---|---|
| Exact Mass |
1251.766
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| CAS # |
889112-06-5
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| PubChem CID |
163332302
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| Appearance |
White to off-white solid powder
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| LogP |
-6.9
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| Hydrogen Bond Donor Count |
17
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| Hydrogen Bond Acceptor Count |
20
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| Rotatable Bond Count |
42
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| Heavy Atom Count |
88
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| Complexity |
2330
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| Defined Atom Stereocenter Count |
11
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| SMILES |
C[C@H]([C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]2CCCN2C(=O)CNC(=O)CNC(=O)CN)O
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| InChi Key |
MLODEUSVVAOABW-PNNPTOSWSA-N
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| InChi Code |
InChI=1S/C56H101N17O15/c1-32(2)28-40(56(87)88)70-52(83)38(18-8-12-24-59)68-50(81)37(17-7-11-23-58)66-47(78)33(3)64-49(80)36(16-6-10-22-57)67-51(82)39(19-9-13-25-60)69-54(85)42-21-15-27-73(42)55(86)46(35(5)74)71-48(79)34(4)65-53(84)41-20-14-26-72(41)45(77)31-63-44(76)30-62-43(75)29-61/h32-42,46,74H,6-31,57-61H2,1-5H3,(H,62,75)(H,63,76)(H,64,80)(H,65,84)(H,66,78)(H,67,82)(H,68,81)(H,69,85)(H,70,83)(H,71,79)(H,87,88)/t33-,34-,35+,36-,37-,38-,39-,40-,41-,42-,46-/m0/s1
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| Chemical Name |
(2S)-2-[[(2S)-6-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-6-amino-2-[[(2S)-1-[(2S,3R)-2-[[(2S)-2-[[(2S)-1-[2-[[2-[(2-aminoacetyl)amino]acetyl]amino]acetyl]pyrrolidine-2-carbonyl]amino]propanoyl]amino]-3-hydroxybutanoyl]pyrrolidine-2-carbonyl]amino]hexanoyl]amino]hexanoyl]amino]propanoyl]amino]hexanoyl]amino]hexanoyl]amino]-4-methylpentanoic acid
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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 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)
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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) |
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.) |
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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