JAK1-IN-21
JAK1-IN-21, biotin-conjugated isoxazole derivative, is a JAK1 inhibitor. JAK1-IN-21 directly engages and stabilizes JAK1, reduces the phosphorylation of JAK1, STAT1 and AKT, induces apoptotic marker cleavage (PARP, Caspase-3, Caspase-7) and exhibits broad-spectrum antiproliferative activity against cancer cells. JAK1-IN-21 can be used for the study of liver cancer, prostate cancer, and breast cancer.
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- Formel: C34H34ClN3O5S
- Molecular Weight:632.17
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
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JAK1 |
STAT1 |
Akt1 |
Caspase-3 |
Caspase-7 |
JAK1-IN-21 (C160) (0.3-10 μM; 72 h) inhibits the proliferation of Mahlavu, SNU475, C4-2, DU145, PC3, T47D and MDA-MB-231 cells, with IC50 values of 2.73, 1.48, 0.89, 1.39, 1.41, 0.52 and 3.05 μM, respectively[1].
JAK1-IN-21 (1-5 μM; 24-48 h) causes pronounced inhibition of STAT1 phosphorylation and markedly reduces phosphorylated JAK1 levels in Mahlavu, DU145 and C4-2 cells[1].
JAK1-IN-21 (10 μM; 30 min) results in a clear, dose-dependent protection of JAK1 from Pronase-mediated digestion[1].
JAK1-IN-21 (5 μM; 1 h) increases the thermal stability of JAK1 in Mahlavu cell lysates in a CETSA assay[1].
JAK1-IN-21 (1-5 μM; 24 h) induces robust cleavage of PARP, Caspase-3 and Caspase-7 in Mahlavu, DU145 and C4-2 cells[1].
JAK1-IN-21 (120 min) exhibits great stability in human plasma retaining 89% of the parent compound[1].
JAK1-IN-21 (0.3-10 μM; 3 days) suppresses C4-2 spheroid growth, resulting in smaller spheroid size, disrupted spheroid morphology and increased signs of apoptosis[1].
JAK1-IN-21 (0.75-5 μM; 10 days) produces a pronounced antiproliferative effect in T47D spheroids[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Mahlavu, SNU475, C4-2, DU145, PC3, T47D, MDA-MB-231 and MCF10A cells
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Concentration:0.3-10 μM
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Incubation Time:72 h
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Result:Inhibited the proliferation of T47D, C4-2, DU145, PC3, SNU475, Mahlavu, and MDA-MB-231 cells, with IC50 values of 0.52, 0.89, 1.39, 1.41, 1.48, 2.73, and 3.05 μM, respectively.
Showed weaker inhibitory activity in MCF10A cells, with an IC50 of 6.10 μM.
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Cell Line:Mahlavu, DU145, and C4-2 cells
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Concentration:1 μM, 5 μM
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Incubation Time:24 h, 48 h
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Result:Robustly inhibited the phosphorylation of JAK1 and STAT1, thereby suppressing JAK/STAT signaling.
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Cell Line:Mahlavu cell lysates
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Concentration:10 μM
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Incubation Time:30 min
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Result:Resulted in a clear, dose-dependent protection of JAK1 from Pronase-mediated digestion.
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Cell Line:Mahlavu cell lysates
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Concentration:5 μM
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Incubation Time:1 h
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Result:Increased the thermal stability of JAK1.
Consistently preserved higher levels of soluble JAK1 between 58 and 62 °C.
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Cell Line:Mahlavu, DU145 and C4-2 cells
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Concentration:1 μM, 5 μM
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Incubation Time:24 h
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Result:Induced robust cleavage of PARP, Caspase-3 and Caspase-7.
Exhibited significant apoptotic responses in Mahlavu and C4-2 cells even at low doses.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wild-type zebrafish larvae at 2 dpf[1]
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Dosage:2 μM, 5 μM, 10 μM or 10 μM, 30 μM, 50 μM
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Administration:72 h; daily medium renewal
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Result:Resulted in no morphological abnormalities or developmental defects at concentrations comparable to those used in cellular assays (2, 5, 10 μM).
Did not cause lethality at up to 50 μM.
Displayed normal morphology with no signs of toxicity even at 50 μM.
Chemical Information
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Molecular Weight 632.17
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Formel C34H34ClN3O5S
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SMILES
O=C(OCC1=NOC(C2=CC=C(OCC3=CC=CC=C3C)C=C2)=C1C4=CC=C(Cl)C=C4)CCCCC5SCC(C5N6)NC6=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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