JAK1 Inhibitor

JAK1 Inhibitors (99):

Cat. No.	Product Name	Effect	Purity

HY-130247A

Flonoltinib TFA	Inhibitor	99.77%
Flonoltinib TFA is a potent and orally active dual JAK2/FLT3 inhibitor with IC₅₀ values of 0.7 nM, 4 nM, 26 nM and 39 nM for JAK2, FLT3, JAK1 and JAK3, respectively. Flonoltinib TFA has anti-cancer activity.

HY-152080

TUL01101	Inhibitor	99.71%
TUL01101 is a potent, selective and orally active JAK1 inhibitor, with an IC₅₀s of 3, 37, 1517 and 36 nM for JAK1, JAK2, JAK3, and TYK2, respectively. TUL01101 can be used for the research of rheumatoid arthritis.

HY-153440

JAK-IN-25	Inhibitor	98.44%
JAK-IN-25 (compound 19) is a potent JAK inhibitor with IC₅₀s of 6 nM, 21 nM, 8 nM, 1051 nM for TYK2, JAK1, JAK2, JAK3, respectively. JAK-IN-25 inhibits human whole blood IL-12 (HEB IL-12) with an IC₅₀ of 28 nM. JAK-IN-25 has the potential for cancer research.

HY-W394903

GS-829845	Inhibitor	99.91%
GS-829845 is a major, active metabolite of Filgotinib (HY-18300). GS-829845 is a JAK1 preferential inhibitor but is approximately 10-fold less potent than the parent and with a longer half-life.

HY-161618

MJ04	Inhibitor	98.08%
MJ04 is a selective inhibitor for Janus Kinase 3 (JAK 3) with an IC₅₀ of 2.03 nM. MJ04 inhibits T cell differentation and inhibits the proinfammatory cytokines in Lipopolysaccharides (HY-D1056)‑induced macrophages. MJ04 exhibits good pharmacokinetic characters in mice, promotes hair growth in DHT-induced androgenetic alopecia (AGA) in athymic mice model, without significant toxicity (LD₅₀ >2 g/kg).

HY-148060

JAK-IN-21	Inhibitor	99.72%
JAK-IN-21 (Example 4) is a selective and potent JAK inhibitor with IC₅₀s of 1.73, 2.04, 109 and 62.9 nM against JAK1, JAK2, J2V617F and TYK2, respectively.

HY-162248

JAK1/2-IN-1	Inhibitor	98.36%
JAK1/2-IN-1 is a potent JAK1 and JAK2 inhibitor with IC₅₀ values of 0.4 nM and 8.1 nM, respectively. JAK1/2-IN-1 also inhibits IL-4 and IL-13 with IC₅₀s of 136.5 nM and 19.1 nM, respectively (WO2023244775A1; Example 33a).

HY-13450

ZM 449829	Inhibitor	99.73%
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.

HY-50859

Ruxolitinib sulfate	Inhibitor
Ruxolitinib sulfate (INCB018424 sulfate) is the first potent, selective JAK1/2 inhibitor to enter the clinic with IC₅₀s of 3.3 nM/2.8 nM, and has > 130-fold selectivity for JAK1/2 versus JAK3.

HY-19569A

Upadacitinib tartrate tetrahydrate	Inhibitor
Upadacitinib (ABT-494) tartrate tetrahydrate is a potent, orally active and selective Janus kinase 1 (JAK1) inhibitor (IC₅₀=43 nM). Upadacitinib tartrate tetrahydrate displays approximately 74 fold selective for JAK1 over JAK2 (200 nM) in cellular assays dependent on specific, relevant cytokines. Upadacitinib tartrate tetrahydrate can be used for several autoimmune disorders research.

HY-19568A

Peficitinib hydrobromide	Inhibitor
Peficitinib (ASP015K) hydrobromide is an orally active JAK inhibitor, with IC₅₀s of 3.9, 5.0, 0.7 and 4.8 nM for JAK1, JAK2, JAK3 and Tyk2, respectively.

HY-14722C

NVP-BSK805 trihydrochloride	Inhibitor
NVP-BSK805 trihydrochloride trihydrochloride is an ATP-competitive JAK2 inhibitor, with IC₅₀s of 0.48 nM, 31.63 nM, 18.68 nM, and 10.76 nM for JAK2 JH1 (JAK homology 1), JAK1 JH1, JAK3 JH1, and TYK2 JH1, respectively.

HY-16379A

Pacritinib hydrochloride	Inhibitor
Pacritinib hydrochloride is a potent inhibitor of both wild-type JAK2 (IC₅₀=23 nM) and JAK2^V617F mutant (IC₅₀=19 nM). Pacritinib hydrochloride also inhibits FLT3 (IC₅₀=22 nM) and its mutant FLT3^D835Y (IC₅₀=6 nM). Pacritinib hydrochloride can be used for the research of acute myeloid leukemia (AML) and myelofibrosis (MF).

HY-161259

JAK-IN-36	Inhibitor
JAK-IN-36 (Compound 12e) is a potent and selective inhibitor of Janus Kinase 1 (JAK1) with a IC₅₀ value of 2.2 nM. JAK-IN-36 can be used in the study of autoimmune diseases.

HY-19568B

Peficitinib hydrochloride	Inhibitor
Peficitinib (ASP015K) hydrochloride is an orally active JAK inhibitor, with IC₅₀s of 3.9, 5.0, 0.7 and 4.8 nM for JAK1, JAK2, JAK3 and Tyk2, respectively.

HY-154994

JAK-IN-30	Inhibitor
JAK-IN-30 (compound 31) is a water-soluble JAK inhibitor with IC₅₀ values of 2, 15, 18 and 2 nM for JAK2, JAK1, JAK3 and TYK2, respectively. JAK-IN-30 has research potential for dry eye disease (DED).

HY-W064657

Momelotinib dihydrochloride	Inhibitor
Momelotinib (dihydrochloride) is a JAK1/JAK2 inhibitor that also antagonizes ACVR1, leading to downregulation of Hepcidin expression and increased availability of iron for erythropoiesis. Momelotinib (dihydrochloride) can reduce transfusion burden and spleen enlargement caused by myelofibrosis, showing potential value in research and application within the field of myelofibrosis.

HY-139649

Ten01	Inhibitor
Ten01 has 5.0 nM activity against JAK1 kinase.

HY-143885

JAK1/TYK2-IN-3	Inhibitor
JAK1/TYK2-IN-3 is a potent, selective and orally active dual TYK2/JAK1 inhibitor with IC₅₀ values of 6 and 37 nM, respectively. JAK1/TYK2-IN-3 also shows selectively relative to JAK2 (IC₅₀=140 nM) and JAK3 (IC₅₀=362 nM). JAK1/TYK2-IN-3 shows anti-inflammatory effect by regulating the expression of related TYK2/JAK1-regulated genes, as well as the formation of Th1, Th2, and Th17 cells.

HY-108342

PF-00956980	Inhibitor
PF-00956980 is a reversible pan-JAK inhibitor with IC₅₀ values of 2.2, 23.1 and 59.9 μM for JAK1, JAK2 and JAK3, respectively. PF-00956980 can be used in the research of lung and skin inflammatory diseases.

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