| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
DJ001 targets protein tyrosine phosphatase-σ (PTPσ), a receptor-type protein tyrosine phosphatase. It acts as a highly specific, selective, and non-competitive inhibitor with an IC50 of 1.43 μM. It displays no inhibitory activity against other phosphatases. By inhibiting PTPσ, it promotes hematopoietic stem cell regeneration, making it a valuable tool for studying stem cell biology and regeneration.
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| ln Vitro |
In comparison to control cultures, the proportion and quantity of BM KSL cells in the culture increased with the addition of DJ001 (5-1000 ng/mL; 3-7 days). In BM KSL cells cultivated for three days, DJ001 treatment also markedly enhanced the number of colony-forming cells (CFC) [1]. After being exposed to 300 cGy of radiation, BM KSL cells were cultured for three days in a medium that contained 20 ng/mL thrombopoietin, 100 ng/mL stem cell factor (SCF), and 50 ng/mL Flt3 ligand, either with or without 1 μg/mL DJ001 and TSF. When BM CFC and multipotent colony-forming unit-granulocyte, erythrocyte, monocyte, megakaryocyte (CFU-GEMM) colonies were treated with DJ001, their recovery was higher than that of control cultures [1].
In vitro, DJ001 potently inhibits PTPσ with an IC50 of 1.43 μM. It is highly specific, showing no inhibitory activity against other phosphatases. It promotes hematopoietic stem cell regeneration in vitro. Its non-competitive mechanism of action distinguishes it from other inhibitors, making it a valuable tool for studying PTPσ function and its role in stem cell biology. |
| ln Vivo |
In C57BL/6 mice, 24 hours after 500 cGy TBI, DJ001 (5 mg/kg; sc; 24 h) dramatically lowers the proportion of apoptotic BM KSL cells. Through RAC1, RhoGTPase, and BCL-XL induction, DJ001 prevents radiation-induced HSC death [1].
In vivo, DJ001 promotes hematopoietic stem cell regeneration. It has been shown to enhance the recovery of hematopoietic stem cells in animal models, suggesting its potential for therapeutic applications in bone marrow transplantation and other conditions requiring stem cell regeneration. Its specificity for PTPσ is key to its in vivo activity and reduced off-target effects. |
| Enzyme Assay |
In vitro enzyme assays for DJ001 involve measuring its inhibition of PTPσ. The enzyme is incubated with increasing concentrations of the compound and a synthetic phosphopeptide substrate. The release of inorganic phosphate is measured using a colorimetric or fluorometric assay. IC50 values are calculated from dose-response curves. Selectivity is confirmed by testing against a panel of other phosphatases.
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: BM KSL Cell Tested Concentrations: 5 ng/mL, 10 ng/mL, 100 ng/mL, 1000 ng/mL Incubation Duration: 3 days or 7 days Experimental Results: Percentage and number of BM increased KSL cell. The number of colony-forming cells (CFC) also increased Dramatically after BM KSL cell culture for 3 days. For in vitro cell-based assays, hematopoietic stem cells are cultured and treated with DJ001. Its effects on stem cell proliferation, differentiation, and self-renewal are assessed. Cell viability is measured by MTT assays. The activation of downstream signaling pathways following PTPσ inhibition is analyzed by Western blot for changes in phosphorylation of key signaling proteins. |
| Animal Protocol |
Animal/Disease Models: Female C57BL/6 mice (8-10 weeks old) total body irradiation (TBI) [1]
Doses: 5 mg/kg Route of Administration: subcutaneous injection; 24-hour Experimental Results: 500 cGy 24 hrs (hrs (hours)) after TBI, C57BL/ The percentage of apoptotic BM KSL cells was Dramatically diminished in 6 mice. In vivo animal studies with DJ001 are conducted in models of hematopoietic stem cell transplantation or bone marrow injury. The compound is administered to animals, and the regeneration of hematopoietic stem cells is measured by flow cytometry for stem cell markers in the bone marrow and peripheral blood. Its effects on recovery from myeloablation or radiation injury are assessed. |
| ADME/Pharmacokinetics |
DJ001 (CAS: 2161305-12-8) has a molecular weight of 268.27 g/mol and a molecular formula of C15H12N2O3. It is a solid and is typically stored as a powder. It is soluble in DMSO. The compound is a highly specific and selective PTPσ inhibitor with an IC50 of 1.43 μM. It promotes hematopoietic stem cell regeneration.
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| Toxicity/Toxicokinetics |
DJ001 is a research compound and is not approved for human therapeutic use. In preclinical studies, it has shown a manageable safety profile. As a specific PTPσ inhibitor, it is expected to have a targeted mechanism of action. Standard laboratory safety precautions should be followed when handling the compound.
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| References | |
| Additional Infomation |
DJ001 is a highly specific, selective, and non-competitive inhibitor of PTPσ with an IC50 of 1.43 μM. It promotes hematopoietic stem cell regeneration. It is not FDA-approved and is intended for research use only.
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| Molecular Formula |
C15H12N2O3
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| Molecular Weight |
268.267383575439
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| Exact Mass |
268.084
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| CAS # |
2161305-12-8
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| PubChem CID |
44161060
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
3.8
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
20
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| Complexity |
370
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(/C=C\NC1C=CC=C(C=1)[N+](=O)[O-])C1C=CC=CC=1
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| InChi Key |
OVTJWWUGQKIRCL-KTKRTIGZSA-N
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| InChi Code |
InChI=1S/C15H12N2O3/c18-15(12-5-2-1-3-6-12)9-10-16-13-7-4-8-14(11-13)17(19)20/h1-11,16H/b10-9-
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| Chemical Name |
(Z)-3-(3-nitroanilino)-1-phenylprop-2-en-1-one
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| Synonyms |
DJ001; DJ-001
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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 |
| 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) |
DMSO : ~250 mg/mL (~931.90 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 | 3.7276 mL | 18.6379 mL | 37.2759 mL | |
| 5 mM | 0.7455 mL | 3.7276 mL | 7.4552 mL | |
| 10 mM | 0.3728 mL | 1.8638 mL | 3.7276 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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