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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- Fòrmula: C31H24ClNO10
- Peso molecular:605.98
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Almacenamiento:
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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Actividad biológica
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Chemical Information
- Protocolo
- Pureza y Documentación
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Help & FAQs
Actividad biológica
Descripciòn
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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Peso molecular 605.98
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Fòrmula 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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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocolo
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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.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
JAK2 activator 1 Related Classifications
HY-189252 Related Classifications
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