jak 1

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

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.

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).

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.

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

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 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].

Ruxolitinib (INCB018424) is a JAK1/2 inhibitor (IC50=3.3/2.8 nM) that is potent and selective. Rixolitinib exhibits antitumor activity and induces autophagy and apoptosis.

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.

Baricitinib (INCB028050) is a JAK1 and JAK2 inhibitor (IC50=5.9/5.7 nM) with selective and oral activity. Baricitinib has potential anti-inflammatory, immunomodulatory and anti-tumor activity.

Itacitinib (INCB039110) is an orally bioavailable Janus-associated kinase 1 (JAK1) inhibitor with potential antineoplastic activity.

Tofacitinib (Tasocitinib) is a Janus kinase inhibitor that inhibits JAK3/2/1 (IC50=1/20/112 nM) and is orally active. Tofacitinib is used for the treatment of moderate to severe rheumatoid arthritis.

Abrocitinib (PF-04965842) (PF-04965842) is a potent, specific and orally-active JAK1 inhibitor (IC50s: 29/803 nM for JAK1/2).

NVP-BSK805 2HCl (1092499-93-8(free base)) (BSK 805)(IC50=0.5 nM), a specific and effective ATP-competitive JAK2 inhibitor, is more than 20-fold specificity over JAK1, JAK3 and TYK2.

Tofacitinib Citrate (CP-690550 citrate) is a a potent, cell-permeable inhibitor of JAK1/2/3 (IC50s: 1/20/112 nM).

Ruxolitinib phosphate (INCB18424 phosphate) is a JAK1 2 inhibitor with IC50 of 3.3 nM 2.8 nM. Its selectivity for JAK1 2 is more than 130 times that of JAK3.

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.

Flonoltinib (JAK2/FLT3-IN-1) is an orally active and potent JAK2/FLT3 inhibitor, inhibiting JAK2, FLT3, JAK1, and JAK3. Flonoltinib has anti-cancer activity and can be used for studying myeloproliferative neoplasms.

JAK3-IN-1 is an orally active, selective and potent JAK3 inhibitor that can be used to study immune system diseases.

Pyridone 6 (JAK Inhibitor)(CMP 6) is a potent and selective inhibitor of JAK1 (IC50=15 nM, murine JAK1), JAK2 (IC50=1 nM), JAK3 (Ki=5 nM), and Tyk2 (IC50=1 nM); displaying significantly weaker affinities (130 nM to 10 mM) for other protein tyrosine kinases.

Ifidancitinib (ATI-50002) is a specific JAK kinase 1 3 inhibitor that induces hair growth in AA-affected C3H HeJ mice.Ifidancitinib can be used to study autoimmune diseases.

Fosifidancitinib is a potent inhibitor of JAK 1 and JAK 3.

NVP-BSK805 (BSK 805) is an ATP-competitive JAK2 inhibitor.

Golidocitinib (AZD4205) is a selective JAK1 inhibitor with an IC50 of 73 nM, while it weakly inhibits JAK2 and JAK3 with IC50 values greater than 14.7 μM and 30 μM, respectively.