tyk2 in 2

TyK2-IN-2 is a selective inhibitor of TYK2 (IC50s: 7 nM, 0.1 μM, and 0.05 μM for TYK2 JH2, IL-23, and IFNα).

RO495 (CS-2667), a potent inhibitor of TYK2, inhibits TYK2 with IC50 of 1.5nM as tested in cell-based pharmacological assays

Tyk2-IN-3 is an inhibitor of Tyk2 pseudokinase (IC50: 485 nM).

Tyk2-IN-5 is a selective and orally active inhibitor of Tyk2 JH2 (Ki: 0.086 nM for Tyk2 JH2; IC50: 25 nM for IFNα).

Tyk2-IN-7 is an inhibitor of TYK2 JH2, binds to the TYK2 JH2 domain (IC50: 0.00053 μM; Ki.app: 0.00007 μM).

Tyk2-IN-9 (Compound 26), a selective Tyk-2 inhibitor, exhibits IC50 values of 0.076 nM for TYK2-JH2 and 1.8 nM for JAK1-JH2, respectively. This specificity makes it suitable for research into inflammatory or autoimmune diseases [1].

Bayer-18 is an inhibitor of TYK2. It inhibits the viability of anaplastic large cell lymphoma cells, including K299, SR786, Mac1, and Mac2a, with an IC50 ranging from 2-3 µM. Additionally, Bayer-18 induces apoptosis in K299 and SR786 cells.

Tyk2-IN-22 (Compound A8) is a selective inhibitor of tyrosine kinase 2 (Tyk2), effectively inhibiting Tyk2, JAK1, and JAK3 with IC50 values of 9.7 nM, 148.6 nM, and 883.3 nM, respectively. Additionally, Tyk2-IN-22 suppresses downstream STAT5 phosphorylation.

DualCathepsinL JAK-IN-1 (Compound A8) serves as a dual inhibitor of Cathepsin L (CTSL) and JAK, exhibiting IC50 values of 0.68 μM for CTSL and 337.1 nM, 5.251 nM, 27.29 nM, and 172.6 nM for JAK1 2 3 and TYK2, respectively. This compound effectively prevents the activation of MAPK, NF-κB, and JAK STAT signaling pathways, leading to significant anti-inflammatory therapeutic effects. DualCathepsinL JAK-IN-1 is applicable in research on acute lung injury (ALI).

TYK2-IN-11 (Compound 5B) is a potent and selective inhibitor of Tyk-2, with IC50 values of 0.016 nM for TYK2-JH2 and 0.31 nM for JAK1-JH2. This compound shows potential for advancing research in inflammatory and autoimmune diseases [1].

TYK2-IN-12 (compound 30) is a selective, orally active inhibitor of TYK2 (tyrosine kinase 2) (Ki: 0.51 nM). It inhibits IL-12-induced IFNγ in human and mouse whole blood with IC50 values of 2.7 and 7.0 μM, respectively, and can be used to study psoriasis.

JAK2 TYK2-IN-2 is a potent and selective inhibitor of TYK2 [IC50: 9 nM] and JAK2 [IC50: 157 nM], exhibiting anti-inflammatory effects.

Deucravacitinib HCl is a Highly Potent and Selective Allosteric Inhibitor of TYK2. BMS-986165 Blocks Il-12, IL-23 and type I Interferon Signaling and Provides for Robust Efficacy in Preclinical Models of Inflammatory Bowel Disease. MS-986165 potently binds to the Tyk2 pseudokinase domain (Ki = 0.02 nM), and is highly selective against a panel of 265 kinases and pseudokinases. The compound potently inhibited IL-23-, IL-12-, and Type I interferon-driven cellular signaling and transcriptional responses (IC50 range 2-14 nM).

JAK-IN-30 (compound 31) is a water-soluble Janus kinase (JAK) inhibitor with IC50 values of 2 nM for JAK2, 15 nM for JAK1, 18 nM for JAK3, and 2 nM for TYK2, identified for its research potential in treating dry eye disease (DED) [1].

ABBV-712 is a selective Tyrosine Kinase 2 (TYK2) inhibitor, demonstrating an IC50 value of 0.195 μM, and is implicated in the regulation of autoimmune diseases [1].

Ivarmacitinib (SHR0302) sulfate, a potent and orally active inhibitor of all JAK family members, exhibits particular selectivity towards JAK1. Its selectivity is >10-fold greater for JAK1 compared to JAK2, 77-fold more than JAK3, and 420-fold more than Tyk2. Ivarmacitinib effectively inhibits JAK1-STAT3 phosphorylation, thereby inducing apoptosis in hepatic stellate cells. Additionally, it demonstrates notable anti-proliferative and anti-inflammatory properties [1] [2].

Tyk2-IN-15 (Compound 97) is a selective inhibitor of tyrosine kinase 2 (Tyk2) with an IC50 value ≤ 10 nM for Tyk2-JH2. It is utilized in the research of inflammatory and autoimmune diseases [1].

Tyk2-IN-10 acts as an inhibitor of the Tyrosine Kinase 2 (Tyk2)-mediated signaling pathway, which plays a role in inflammation regulation.