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Cat. No.: HY-189252

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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.

For research use only. We do not sell to patients.

Formula: C₃₁H₂₄ClNO₁₀
Molecular Weight:605.98

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

JAK2 activator 1 Chemical Structure

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

^[1]

JAK2

64 nM (EC₅₀)

p-STAT3

All JAK Isoforms :

All STAT Isoforms :

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 K_D 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.

Cell Viability Assay^[1]

Cell Line:

BMHSCs
Concentration:

2.5, 5, 10 μM
10 μM AZD1480
Incubation Time:

6 h
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.

Immunofluorescence^[1]

Cell Line:

BMHSCs
Concentration:

10 μM
10 μM AZD1480
Incubation Time:

6 h
Result:

Detected elevated CD34 fluorescence intensity after compound 32 treatment, and this upregulation effect was abolished by the JAK2 inhibitor AZD1480.

Western Blot Analysis^[11]

Cell Line:

BMHSCs
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

Species	Dose	Route	T_1/2	CL	V_z	AUC_0-24	T_max	C_max	F
Rat^[1]	50 mg/kg mg/kg	p.o.	2.81 h	20.6 L/h/kg	83.3 L/kg	735 ng·h/mL	1.4 h	140.2 ng/mL	60.2 %
Rat^[1]	5 mg/kg mg/kg	i.v.	1.58 h	2.05 L/h/kg	45.6 L/kg	122 ng·h/mL	/	/	/

In Vivo

JAK2 activator 1 (Compound 32) (25-50 mg/kg; p.o.; once daily; for 20 consecutive days) effectively ameliorates chemotherapy-induced myelosuppression in mice by promoting hematopoietic recovery^[1].
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.

Animal Model:

BALB/c mice (male, 7-8 weeks old, 20-22 g)^[1]
Dosage:

25 mg/kg; 50 mg/kg
Administration:

i.g.; once daily; 20 consecutive days
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

Molecular Weight 605.98
Formula C₃₁H₂₄ClNO₁₀
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Qian J, et al. Design and Synthesis of Type-A Proanthocyanidin Derivatives as JAK2 Activators to Protect against Chemotherapy-Induced Myelosuppression. Journal of medicinal chemistry. 2026 Aug 13;69(15):18813-18837.

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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MOQ

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100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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JAK2 activator 1

All JAK Isoforms

All STAT Isoforms