JAK2 activator 1
JAK2 activator 1 is an orally active and selective JAK2 activator derived from Proanthocyanidin A1 (HY-N2344) (EC50 = 64 nM). JAK2 activator 1 directly binds to JAK2, triggers conformational changes, and achieves allosteric activation of the JAK2/STAT3 signaling pathway. JAK2 activator 1 promotes hematopoietic recovery in chemotherapy-induced myelosuppression by protecting hematopoietic stem cells from Carboplatin (HY-17393)-induced damage. JAK2 activator 1 does not promote the proliferation of A549, HepG2, or CaCo2 tumor cells, nor does it attenuate the antitumor effect of Carboplatin. JAK2 activator 1 can be used in research related to cancer chemotherapy-induced myelosuppression.
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- Formule: C31H24ClNO10
- Masse moléculaire:605.98
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
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Help & FAQs
Activité biologique
Description
IC50 & Target
[1]|
JAK2 64 nM (EC50) |
p-STAT3 |
In Vitro
JAK2 activator 1 (Compound 32) (0.078-80 μM) is a JAK2 activator that exhibits an EC50 of 64 nM in a cell-free purified enzyme system; it preferentially targets JAK2 within a complex kinase network with minimal interference with other kinases, demonstrating excellent selectivity[1].
JAK2 activator 1 directly binds to JAK2 JH2 as determined by SPR, with a KD value of 178 nM, and preferentially binds to the JAK2 JH2 pseudokinase domain rather than the JH1 catalytic domain[1].
JAK2 activator 1 (2.5-10 μM; pretreatment for 6 h followed by Carboplatin (HY-17393) injury stimulation) attenuates Carboplatin-induced cellular damage in primary mouse bone marrow hematopoietic stem cells (BMHSCs), and co-treatment with the JAK2 inhibitor AZD1480 (HY-10193) abolishes this protective effect[1].
JAK2 activator 1 (2.5-10 μM; 15-60 min) increases the phosphorylation levels of JAK2 and STAT3 in primary mouse BMHSCs in a concentration- and time-dependent manner[1].
JAK2 activator 1 does not promote the proliferation of A549, HepG2, and CaCo2 tumor cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:BMHSCs
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Concentration:2.5, 5, 10 μM
10 μM AZD1480 -
Incubation Time:6 h
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Result:Attenuated Carboplatin-induced cellular damage in primary mouse bone marrow hematopoietic stem cells (BMHSCs), and co-treatment with the JAK2 inhibitor AZD1480 abolishes this protective effect.
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Cell Line:BMHSCs
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Concentration:10 μM
10 μM AZD1480 -
Incubation Time:6 h
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Result:Detected elevated CD34 fluorescence intensity after compound 32 treatment, and this upregulation effect was abolished by the JAK2 inhibitor AZD1480.
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Cell Line:BMHSCs
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Concentration:2.5, 5, 10 μM (concentration-dependent)
10 μM (time-dependent) -
Incubation Time:60 min (concentration-dependent)
0, 15, 30, 45, 60 min (time-dependent) -
Result:Increased the phosphorylation levels of JAK2 and STAT3 in primary mouse BMHSCs in a concentration- and time-dependent manner.
Parmacokinetics
In Vivo
JAK2 activator 1 (500 mg/kg; p.o.; single administration) does not cause significant acute toxicity or histopathological abnormalities in mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c mice (male, 7-8 weeks old, 20-22 g)[1]
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Dosage:25 mg/kg; 50 mg/kg
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Administration:i.g.; once daily; 20 consecutive days
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Result:Dose‑dependently mitigated CBP‑provoked weight loss and recovered peripheral blood cell counts.
Preserved bone‑marrow histology and dose‑dependently elevated HSC‑related marker (Sca‑1, CD117, CD41, CD61) expression.
Markedly rescued LSK (Lin‑Sca‑1+ c‑Kit+) and megakaryocyte‑associated cell fractions, with stronger effects at 50 mg/kg.
Chemical Information
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Masse moléculaire 605.98
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Formule C31H24ClNO10
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SMILES
OC1=C2C(O[C@@]3(C(C=C4)=CC=C4OC)OC5=CC=C([N+]([O-])=O)C=C5[C@@H]2[C@H]3Cl)=CC6=C1C[C@@H](O)[C@@H](C7=CC(O)=C(C=C7)O)O6
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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.
Protocole
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
JAK2 activator 1 Related Classifications
HY-189252 Related Classifications
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