jak in 1

JAK-IN-1 shows improved selectivity for JAK3 over JAK1. JAK-IN-1 is a JAK1/2/3 inhibitor with IC50s of 0.26, 0.8 and 3.2 nM, respectively.

JAK-STAT-IN-1 is a specific JAK-STAT inhibitor indicated for the study of autoimmune diseases.

HDAC/JAK/BRD4-IN-1 (compound 25ap) is a potent triple inhibitor targeting HDAC, JAK, and BRD4. This compound not only inhibits cell proliferation but also induces apoptosis in MDA-MB-231 cells and demonstrates in vivo anticancer efficacy [1].

JAK-2 3-IN-1 is a highly effective inhibitor targeting both JAK-2 and JAK-3 isoforms, exhibiting remarkable potency with Ki values below 250 nM for both isoforms.

JAK kinase-IN-1 (Example 1) is a potent inhibitor targeting the JAK family, including TYK2, JAK1, JAK2, and JAK3, with IC50 values of 4.2 nM, 32 nM, 27 nM, and 3473 nM, respectively [1].

SYK/JAK-IN-1 is a dual SYK/JAK inhibitor with IC50 values of less than 5 nM for both SYK and JAK2.

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

JAK1/2/3 Inhibitor 1 is a potent protein kinase inhibitor.JAK1/2/3 Inhibitor 1 has antitumor activity that inhibits the growth of a variety of cancer cell lines. It inhibits the growth of cancer cells by binding to the cancer cell backbone and inhibiting the production of new proteins.

JAK3/ BTk-in-1 is a dual JAK3/BTK inhibitor that specifically targets and inhibits Janus kinase 3 (JAK3) and Bruton's tyrosine kinase (BTK), two important targets in autoimmune diseases. JAK3/ BTk-in-1 simultaneously inhibited the BTK/JAK3 signaling pathway, showing a synergistic effect. JAK3/ BTK-in-1 is a potential compound for the treatment of immune-related diseases, such as autoimmune diseases, certain types of cancer (including lymphoma and leukemia), and other diseases that may be characterized by an unbalanced immune response.

JAK1-IN-8, a specific inhibitor of Janus kinase 1 (JAK1, IC50<500 nM).

JAK1 TYK2-IN-4 serves as a dual inhibitor targeting both JAK and TYK2, displaying IC50 values of 39 nM and 21 nM, respectively. It is also orally bioavailable [1].

JAK1-IN-4 is a selective JAK1 inhibitor (IC50s: 85 nM, 12.8 μM and >30 μM for JAK1, JAK2, and JAK3, respectively). JAK1-IN-4 inhibits STAT3 phosphorylation in NCI-H 1975 cells (IC50, 227 nM).

JAK3-IN-1 is a selective and orally active JAK3 inhibitor (IC50: 4.8 nM). JAK3-IN-1 displays over 180-fold more selective for JAK3 than JAK1 (IC50: 896 nM) and JAK2 (IC50: 1050 nM).

JAK1 TYK2-IN-1 is a dual inhibitor of TYK2 [IC50 = 29 nM] and JAK1 (IC50 = 41 nM).

JAK1-IN-9 (compound 23a) is a potent, selective JAK1 inhibitor with an IC50 of 72 nM, exhibiting over 12-fold selectivity against other JAK family members [1].

JAK2/FLT3-IN-1 has anti-cancer activity. JAK2/FLT3-IN-1 is a potent and orally effective dual JAK2/FLT3 (Janus kinase 2/ FMS-like tyrosine kinase 3) inhibitor with IC50 values of 0.7 nM, 4 nM, 26 nM and 39 nM for JAK2, FLT3, JAK1 and JAK3, respectively.

JAK3 Covalent Inhibitor-1 is a compound characterized by its potent and selective inhibition of Janus kinase 3 (JAK3), possessing an IC50 of 11 nM and demonstrating a 246-fold selectivity compared to other JAKs.

JAK1 TYK2-IN-3 is a selective, potent, orally active dual inhibitor of TYK2 (IC50: 6 nM) and JAK1 (IC50: 37 nM), with selective action on JAK2 (IC50: 140 nM) and JAK3 (IC50: 362 nM). It regulates the expression of TYK2 JAK1-related genes and formation of Th1, Th2, and Th17 cells to exert anti-inflammatory activity.

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.

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.

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].

JAK1-IN-11 (compound 11) is a potent Janus kinase inhibitor with nanomolar IC50 values of 0.02 nM for JAK1 and 0.44 nM for JAK2, demonstrating high selectivity for JAK1 over JAK2 [1].

JAK1-IN-10 (compound 9), a cyano-substituted cyclic hydrazine derivative, is a potent and selective inhibitor of JAK1 [1].

JAK1-IN-B61 is a JAK1 inhibitor.

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

JAK1-IN-13 (compound 36b) functions as an orally active, potent, and highly selective JAK1 inhibitor, exhibiting an IC 50 of 0.044 nM. It effectively reduces STAT3 phosphorylation [1].

JAK1-IN-12, a selective inhibitor of JAK1, exhibits an IC50 of 0.0246 μM and demonstrates IC50 values of 0.423 μM, 0.410 μM, and 1.12 μM for JAK2, JAK3, and TYK2, respectively. It promotes hair growth in mice and is applicable for researching immune and inflammatory diseases [1].

Osunprotafib (ABBV-CLS-484) is a potent, orally bioavailable PTP1B PTPN2 inhibitor in clinical trials for solid tumors. [1] Osunprotafib (ABBV-CLS-484) stimulates the tumor microenvironment and promotes natural killer cell and CD8 T cell function and enhances T cell anti-tumor immunity by enhancing JAK-STAT signaling and reducing T cell dysfunction. [2]

Upadacitinib (ABT-494) (ABT-494) is a selective Janus kinase (JAK) 1 inhibitor, which is being studied for the treatment of several autoimmune disorders in the IC50 of 43 nM.

JAK3-IN-11 (Compound 12) exhibits potent, noncytotoxic, irreversible, orally active JAK3 inhibitory activity (IC50 = 1.7 nM) with an excellent selectivity profile (>588-fold compared to other JAK isoforms), covalently binds to the ATP-binding pocket in JAK3. JAK3-IN-11 strongly inhibits JAK3-dependent signaling and T-cell proliferation which is a promising tool for studying autoimmune diseases [1].

JAK-IN-5 hydrochloride is a JAK inhibitor [1].

Momelotinib (LM-1149) is an orally bioavailable small-molecule inhibitor of Janus kinases 1 and 2 (JAK1/2) with IC50 of 11 nM/18 nM. JAK1/2 inhibitor CYT387 competes with JAK1/2 for ATP binding, which may result in inhibition of JAK1/2 activation, inhibition of the JAK-STAT signaling pathway, and so the induction of apoptosis and a reduction of tumor cell proliferation in JAK1/2-expressing tumor cells.

W1131 TFA is a potent STAT3 inhibitor inducing ferroptosis and effectively halting cancer progression in subcutaneous xenograft, organoid, and PDX models of gastric cancer. It mitigates chemoresistance to 5-FU in cancer cells and modulates the cell cycle, DNA damage response, and oxidative phosphorylation, targeting pathways such as IL6-JAK-STAT3 and ferroptosis [1].

Mollugin (Rubimaillin) may be a JAK2 inhibitor and inhibits LPS-induced inflammatory responses by blocking the activation of the JAK-STAT pathway. Mollugin as a candidate for a chemotherapeutic agent in OSCCs via the upregulation of the HO-1 and Nrf2 pathways and the downregulation of NF- κ B. Mollugin may be a novel therapeutic candidate for bone loss-associated disorders including osteoporosis, rheumatoid arthritis, and periodontitis. Also, it has anticancer efficacy, can modulate the HER2 pathway in HER2-overexpressing Y cells with a potential role in the treatment and prevention of human breast and ovarian Y with HER2 overexpression.

JAK-IN-27, also known as compound 1, is an orally active, potent inhibitor of the JAKS family kinases, displaying inhibitory concentrations (IC50s) of 3.0 nM for TYK2, 7.7 nM for JAK1, and 629.6 nM for JAK3. Moreover, JAK-IN-27 impedes IFN-α2B-induced phosphorylation of STAT3 in Jurkat cells with an IC50 of 23.7 nM [1].

TK4b can be used in the research of leukemia cancer and lymphoid-derived diseases. TK4b is a Janus kinase (JAK) inhibitor with the IC50 values of 18.42 nM and 19.40 nM for JAK3 and JAK2, respectively [1].

JAK-IN-14 is a potent and selective JAK1 inhibitor with an IC50 of <5 μM, exhibiting over 8-fold selectivity for JAK1 compared to JAK2 and JAK3 [1].

Upadacitinib-15N-d2 the 15N and deuterated compound of Upadacitinib. Upadacitinib has a CAS number of 1310726-60-3. Upadacitinib (ABT-494) is a selective Janus kinase (JAK) 1 inhibitor, which is being studied for the treatment of several autoimmune disorders in the IC50 of 43 nM.

W1131, a potent STAT3 inhibitor, effectively triggers ferroptosis and suppresses cancer progression across various models including gastric cancer cell subcutaneous xenograft, organoids, and patient-derived xenograft (PDX). Additionally, W1131 overcomes chemical resistance in cancer cells to 5-FU by regulating cell cycle, DNA damage response, and oxidative phosphorylation pathways, notably the IL6-JAK-STAT3 and ferroptosis pathways [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].

Tofacitinib metabolite-1, a derivative of Tofacitinib, which is a JAK inhibitor, is employed in studies focused on the pharmacokinetics and metabolism of tofacitinib[1][2].

Lepzacitinib, a Janus kinase inhibitor, specifically targets JAK 1/3. It demonstrates an anti-inflammatory effect and efficacy in inhibiting atopic dermatitis as well as other skin diseases [1].

JAK-IN-26 (compound 2) is an orally active Janus kinase (JAK) inhibitor with favorable pharmacokinetic properties, demonstrating potency in suppressing IFN-α2B-induced STAT3 phosphorylation in Jurkat cells, with an IC50 value of 17.2 nM [1].

JAK-IN-28 (Compound 111) is a Janus kinase (JAK) inhibitor with potential applicability in cancer and inflammatory disease research [1].

1. Ganoderic acid A exhibits antitumor activity, mediated through its inhibitory effect on nuclear transcription factor-kappaB and activator protein-1. 2. Ganoderic acid A can induce proliferation inhibition, apoptosis and suppression of invasion in human

1. Curculigoside (Curculigoside A) can prevent bone loss , improve osteogenesis and inhibit osteoclastogenesis of hAFSCs, suggesting its potential use to regulate hAFSC osteogenic differentiation for treating bone disorders. 2. Curculigoside can promote calcium deposition and increase the levels of ALP and Runx2 in osteoblasts under oxidative stress via anti-oxidative character. 3. Curculigoside possesses potent antioxidant properties against oxidative stress insults. can protect endothelial cells against oxidative injury induced by H2O2, suggesting that this compound may constitute a promising intervention against cardiovascular disorders.

JAK HDAC-IN-3 (13a), a dual inhibitor of JAK and HDAC, exhibits IC50 values of 25.36 nM for JAK2, 0.2 μM for HDAC, and 0.43 μM for HDAC1, respectively [1].

Upadacitinib is a potent and selective JAK inhibitor. Upadacitinib is approximately 74 fold selective for Jak1 over Jak2 in cellular assays dependent on specific, relevant cytokines. Upadacitinib demonstrates efficacy in rat arthritis models.