1. Epigenetics
    Stem Cell/Wnt
    JAK/STAT Signaling
    Apoptosis
  2. JAK
    Apoptosis
  3. SHR0302

SHR0302 

Cat. No.: HY-112724
Handling Instructions

SHR0302 is a potent and orally active all members of the JAK family inhibitor, particularly JAK1. The selectivity of SHR0302 for JAK1 is >10-fold for JAK2, 77-fold for JAK3, 420-fold for Tyk2. SHR0302 inhibits JAK1-STAT3 phosphorylation and induces the apoptosis of hepatic stellate cells. SHR0302 has anti-proliferative and anti-inflammatory effects.

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

SHR0302 Chemical Structure

SHR0302 Chemical Structure

CAS No. : 1445987-21-2

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Description

SHR0302 is a potent and orally active all members of the JAK family inhibitor, particularly JAK1. The selectivity of SHR0302 for JAK1 is >10-fold for JAK2, 77-fold for JAK3, 420-fold for Tyk2. SHR0302 inhibits JAK1-STAT3 phosphorylation and induces the apoptosis of hepatic stellate cells. SHR0302 has anti-proliferative and anti-inflammatory effects[1][2].

IC50 & Target[1]

JAK1

 

JAK2

 

JAK3

 

Tyk2

 

In Vitro

SHR0302 (1 nM-10 µM; 48 hours; HSCs) treatment displays an inhibitory effect on the proliferation of HSCs in a concentration-dependent manner[2].
SHR0302 (1 nM-10 µM) exerts an inhibitory effect on the activation, proliferation and migration of HSCs[2].
SHR0302 (1 nM-10 µM; 48 hours; HSCs) treatment induces the apoptosis of HSCs[2].
SHR0302 (1 nM-10 µM; 48 hours; HSCs) treatment significantly increases the activation of caspase-3 and Bax in HSCs, and decreases the expression of Bcl-2. SHR0302 also inhibits the activation of Akt signaling pathway[2].

Cell Proliferation Assay[2]

Cell Line: Hepatic stellate cells (HSCs)
Concentration: 1 nM, 10 nM, 100 nM, 1µM, 10 µM
Incubation Time: 48 hours
Result: Displayed an inhibitory effect on the proliferation of HSCs, and that inhibition ocurred in a concentration-dependent manner.

Apoptosis Analysis[2]

Cell Line: Hepatic stellate cells (HSCs)
Concentration: 1 nM, 10 nM, 100 nM, 1µM, 10 µM
Incubation Time: 48 hours
Result: Induced the apoptosis of HSCs.

Western Blot Analysis[2]

Cell Line: Hepatic stellate cells (HSCs)
Concentration: 1 nM, 10 nM, 100 nM, 1µM, 10 µM
Incubation Time: 48 hours
Result: Significantly increased the activation of caspase-3 and Bax in HSCs, and decreased the expression of Bcl-2. Also inhibited the activation of Akt signaling pathway.
In Vivo

SHR0302 (0.3-3.0 mg/kg; intragastric administration; twice a day; for 14 days; male Sprague-Dawley (SD) rats) treatment suppresses the severity of AA rats by attenuating the arthritis index, arthritis global assessment and paw swelling degree, and alleviated histopathology of spleen and joint of AA rats[1].
SHR0302 can inhibit the proliferation of T, B and fibroblast-like synoviocytes (FLS), and down-regulates cytokines TNF-α, IL-1β, IL-17 and antibody IgG1, IgG2a levels, and suppresses the proportion of Th17 and total B, and inhibits JAK1-STAT3 phosphorylation[1].

Animal Model: Male Sprague-Dawley (SD) rats (150-180 g) injected with complete Freund’s adjuvant (CFA)[1]
Dosage: 0.3 mg/kg,1.0 mg/kg, 3.0 mg/kg
Administration: Intragastric administration; twice a day; for 14 days
Result: Suppressed the severity of adjuvant-induced arthritis (AA) rats by attenuating the arthritis index, arthritis global assessment and paw swelling degree, and alleviated histopathology of spleen and joint of AA rats.
Molecular Weight

414.48

Formula

C₁₈H₂₂N₈O₂S

CAS No.

1445987-21-2

SMILES

O=C(N1C[[email protected]@]2([H])[[email protected]@](C[[email protected]](N(C)C3=C4C(NC=C4)=NC=N3)C2)([H])C1)NC5=NC(OC)=NS5

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References
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Keywords:

SHR0302SHR 0302SHR-0302JAKApoptosisJanus kinaseJAK1arthritisJAK1-STAT3phosphorylationanti-proliferationTh17B-cellanti-inflammatorymigrationcollagenhepaticfibrosisInhibitorinhibitorinhibit

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SHR0302
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