AK2

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.

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.

PROTAC JAK2 degrader-1 (Compound 10i) is a JAK2 PROTAC degrader with a DC50 of 27.35 nM against JAK2V617F. It facilitates the ubiquitination and degradation of JAK2. This compound also inhibits the phosphorylation of JAK2, STAT3, and STAT5, and is applicable in the study of myeloproliferative neoplasms.

JAK2-IN-12 (compound 23) is a JAK2 inhibitor with a pIC50 value of 8.2. It is employed in the research of myelofibrosis.

JAK2-IN-13 is a potent and orally active JAK2 inhibitor with an IC50 of 54.7 nM. It downregulates the expression of p-STAT3 and p-STAT5 and exhibits good bioavailability. JAK2-IN-13 effectively suppresses recombinant human erythropoietin-induced extramedullary erythropoiesis as well as polycythemia vera. It is used in the study of myeloproliferative neoplasms.

PROTACFLT3/JAK2/BRD4 Degrader-1 is a PROTAC degrader targeting FLT3, JAK2, and BRD4, with DC50 values of 5.23 nM, 0.678 nM, and 1.17 nM, respectively. It exhibits potent antiproliferative activity against MV4;11 cells (IC50= 0.79 nM) and FLT3-mutated Ba/F3 cells. Additionally, PROTACFLT3/JAK2/BRD4 Degrader-1 induces apoptosis in MV4;11 cells and demonstrates significant antitumor efficacy in an MV4;11 xenograft model established in NOD SCID mice. This compound is applicable for research in acute myeloid leukemia (AML).

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.

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-IN-10 (compound 5) is a potent inhibitor of JAK2v617f, with an IC50 value of ≤10 nM.

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.

pJAK2(1001–1013) acts as a SOCS1/3 antagonist, enhancing the JAK/STAT signaling pathway by inhibiting the negative regulatory effects of SOCS proteins, thereby playing a crucial role in antiviral immune responses.