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You are here:Home-Inhibitors & Agonists-JAK/STAT Signaling-JAK

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Janus kinase (JAK) is a family of intracellular, nonreceptor tyrosine kinases that transduce cytokine-mediated signals via the JAK-STAT pathway. Since members of the type I and type II cytokine receptor families possess no catalytic kinase activity, they rely on the JAK family of tyrosine kinases to phosphorylate and activate downstream proteins involved in their signal transduction pathways. The receptors exist as paired polypeptides, thus exhibiting two intracellular signal-transducing domains. JAKs associate with a proline-rich region in each intracellular domain, which is adjacent to the cell membrane and called a box1/box2 region. After the receptor associates with its respective cytokine/ligand, it goes through a conformational change, bringing the two JAKs close enough to phosphorylate each other. The JAK autophosphorylation induces a conformational change within itself, enabling it to transduce the intracellular signal by further phosphorylating and activating transcription factors called STATs. The activated STATs dissociate from the receptor and form dimers before translocating to the cell nucleus, where they regulate transcription of selected genes.

Cat. No. Product Name CAS No. Information
H9585

Povorcitinib

 		1637677-22-5

Povorcitinib is a potent and selective inhibitor of JAK1. Povorcitinib has the potential for the research of disease selected from cutaneous lupus erythematosus (CLE) and Lichen planus (LP) .
H9530

Atinvicitinib

 		2169273-59-8

Atinvicitinib is a selectivity,highly ligand efficient and efficacious Janus Kinase 1 inhibitor with IC50 value of 0.1 nM; Atinvicitinib has the potential for the research of atopic dermatitis .
H9479

Ilunocitinib

 		1187594-14-4

Ilunocitinib is a potent Janus kinase inhibitor
H9374

PF-06826647

 		2127109-84-4

PF-06826647(Ropsacitinib) is an orally active and selective TYK2 inhibitor (IC50=17 nM), which binds to TYK2 catalytically active JH1 domain. PF-06826647 displays selectivity for TYK2 over JAK1 (IC50=383 nM) and JAK2 (74 nM);PF-06826647 can be used for the research of psoriasis, ulcerative colitis, and hidradenitis suppurativa.
H9373

BMS-986202

 		1771691-34-9

BMS-986202 is a potent, selective and orally active Tyk2 inhibitor that binds to Tyk2 JH2 with an IC50 of 0.19 nM and a Ki of 0.02 nM; BMS-986202 is remarkably selective over other kinases including Jak family members. BMS-986202 is also a weak inhibitor of CYP2C19 with an IC50 of 14 μM. BMS-986202 can be used for IL-23-driven acanthosis, anti-CD40-induced colitis, and spontaneous lupus research.
H9249

NSC33994

 		82058-16-0

NSC 33994 (G6) is a selective JAK2 inhibitor, with an IC50 of 60 nM.
H9248

ZM 449829

 		4452-06-6

ZM 449829 is a potent, selective and ATP competitive inhibitor of JAK3, with a pIC50 of 6.8. ZM 449829 will be useful pharmacological tools for the investigation of the JAK3.
H9188

Nezulcitinib

 		2412496-23-0

Nezulcitinib is a potent JAK kinase inhibitors for treatment of respiratory diseases.
H8971

SHR-0302 sulfate

 		1639419-51-4

SHR0302 sulfate(Ivarmacitinib) is a potent and orally active all members of the JAK family inhibitor, particularly JAK1. The selectivity of SHR0302 for JAK1 is >10-fold for JAK2, 77-fold for JAK3, 420-fold for Tyk2. SHR0302 inhibits JAK1-STAT3 phosphorylation and induces the apoptosis of hepatic stellate cells. SHR0302 has anti-proliferative and anti-inflammatory effects.
H8970

SHR-0302

 		1445987-21-2

SHR0302(Ivarmacitinib) is a potent and orally active all members of the JAK family inhibitor, particularly JAK1. The selectivity of SHR0302 for JAK1 is >10-fold for JAK2, 77-fold for JAK3, 420-fold for Tyk2. SHR0302 inhibits JAK1-STAT3 phosphorylation and induces the apoptosis of hepatic stellate cells. SHR0302 has anti-proliferative and anti-inflammatory effects.

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