| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
PROTAC SKP2 degrader-1 (compound HD15) (48 h) inhibited Jurkat cell proliferation with an IC50 of 0.98 μM[1]. PROTAC SKP2 degrader-1 (0.0625-1 μM; 48 h) induced proteasome-dependent degradation of SKP2 in Jurkat cells with a DC50 of 0.29 μM[1]. PROTAC SKP2 degrader-1 (0.0625-1 μM; 48 h) regulated the SOCS1/JAK/STAT1/immunopisome axis in Jurkat cells, upregulating SOCS1 in a concentration-dependent manner, inhibiting p-STAT1, and downregulating immunoproteasome subunits PSMB8, PSMB9, and PSMB10[1]. PROTAC SKP2 degrader-1 (0-6 μM; 48 h) inhibited DNA synthesis and proliferation in Jurkat and Hut78 cells in a dose-dependent manner[1]. PROTAC SKP2 degrader-1 (0.1875-6 μM; 48 h) induced Jurkat cell apoptosis in a dose-dependent manner [1].
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|---|---|
| ln Vivo |
PROTAC SKP2 degrader-1 (10–40 mg/kg; intraperitoneal injection; daily; 14 days) dose-dependently inhibited the growth of subcutaneous Jurkat xenograft tumors in female NCG mice [1].
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| Cell Assay |
Western Blot Analysis [1]
Cell Types: Jurkat cells Tested Concentrations: 0.0625, 0.125, 0.25, 0.5, and 1 μM Incubation Duration: 48 hours Experimental Results: SKP2 protein concentration-dependent degradation was induced in Jurkat cells at a DC50 of 0.29 μM. Co-treatment with MG132 blocked SKP2 degradation, confirming its proteasome-dependent activity. Apoptosis analysis [1] Cell Types: Jurkat cells Tested Concentrations: 0.1875, 0.75, 1.5, 3 and 6 μM Incubation Duration: 48 hours Experimental Results: Jurkat cells were induced to apoptosis in a dose-dependent manner. |
| Animal Protocol |
Animal/Disease Models:NCG mice (female, 6-7 weeks old, 20-25 g, subcutaneously inoculated with Jurkat cell xenograft)[1]
Doses: 10 mg/kg; 20 mg/kg; 40 mg/kg Route of Administration: Intraperitoneal injection; once daily for 14 days Experimental Results: The tumor growth inhibition rate (TGI) in the 40 mg/kg dose group reached 66%. The TGI in the 20 mg/kg dose group exceeded 50%. Compared with the solvent control group, all dose groups significantly reduced tumor volume and weight. In tumor tissue, the expression of SKP2, phosphorylated STAT1, and immunoproteasome subunits PSMB8, PSMB9, and PSMB10 was inhibited in a dose-dependent manner. The expression of SOCS1 in tumor tissue was upregulated. Dose-dependent tumor cell apoptosis and necrosis were induced. Microvessel density and proliferation were reduced in a dose-dependent manner. No significant changes were observed in body weight, liver function biomarkers, or kidney function biomarkers at any of the doses. No pathological changes were observed in the heart, liver, spleen, lungs, or kidneys. |
| References |
| Molecular Formula |
C60H91N5O10S
|
|---|---|
| Molecular Weight |
1074.46
|
| CAS # |
3120650-15-6
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| Appearance |
Typically exists as solids at room temperature
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| SMILES |
O=C(N1[C@@H](C[C@H](C1)O)C(NCC2=CC=C(C3=C(N=CS3)C)C=C2)=O)[C@H](C(C)(C)C)NC(COCCOCCOCCNC([C@]45[C@](CC(C)(CC5)C)([H])C6=CC[C@@]([C@@]7([C@@]([C@@](C)([C@H](CC7)O)CO)([H])CC8)C)([H])[C@]8(C)[C@@]6(CC4)C)=O)=O
|
| 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) |
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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.9307 mL | 4.6535 mL | 9.3070 mL | |
| 5 mM | 0.1861 mL | 0.9307 mL | 1.8614 mL | |
| 10 mM | 0.0931 mL | 0.4654 mL | 0.9307 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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