PROTAC JAK2 degrader-1
PROTAC JAK2 degrader-1 is a JAK2 PROTAC degrader, with a DC50 of 27.35 nM. PROTAC JAK2 degrader-1 induces JAK2 degradation via the ubiquitin-proteasome pathway. PROTAC JAK2 degrader-1 inhibits the JAK2-STAT signaling pathway. PROTAC JAK2 degrader-1 induces G2/M phase arrest and apoptosis in cancer cells. PROTAC JAK2 degrader-1 exhibits antiproliferative activity against cancer cells. PROTAC JAK2 degrader-1 inhibits recombinant human erythropoietin (rhEPO)-mediated polycythemia and splenomegaly in mice. PROTAC JAK2 degrader-1 can be used for research on myeloproliferative neoplasms, including polycythemia vera.
(Pink: JAK2 ligand (HY-174430); Blue: Cereblon ligand (HY-W087383); Black: linker).
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- Formule: C45H51ClFN9O5
- Masse moléculaire:852.40
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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p-STAT3 |
STAT5 |
JAK2-V617F 27.35 nM (DC50) |
Cereblon |
PROTAC JAK2 degrader-1 (Compound 10i) (8 nM-5 μM; 24 h) potently degrades JAK2V617F protein in SET-2 cells via a proteasome-dependent pathway, with a DC50 of 27.35 nM and a degradation rate of up to 91.32% after 24 h of treatment at 5 μM[1].
PROTAC JAK2 degrader-1 (8 nM-5 μM; 24 h) inhibits the JAK2-STAT signaling pathway in SET-2 cells in a dose-dependent manner by reducing the phosphorylation levels of JAK2, STAT3 and STAT5[1].
PROTAC JAK2 degrader-1 potently inhibits the proliferation of SET-2 cells with an IC50 of 0.12 μM; it also inhibits the proliferation of HEL cells with an IC50 of 1.43 μM[1].
PROTAC JAK2 degrader-1 (0-1 μM, 24 h) blocks the G2/M cell cycle progression of SET-2 cells and induces apoptosis in a dose-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SET-2 cells (carrying JAK2 V617F mutation)
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Concentration:8 nM, 40 nM, 200 nM, 1 μM, 5 μM
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Incubation Time:24 h
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Result:Induced dose-dependent degradation of JAK2 V617F protein in SET-2 cells, achieving degradation rates of 15.12% at 8 nM, 56.91% at 40 nM, 76.45% at 200 nM, 78.40% at 1 μM, and 91.32% at 5 μM.
Achieved a DC50 of 27.35 nM.\nDose-dependently inhibited phosphorylation of JAK2, STAT3, and STAT5 in SET-2 cells, with no significant effect on total STAT3 and STAT5 protein levels.
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Cell Line:Jurkat cells
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Concentration:8 nM, 40 nM, 200 nM, 1 μM, 5 μM
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Incubation Time:24 h
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Result:Showed no significant degradation of JAK1, JAK3, TYK2, or GSPT1 in Jurkat cells even at the highest tested concentration of 5 μM.
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Cell Line:SET-2 cells
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Concentration:0, 0.1, 1 μM
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Incubation Time:24 h
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Result:Blocked the G2/M cell cycle progression.
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Cell Line:SET-2 cells
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Concentration:0, 0.1, 1 μM
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Incubation Time:24 h
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Result:Induced apoptosis in a dose-dependent manner.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c (female, 8−10 weeks, 20−25 g, rhEPO-induced polycythemia and splenomegaly)[1]
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Dosage:30 mg/kg
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Administration:i.p.; daily; 4 days
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Result:Reduced reticulocyte count from 18.25% (model group) to 10.94%.
Reduced hematocrit from 49.80% (model group) to 44.81%.
Decreased the proportion of Ter119/CD71 positive erythroid progenitor cells in the spleen from 41.25% (model group) to 25.43% and in bone marrow from 19.71% (model group) to 6.16%.
Reduced average spleen weight from 0.269 g (model group) to 0.216 g.
Decreased JAK2 protein levels and suppressed phosphorylation of STAT3 and STAT5 in spleen tissue.
Chemical Information
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Masse moléculaire 852.40
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Formule C45H51ClFN9O5
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SMILES
FC1=CC([C@H](OC2=C(N=CC(C3=CN(N=C3)C4CCN(CC4)CC5CN(CC5)CC6CCN(CC6)C7=CC(C(N8C9CCC(NC9=O)=O)=O)=C(C=C7)C8=O)=C2)N)C)=C(C=C1)Cl
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PROTAC JAK2 degrader-1 Related Classifications
HY-174428 Related Classifications
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