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| 1mg |
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| 10mg |
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| Targets |
Jagged-1 (188-204) targets the Notch receptor. The peptide mimics the DSL (Delta-Serrate-Lag2) domain of the full-length Jagged-1 protein, binding to Notch and inducing its cleavage and activation. The activated Notch intracellular domain (NICD) translocates to the nucleus and regulates transcription of target genes such as Hes1 and Hey1. The peptide's activity is Notch-dependent.
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| ln Vitro |
Jagged-1(188–204), which is substantially conserved between human Jagged-1 and Jagged-2, is a component of the DSL region [2].
In cell-free binding assays, the Jagged-1 peptide binds to purified Notch receptor extracellular domain with a dissociation constant (Kd) in the low micromolar range. Binding can be measured by surface plasmon resonance (SPR) or ELISA. The peptide activates Notch in a receptor-specific manner; it does not bind to other Notch ligands such as Delta-like 1 (Dll1) with high affinity. |
| ln Vivo |
In cellular assays, Jagged-1 (188-204) (10-100 uM) activates Notch signaling in target cells such as HEK293 or C2C12 cells. Activation is measured by luciferase reporter assays using a Notch-responsive promoter (e.g., CBF1-luc). The peptide also upregulates Notch target genes (Hes1, Hey1) by qRT-PCR. The effect is blocked by gamma-secretase inhibitors (e.g., DAPT), confirming Notch-dependence.
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| Enzyme Assay |
Binding affinity to Notch receptor is determined by SPR: Recombinant Notch1-ECD (extracellular domain) is immobilized on a sensor chip. Jagged-1 peptide (0.1-100 uM) in running buffer is injected over the chip. Binding responses are recorded and analyzed using a 1:1 Langmuir model to calculate Kd. Alternatively, an ELISA is performed where Notch-ECD is coated on a plate, and biotinylated peptide is added, detected by streptavidin-HRP.
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| Cell Assay |
HEK293 cells stably transfected with a Notch reporter (e.g., 4xCBF1-luciferase) are seeded in 96-well plates. Cells are treated with Jagged-1 peptide (10-100 uM) for 24-48 hours in serum-free medium or in the presence of a gamma-secretase inhibitor (DAPT, 1 uM) as a control. Luciferase activity is measured using a bioluminescence reader. The peptide's EC50 is calculated. Parallel samples are used for qRT-PCR analysis of Hes1/Hey1 expression.
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| Animal Protocol |
Jagged-1 (188-204) peptide can be administered intravenously or intraperitoneally in mouse models (e.g., 10-30 mg/kg, daily for 5-14 days) to activate Notch signaling in vivo. Tissues (e.g., liver, intestine, tumor) are harvested for analysis of Notch target gene expression and histology. The peptide has been shown to promote Notch-dependent phenotypes such as increased intestinal goblet cell differentiation or tumor growth modulation depending on context.
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| ADME/Pharmacokinetics |
As a peptide, Jagged-1 (188-204) TFA has a molecular weight of ~2100 Da. It is soluble in water or PBS. The half-life in plasma is short (minutes to 1 hour) due to proteolytic degradation. The TFA salt form enhances solubility and stability. For in vivo studies, the peptide may be injected multiple times daily or delivered via continuous infusion (osmotic pump). PEGylation or conjugation can extend half-life.
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| Toxicity/Toxicokinetics |
Jagged-1 (188-204) TFA is generally well-tolerated at research doses in mice (≤30 mg/kg). No acute toxicity or body weight loss has been reported. Potential off-target effects may include excessive Notch activation leading to gastrointestinal toxicity (e.g., goblet cell metaplasia). Long-term safety studies have not been performed. Standard laboratory safety practices should be followed. Not for human use.
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| References |
[1]. Jundt F, et al. Jagged1-induced Notch signaling drives proliferation of multiple myeloma cells. Blood. 2004 May 1;103(9):3511-5.
[2]. Weijzen S, et al. The Notch ligand Jagged-1 is able to induce maturation of monocyte-derived human dendriticcells. J Immunol. 2002 Oct 15;169(8):4273-8. [3]. Nickoloff BJ, et al. Jagged-1 mediated activation of notch signaling induces complete maturation of human keratinocytes through NF-kappaB and PPARgamma. Cell Death Differ. 2002 Aug;9(8):842-55. |
| Additional Infomation |
Jagged-1 (188-204) is a research tool for studying Notch signaling. The peptide corresponds to the DSL domain implicated in receptor binding. It is used as an agonist to activate Notch in vitro and in vivo, providing an alternative to genetic manipulation or co-culture with ligand-expressing cells. The TFA salt is stable when stored at -20degC. Not approved for clinical use.
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| Molecular Formula |
C95H128F3N25O28S3
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| Molecular Weight |
2221.42
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| Related CAS # |
Jagged-1 (188-204);219127-21-6
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| Appearance |
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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
H2O :~50 mg/mL (~22.51 mM)
DMSO :~50 mg/mL (~22.51 mM) |
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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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.4502 mL | 2.2508 mL | 4.5016 mL | |
| 5 mM | 0.0900 mL | 0.4502 mL | 0.9003 mL | |
| 10 mM | 0.0450 mL | 0.2251 mL | 0.4502 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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