ak2

JAK2 STAT3-IN-1 is a GP130 inhibitor with anti-tumor effects and can be used to study inflammation, autoimmunity and cancer.

(R)-JAK2 STAT3-IN-10a is the R-isomer of JAK2 STAT3-IN-1.JAK2 STAT3-IN-1 is a GP130 D1 structural domain inhibitor with antitumor activity that inhibits the phosphorylation of JAK2 and STAT3. The KD value of (R)-JAK2 STAT3-IN-1 on GP130 protein is 3.8 μM.

Drak2-in-1, a potent, selective and ATP-competitive DRAK2 inhibitor, has an IC50 and KIvalue of 3 nM and 0.26 nM, respectively.Drak2-in-1 also had an effect on DRAK1 (IC50=51 nM).

JAK2-IN-4 is a selective JAK2 JAK3 inhibitor, with IC50 values of 0.7 nM and 23.2 nM for JAK2 and JAK3, respectively.

JAK2-IN-11 (Example 6) is a JAK2 kinase inhibitor with potent antitumor activity, exhibiting an IC50 of ≤10 nM against JH2 BIND WT V617F. This compound effectively suppresses tumor growth.

BAK2-66 is a selective antagonist of the dopamine D3 receptor.

JAK2 Inhibitor V (JAK2 Inhibitor V Z3) is a novel specific inhibitor of Jak2, inhibiting Jak2-V617F and Jak2-WT autophosphorylation in a dose-dependent manner.

TAK285-IODO, similar to TAK285 in which the trifluoro group is replaced by iodo, is a novel dual erbB protein kinase inhibitor that specifically targets human epidermal growth factor receptor (EGFR) and HER2.

JAK2-IN-7, a selective inhibitor targeting Janus Kinase 2 (JAK2), exhibits inhibitory concentrations (IC50) of 3 nM for JAK2, 11.7 nM for SET-2 cells, and 41 nM for Ba F3 V617F cells, indicative of its potency and selectivity. This compound demonstrates more than 14-fold selectivity against JAK1, JAK3, and FLT3, underlining its specificity. JAK2-IN-7 effectively induces cell cycle arrest at the G0 G1 phase and promotes apoptosis in tumor cells, manifesting significant antitumor activities [1].

JAK2-IN-6, a polysubstituted aminothiazole derivative, is a potent and selective inhibitor of JAK2 (ic50 at 22.86 μg mL). Jak2-in-6 inhibits the activity of JAK2 enzymes by interfering with Jak2-related signaling pathways, thereby producing therapeutic effects on the specific disease IN which JAK2 is dysregulated, and does not show activity on JAK1 and JAK3. JAK2 is a protein involved in signaling pathways that regulate cell growth and division. Abnormal activation of JAK2 has been linked to a variety of diseases, including some types of cancer and inflammatory diseases. JAK2-IN-6 has antiproliferative activity against cancer cells.

α7 nAchR-JAK2-STAT3 agonist 1 is a potent inhibitor of the α7 nAchR-JAK2-STAT3 pathway that acts on nitric oxide (NO) (IC50: 0.32 μM). It has demonstrated positive effects on iNOS, IL-1β, and IL-1β in murine macrophages RAW264.7, and inhibited the expression of iNOS, IL-1β, and IL-6 in mouse macrophages. Additionally, α7 nAchR-JAK2-STAT3 agonist 1 suppressed LPS-induced NO release, NF-κB activation, and cytokine production, making it useful for studying sepsis.

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

JAK2 FLT3-IN-1 (TFA) is an orally active dual inhibitor of JAK2 (IC50: 0.7 nM) and FLT3 (IC50: 4 nM) that demonstrates anticancer effects, also affecting JAK1 (IC50: 26 nM) and JAK3 (IC50: 39 nM).

JAK2 JH2 binder-1 is a potent and selective JAK2 JH2 binder (Ki: 37.1 nM). JAK2 JH2 binder-1 has the potential to be used in the study of various myeloproliferative neoplasms.

Jak2-IN-7j is a selective Jak2 inhibitor which demonstrates a time-dependent knock-down of pSTAT5, which is a downstream target of Jak2.

Compound A8, known as JAK2-IN-9, is a selective JAK2 inhibitor with an IC50 of 5 nM. It effectively inhibits the phosphorylation of JAK2, STAT3, and STAT5, possesses metabolic stabilities, and induces apoptosis. This compound is utilized in the study of myeloproliferative neoplasms (MPNs) [1].

Tubulin JAK2-IN-1 (compound 7g) is a potent dual inhibitor of Janus kinase 2 (JAK2) and microtubules, exhibiting significant antiproliferative effects against cancer cells [1].

JAK2 FLT3-IN-3 (11r) is a dual inhibitor of FLT3 and JAK2, with IC50 values respectively at 0.51 nM for FLT3, 2.01 nM for JAK2, and 104.40 nM for JAK3. It can induce apoptosis and exhibits anticancer activity.

Itaconate-alkyne (ITalk) is a bioorthogonal probe for quantitative, site-specific chemoproteomic profiling of itaconate in inflammatory macrophages, facilitating biochemical evaluation and proteomic analysis of its direct targets.

AK-2-38 is a nifedipine analogue with potent smooth muscle calcium antagonist action and partial agonist effects on isolated guinea pig left atrium.

JAK-IN-23 is an orally active dual JAK STAT and NF-κB inhibitor that inhibits JAK1 (IC50: 8.9 nM), JAK2 (IC50: 15 nM), and JAK3 (IC50: 46.2 nM). It exhibits strong anti-inflammatory effects and can reduce the release of various pro-inflammatory factors. JAK-IN-23 can be used to study inflammatory bowel disease (IBD).