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| Targets |
The primary target of Dusquetide is the protein p62 (also known as SQSTM1). p62 is a multifunctional adaptor protein that plays a central role in several key cellular signaling pathways. It is involved in selective autophagy, where it helps to target ubiquitinated proteins and organelles for degradation. It also serves as a scaffold for the NF-κB signaling pathway, modulating the inflammatory response. Furthermore, p62 is involved in the Nrf2-mediated oxidative stress response. By binding to p62, Dusquetide modulates the innate immune response to both PAMPs (from pathogens) and DAMPs (from damaged cells). This interaction fine-tunes the immune response, reducing excessive inflammation while enhancing the clearance of pathogens. This mechanism is distinct from traditional antimicrobials, which directly kill or inhibit microbes.
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| ln Vitro |
Dusquetide's in vitro activity is defined by its immunomodulatory properties. It modulates the innate immune response by binding to p62. In cell-based assays, it has been shown to reduce the production of pro-inflammatory cytokines while enhancing the clearance of bacteria. For example, it can modulate the response of immune cells (such as macrophages and neutrophils) to lipopolysaccharide (LPS, a PAMP) or to cellular damage signals. It demonstrates anti-inflammatory activity by reducing the release of inflammatory mediators. Its anti-infective activity is indirect, stemming from its ability to enhance the host's own immune defenses. Its anti-mucositis activity is related to its ability to reduce inflammation and promote tissue healing.
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| ln Vivo |
Radiation therapy displayed a trend toward lowering tumor growth and improving survival, while dusquetide (SGX942) (25 mg/kg; intravenously; days 0, 4, 7, 10, and 14) showed no increase in tumor growth or worsening of survival [1].
Dusquetide has been evaluated in vivo and has shown promising activity. As a first-in-class innate defense regulator, it has been studied in various animal models of infection, inflammation, and mucositis. Its mechanism of action is based on modulating the host's immune response, which can be beneficial in a wide range of conditions. It has been shown to reduce the severity of mucositis, an inflammatory condition of the mucous membranes, which is a common side effect of cancer chemotherapy and radiation therapy. Its anti-infective activity has been demonstrated in models of bacterial infection, where it enhanced the host's ability to clear the infection. Its anti-inflammatory properties have been shown in models of sterile inflammation. These in vivo studies are crucial for validating its unique mechanism of action. |
| Enzyme Assay |
Specific in vitro enzyme or receptor binding assays for Dusquetide are not standard, as its target, p62, is not an enzyme in the traditional sense but a scaffold protein. The primary assay for studying its interaction with p62 is a binding assay, such as surface plasmon resonance (SPR) or isothermal titration calorimetry (ITC), using purified p62 protein. In these assays, the affinity of Dusquetide for p62 is measured. Additionally, cell-based assays are used to study the functional consequences of p62 binding.
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| Cell Assay |
In vitro cell-based assays for Dusquetide evaluate its immunomodulatory effects. Immune cells, such as macrophages or dendritic cells, are treated with Dusquetide and then stimulated with a PAMP (e.g., LPS) or a DAMP. The production of cytokines (e.g., TNF-α, IL-6, IL-10) is measured by ELISA. The compound's ability to modulate the cytokine profile, reducing pro-inflammatory cytokines while maintaining or enhancing anti-inflammatory cytokines, is a key readout. Additionally, its effect on the phagocytic activity of macrophages or neutrophils can be assessed. These assays confirm the compound's mechanism of action at the cellular level.
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| Animal Protocol |
Animal/Disease Models: Female nude mice (MCF-7 tumor xenograft) [1]
Doses: 25 mg/kg Route of Administration: intravenous (iv) (iv)injection; results on days 0, 4, 7, 10 and 14: demonstrated no increase in tumor growth or survival rates worsen, and radiation therapy has a tendency to reduce tumor growth and improve survival. In vivo animal studies for Dusquetide have been conducted in various models. For its anti-infective activity, mouse models of bacterial infection (e.g., sepsis or pneumonia) are used. In these models, animals are infected with a pathogen, and Dusquetide is administered. Survival, bacterial load, and inflammatory markers are measured. For its anti-mucositis activity, models using chemotherapy- or radiation-induced mucositis are employed. The severity of mucosal damage and inflammation is assessed. These studies demonstrate the compound's therapeutic potential in clinically relevant contexts. |
| ADME/Pharmacokinetics |
Detailed pharmacokinetic data for Dusquetide is not provided in the search results. As a peptide, it is likely to be administered via intravenous or subcutaneous injection, as oral bioavailability is generally poor for peptides. Its peptide nature means it would be susceptible to proteolytic degradation.
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| Toxicity/Toxicokinetics |
Specific toxicity data for Dusquetide is not publicly available. As an immunomodulator, there is a potential for immune-related side effects. It is classified as a research tool and is not intended for human use.
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| References | |
| Additional Infomation |
See also: Dusquetide (note moved to).
Dusquetide is a first-in-class innate defense regulator (IDR) that represents a novel approach to treating infectious and inflammatory diseases. By modulating the host immune response through p62, it offers a potential alternative to traditional antimicrobials and anti-inflammatory drugs. It has been investigated in clinical trials, and as of the latest information, it has not received FDA approval. |
| Molecular Formula |
C25H47N9O5
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|---|---|
| Molecular Weight |
553.697984933853
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| Exact Mass |
553.37
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| Elemental Analysis |
C, 54.23; H, 8.56; N, 22.77; O, 14.45
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| CAS # |
931395-42-5
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| Related CAS # |
Dusquetide TFA
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| PubChem CID |
71722017
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| Appearance |
White to off-white solid powder
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| LogP |
-2.7
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| Hydrogen Bond Donor Count |
7
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
15
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| Heavy Atom Count |
39
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| Complexity |
906
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| Defined Atom Stereocenter Count |
6
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| SMILES |
O=C([C@H](C(C)C)NC([C@H]([C@@H](C)CC)NC([C@H](CCC/N=C(\N)/N)N)=O)=O)N1CCC[C@H]1C(N[C@H](C(N)=O)C)=O
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| InChi Key |
ZUJBBVJXXYRPFS-DYKIIFRCSA-N
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| InChi Code |
InChI=1S/C25H47N9O5/c1-6-14(4)19(33-21(36)16(26)9-7-11-30-25(28)29)23(38)32-18(13(2)3)24(39)34-12-8-10-17(34)22(37)31-15(5)20(27)35/h13-19H,6-12,26H2,1-5H3,(H2,27,35)(H,31,37)(H,32,38)(H,33,36)(H4,28,29,30)/t14-,15-,16-,17-,18-,19-/m0/s1
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| Chemical Name |
(2S)-1-[(2S)-2-[[(2S,3S)-2-[[(2S)-2-amino-5-(diaminomethylideneamino)pentanoyl]amino]-3-methylpentanoyl]amino]-3-methylbutanoyl]-N-[(2S)-1-amino-1-oxopropan-2-yl]pyrrolidine-2-carboxamide
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| Synonyms |
SGX 942; dusquetide; L-arginyl-L-isoleucyl-L-valyl-L-prolyl-L-alaninamide; SGX94; SGX942; IMX-942; IMX942; IKX7W49NLN; SGX-94; IMX 942; SGX-942
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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) |
H2O : ~50 mg/mL (~90.30 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 | 1.8060 mL | 9.0302 mL | 18.0603 mL | |
| 5 mM | 0.3612 mL | 1.8060 mL | 3.6121 mL | |
| 10 mM | 0.1806 mL | 0.9030 mL | 1.8060 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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