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).

TYK2ligand 2 is the TYK2 ligand of PROTACTYD-68. TYD-68 is a highly potent and selective CRBN-recruiting TYK2 PROTAC degrader with a DC50 value of 0.42 nM.

TYK2activator-1 (16b) is a TYK2 activator with an EC50 value of 1.78 μM. It inhibits JAK2 and JAK3 with IC50 values of 6.8 μM and 6.3 μM, respectively.

PROTAC TYK2 Degradation Agent1 is a potent, subtype-selective degrader of TYK2, exhibiting degradation activity with a DC50 of 14 nM. It is utilized in autoimmune disease research [1].

PROTAC TYK2 degrader-1 (CPD-155) functions as a selective degrader of TYK2, demonstrating a degradation maximum (D max) greater than 60%. This compound effectively targets TYK2 for degradation, utilizing a linker to connect the TYK2 ligand with the VHL ligand Thalidomide, each color-coded for identification.

TYK2ligand 1 is a ligand for TYK2, suitable for synthesizing the TYK2PROTAC degrader (CPD-155).

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.

Tyk2-IN-20 (Example 289) is an effective inhibitor of Tyk2 with an IC50 value below 5 nM. Additionally, it inhibits JAK1, JAK2, and JAK3 with IC50 values under 100 nM. This compound is utilized for the research of inflammatory diseases.

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].

Delgocitinib (JTE-052) is a JAK inhibitor and a specific JAK1/2/3/Tyk2 inhibitor (IC50=2.6-58 nM) that blocks multiple cytokine signaling pathways and inhibits pruritus, used for research on inflammatory and autoimmune diseases.

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.

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).

Soficitinib (Compound 20) is a selective inhibitor targeting tyrosine kinase 2 (TYK2) and Janus kinase 2 (JAK2), with IC50 values of 0.5 nM and 1.2 nM, respectively. It holds potential for research in autoimmune diseases such as psoriasis and rheumatoid arthritis, as well as inflammatory conditions.

JAK2-IN-14 is an orally effective JAK2 inhibitor with an IC50 of 2 nM. It exhibits selectivity for JAK2 over JAK1, JAK3, and TYK2 by factors of 89.5, 80.5, and 51 times, respectively. JAK2-IN-14 inhibits the STAT5 signaling pathway and can cause tumor cell cycle arrest and apoptosis (apoptosis). It is applicable in the research of myeloproliferative neoplasms (MPN).

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 hydrochloride 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].