SHR-0302

SHR-0302 is a JAK inhibitor (IC₅₀s = 0.1, 0.9, and 7.7 nM for JAK1, -2, and -3, respectively).¹ It is selective for these kinases over tyrosine kinase 2 (TYK2; IC₅₀ = 42 nM). SHR-0302 inhibits the activation, proliferation, and TGF-β-1-induced migration of HSC-T6 rat hepatic stellate cells when used at concentrations ranging from 0.1 to 10 µM.² It also decreases collagen production and JAK1 and STAT3 phosphorylation in HSC-T6 cells. In vivo, SHR-0302 (3 mg/kg) decreases disease severity and paw swelling in a rat model of adjuvant-induced arthritis.³ It increases survival, white blood cell count, red blood cell count, and platelet count and decreases body weight loss and disease severity in a mouse model of bone marrow transplant-induced graft-versus-host disease (GVHD) when administered prophylactically at a dose of 5 mg/kg.¹

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1. Sun, X., He, Q., Yang, J., et al. Preventive and therapeutic effects of a novel JAK inhibitor SHR0302 in acute graft-versus-host disease. Cell Transplant. 30, 1-16 (2021).

2. Gu, Y.-J., Sun, W.-Y., Zhang, S., et al. Targeted blockade of JAK/STAT3 signaling inhibits proliferation, migration and collagen production as well as inducing the apoptosis of hepatic stellate cells. Int. J. Mol. Med. 38(3), 903-911 (2016).

3. Wu, H., Yan, S., Chen, J., et al. JAK1-STAT3 blockade by JAK inhibitor SHR0302 attenuates inflammatory responses of adjuvant-induced arthritis rats and decreases Th17 and total B cells. Joint Bone Spine 83(5), 525-532 (2016).