Janus kinase (JAK) is a family of intracellular, nonreceptor tyrosine kinases that transduce cytokine-mediated signals via the JAK-STAT pathway.Members of the type I and type II cytokine receptor families depend on the JAK family of tyrosine kinases to phosphorylate and activate downstream proteins involved in their signal transduction pathways because they lack catalytic kinase activity.The receptors have two intracellular signal-transducing domains because they are paired polypeptides. Each intracellular domain contains a proline-rich region called a box1/box2 region that is close to the cell membrane and where JAKs bind. The two JAKs are brought close enough to phosphorylate one another after the receptor undergoes a conformational change following association with the corresponding cytokine or ligand. By further phosphorylating and activating STAT transcription factors, JAK autophosphorylation causes a conformational change within itself, enabling it to transduce the intracellular signal. When STATs are activated, they separate from their receptor and coalesce into dimers before moving into the cell nucleus, where they control the transcription of particular genes.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
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V0327 | Go6976 (PD40697) | 136194-77-9 | Go6976 (also known as PD-40697) is a novel, potent and selective inhibitor of PKC (Protein Kinase C)with potential antitumor activity. |
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V31779 | Golidocitinib (AZD-4205) | 2091134-68-6 | Golidocitinib (AZD-4205; JAK1-IN-3) is a novel and potent JAK1 (Janus Kinase)inhibitor with anticancer activity. |
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V53204 | Golotimod hydrochloride (SCV 07 hydrochloride; Gamma-D-glutamyl-L-tryptophan hydrochloride) | 1029401-59-9 | Golotimod (SCV 07) HCl An immunomodulatory peptide with antimicrobial activity that significantly increases efficacy in anti-tuberculosis studies, stimulates thymic and splenocyte proliferation, and improves macrophage function. |
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V53639 | Golotimod TFA (SCV 07 TFA; Gamma-D-glutamyl-L-tryptophan TFA) | 2828433-07-2 | Golotimod TFA (SCV 07 TFA) An immunomodulatory peptide with antimicrobial activity that significantly increases the efficacy of anti-tuberculosis studies, stimulates thymus and splenocyte proliferation, and improves macrophage function. |
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V51529 | GS-829845 | 1257705-09-1 | GS-829845 is the primary active adjuvant of filgotinib. |
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V51512 | Gusacitinib (ASN002) HCl | 2228989-14-6 | Gusatinib HCl (ASN-002) is an interface-potent SYK/JAK diploid, which inhibits SYK, JAK1, JAK2, JAK3 and TYK2 with IC50s of 5, 46, 4, 11 and 8 nM, respectively. |
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V51521 | HAT-SIL-TG-1&AT | HAT-SIL-TG-1&AT is a Janus tyrosine kinase (JAK) inhibitor (antagonist) with anti-tumor effects. | |
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V51977 | HODHBt (HOOBt) | 28230-32-2 | HODHBt (HOOBt) inhibits the STAT5-SUMO interaction and can block the SUMOylation of phosphorylated STAT5. |
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V26667 | Ilginatinib (NS-018) | 1239358-86-1 | Ilginatinib (NS018;NS-018) is an orally bioavailable, small molecule inhibitor of Janus-associated kinase 2 (JAK2) and Src-family kinases, with potential antineoplastic activity. |
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V51524 | Ilunocitinib | 1187594-14-4 | Ilunocitinib (compound 27) is an inhibitor (blocker/antagonist) of JAK (information from patent WO2009114512A1). |
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V0065 | Itacitinib (INCB-039110) | 1334298-90-6 | Itacitinib (also known as INCB39110) is a potent, selective and orally bioavailable inhibitor of JAK1 (Janus-associated kinase 1)with >20-fold selectivity for JAK1 over JAK2 and >100-fold over JAK3 and TYK2 (IC50 for JAK1, 2, 3, and TYK2 are 2, 63, >2000, and 795 nM, respectively). |
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V0066 | Itacitinib adipate (INCB 39110 adipate) | 1334302-63-4 | Itacitinib adipate, the adipate salt of itacitinib which is also known as INCB39110, is a potent, selective and orally bioavailable inhibitor of JAK1 (Janus-associated kinase 1)with potential antineoplastic activity, currently in Phase II clinical trials for the treatment of myelofibrosis, rheumatoid arthritis and plaque psoriasis. |
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V51519 | Itacnosertib (TP-0184) | 1628870-27-8 | Itacnosertib (TP-0184) is an inhibitor (blocker/antagonist) of JAK2, ACVR1 (ALK2) and ALK5 as described in WO2014151871. |
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V51548 | J30-8 | 2366255-71-0 | J30-8 is a highly efficient, isoform-selective JNK3 conjugate with IC50 of 40 nM and 2500-fold selectivity over JNK1α1 and JNK2α2 isoforms. |
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V56097 | JAKkinase-IN-1 | 2698389-43-2 | JAK kinase-IN-1 (Example 1) is a JAK inhibitor. |
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V51494 | JAK-2/3-IN-1 | 1036241-36-7 | JAK-2/3-IN-1 is a potent JAK-2 and JAK-3 analogue. |
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V51492 | JAK-2/3-IN-3 | 2242031-31-6 | JAK-2/3-IN-3 (compound ST4j) is a potent JAK2/3 surrogate with IC50s of 13.00 and 14.86 nM for JAK2 and JAK3, respectively. |
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V51487 | JAK-IN-14 | 1973485-06-1 | JAK-IN-14 is a potent and specific JAK1 pairing with IC50 of less than 5 μM. |
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V51501 | JAK-IN-15 | 1973485-05-0 | JAK-IN-15 is a JAK inhibitor WO2016119700A1 (Compound 15). |
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V51486 | JAK-IN-21 | 2445499-20-5 | JAK-IN-21 (Example 4) is a selective and efficient JAK conjugate with IC50 of 1.73, 2.04, 109 and 62.9 nM for JAK1, JAK2, J2V617F and TYK2 respectively. |
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