JAK Inhibitor

Tyk2-IN-5 (Standard) is the analytical standard of Tyk2-IN-5 (HY-111745). This product is intended for research and analytical applications. Tyk2-IN-5 (compound 6) is a potent, selective and orally active tyrosine K_inase 2 (Tyk2) inhibitor that acts on the JH2 structural domain. Tyk2-IN-5 shows a K_i value of 0.086 nM for Tyk2 JH2 and an IC₅₀ value of 25 nM for IFNα. Tyk2-IN-5 efficiently inhibits the production of IFNγ in a pharmacodynamic rat model and is fully efficacious in a rat model of arthritis.

JAK-IN-38 (Compound 1) is a JAK inhibitor, with IC₅₀s of 0.03, 0.06, 0.12, 0.44 μM for Tyk2, JAK3, JAK2, JAK1 respectively. JAK-IN-38 is a collagen VII (C7) inducer and has anti-inflammatory activity. JAK-IN-38 can upregulate the expression of COL7A1 mRNA in donor-derived keratinocytes and works together with Gentamicin (HY-A0276A) to boost overall C7 levels.

WHI-P97 (Standard) is the analytical standard of WHI-P97 (HY-11067). This product is intended for research and analytical applications. WHI-P97 is a potent and selective JAK-3 inhibitor. WHI-P97 is effective in preventing the development allergic asthma in vivo.

Tyk2-IN-18-d3 (Compound 18) is a Tyk2 inhibitor with an IC₅₀ value of < 30 nM for both IL-23 and IFNα. Tyk2-IN-18-d3 can be used for research on autoimmune diseases.

Tofacitinib hydrochloride (Tasocitinib hydrochloride) is an orally active, blood-brain barrier permeable selective inhibitor of JAK1/JAK3. Tofacitinib hydrochloride blocks the JAK-STAT/NF-κB signaling pathway, inhibits cytokine signal transduction, phosphorylation of STAT1/STAT5, and suppresses innate and adaptive immune responses. Tofacitinib hydrochloride can be used in research related to major depressive disorder, rheumatoid arthritis, pulmonary diseases, systemic lupus erythematosus, and immune-mediated liver injury.

TyK2-IN-2 (Standard) is the analytical standard of TyK2-IN-2 (HY-101762). This product is intended for research and analytical applications. TyK2-IN-2 (Compoud 18) is a potent and selective TYK2 inhibitor with IC₅₀s of 7 nM, 0.1 μM and 0.05 μM for TYK2 JH2, IL-23 and IFNα, respectively. TyK2-IN-2 also inhibits phosphodiesterase 4 (PDE4) with an IC₅₀ of 62 nM. TyK2-IN-2 can be used for the research of inflammatory and autoimmune diseases.

AZD-1480 (Standard) is the analytical standard of AZD-1480 (HY-10193). This product is intended for research and analytical applications. AZD-1480 is an ATP-competitive inhibitor of JAK1 and JAK2 with IC₅₀s of 1.3 nM and <0.4 nM, respectively.

PF-1367550 is a pan-JAK inhibitor. PF-1367550 can decrease the levels of release of CXCL9, CXCL10 and CXCL11 from primary airway epithelial cells.

Tyk2-IN-26 (compound 18) is a TYK2 inhibitor that suppresses TYK2/STAT signaling induced by IL-23 and IFNα, with IC₅₀ values all below 30 nM. Tyk2-IN-26 is applicable to research related to TYK2, IL-23, type I IFN signaling, as well as inflammatory immunity.

PF-06263276 (Standard) is the analytical standard of PF-06263276 (HY-101024). This product is intended for research and analytical applications. PF-06263276 (PF 6263276) is a potent and selective pan-JAK inhibitor, with IC50s of 2.2 nM, 23.1 nM, 59.9 nM and 29.7 nM for JAK1, JAK2, JAK3 and TYK2, respectively. PF-06263276 inhibits pSTAT3 and TYK2 pathway. PF-06263276 has a protective effect against ear skin inflammation.

JAK1/3-IN-1 is a selective, orally active JAK1/3 inhibitor with IC₅₀ values of 1.9 nM and 0.9 nM, respectively. JAK1/3-IN-1 significantly reduces the mean arterial blood pressure and significantly increases the heart rate in rabbits. JAK1/3-IN-1 decreases the mean arterial blood pressure in conscious telemetered rats and induces lethal cardiovascular effects.

DTP3 (Standard) is the analytical standard of DTP3 (HY-100538). This product is intended for research and analytical applications. DTP3 TFA is a potent and selective GADD45β/MKK7 inhibitor. DTP3 TFA targets an essential, cancer-selective cell-survival module downstream of the NF-κB pathway.

Abrocitinib (Standard) is the analytical standard of Abrocitinib. This product is intended for research and analytical applications. Abrocitinib (PF-04965842) is a potent, orally active and selective JAK1 inhibitor, with IC₅₀s of 29 and 803 nM for JAK1 and JAK2, respectively. Abrocitinib (PF-04965842) exhibits less active effect on TYK2 (IC₅₀, 1.253 μM), and inhibits phosphorylation of STAT1, STAT3 and STAT5 after stimulation. Effective in autoimmune disease.

Fedratinib (hydrochloride hydrate) (Standard) is the analytical standard of Fedratinib (hydrochloride hydrate). This product is intended for research and analytical applications. Fedratinib hydrochloride hydrate (TG-101348 hydrochloride hydrate) is a potent, selective, ATP-competitive and orally active JAK2 inhibitor with IC50s of 3 nM for both JAK2 and JAK2V617F kinase. Fedratinib hydrochloride hydrate shows 35- and 334-fold selectivity over JAK1 and JAK3, respectively. Fedratinib hydrochloride hydrate induces cancer cell apoptosis and has the potential for myeloproliferative disorders research.

Ritlecitinib (Standard) is the analytical standard of Ritlecitinib (HY-100754). This product is intended for research and analytical applications. Ritlecitinib (PF-06651600) is a highly selective, orally active, irreversible covalent JAK3 inhibitor (IC50=33 nM) without inhibitory activity towards JAK1, JAK2, and TYK2 (IC50 >10 μ M). Ritlecitinib rapidly inactivates the JAK3 kinase, and blocks signaling and downstream STAT phosphorylation mediated by common gamma chain cytokines such as IL-2 and IL-15. Ritlecitinib can inhibit Th1/Th17 cell differentiation and function, and effectively suppress preclinical animal models such as alopecia areata, adjuvant-induced arthritis (AIA), and experimental autoimmune encephalomyelitis (EAE).

Tofacitinib-¹³C (Tasocitinib-¹³C; CP-690550-¹³C) is the ¹³C-labeled Tofacitinib (HY-40354). Tofacitinib (Tasocitinib) is an orally active, blood-brain barrier permeable selective inhibitor of JAK1/JAK3. Tofacitinib blocks the JAK-STAT/NF-κB signaling pathway, inhibits cytokine signal transduction, phosphorylation of STAT1/STAT5, and suppresses innate and adaptive immune responses. Tofacitinib can be used in research related to major depressive disorder, rheumatoid arthritis, pulmonary diseases, systemic lupus erythematosus, and immune-mediated liver injury.

CEE321 is a potent pan-JAK inhibitor with an IC₅₀ value of 54 nM. CEE321 potently inhibits biomarkers associated with atopic dermatitis.

Gusacitinib (Standard) is the analytical standard of Gusacitinib (HY-103018). This product is intended for research and analytical applications. Gusacitinib (ASN-002) is an orally active dual SYK/JAK kinase inhibitor with IC₅₀ values of 5, 46, 4, 11 and 8 nM for SYK, JAK1, JAK2, JAK3 and TYK2, respectively. Gusacitinib rapidly and significantly suppressed key inflammatory pathways implicated in atopic dermatitis pathogenesis. Gusacitinib can be used in the research of chronic hand eczema and cancers such as basal cell carcinoma.

JAK-IN-3 (Standard) is the analytical standard of JAK-IN-3 (HY-111750). This product is intended for research and analytical applications. JAK-IN-3 (compound 22) is a potent JAK inhibitor, with IC₅₀ values of 3 nM, 5 nM, 34 nM and 70 nM for JAK3, JAK1, TYK2 and JAK2, respectively.

Graveoline (Standard) is the analytical standard of Graveoline (HY-12538). This product is intended for research and analytical applications. Graveoline (Rutamine) is an orally active alkaloid with various activities such as antifungal, antiparasitic, anti-inflammatory, and antitumor effects. Graveoline can induce tumor cell apoptosis and autophagy through a reactive oxygen species-mediated pathway. Graveoline has an MIC of 500 μg/mL for Candida albicans. Graveoline can be used in the research of various diseases such as tumors and liver injury.