Search Result

Isoforms Recommended:	JAK1

Results for "

JAK1

" in MCE Product Catalog:

By Targets:	Apoptosis (15) Autophagy (6) Bacterial (2) Btk (1) Drug Metabolite (1) Endogenous Metabolite (1) FLT3 (4) Fungal (2) GSK-3 (1) HBV (1) HCV (1) IFNAR (3) Influenza Virus (2) Interleukin Related (2) JAK (92) Mitophagy (2) NF-κB (1) PERK (2) PKC (1) Polo-like Kinase (PLK) (1) RAR/RXR (1) STAT (5) STING (1) Syk (5)
By Research Areas:	Cancer (53) Infection (3) Inflammation/Immunology (49) Neurological Disease (1)

Inhibitors & Agonists

Screening Libraries

Recombinant Proteins

Isotope-Labeled Compounds

Antibodies

Cat. No.	Product Name	Target	Research Areas

HY-144440

JAK1-IN-9
JAK Cancer

JAK1-IN-9 (compound 23a) is a potent and selective JAK1 inhibitor with an IC₅₀ of 72 nM. JAK1-IN-9 shows selective against other JAKs by 12 times or more.

JAK1-IN-9	JAK	Cancer
JAK1-IN-9 (compound 23a) is a potent and selective *JAK1* inhibitor with an IC₅₀ of 72 nM. JAK1-IN-9 shows selective against other JAKs by 12 times or more.

HY-116505

JAK1-IN-4	JAK	Cancer
JAK1-IN-4 is a potent and selective *JAK1* inhibitor, with IC₅₀s of 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).

HY-139423

JAK1-IN-8
JAK Cancer Inflammation/Immunology

JAK1-IN-8, a potent JAK1 inhibitor (IC₅₀<500 nM), compound 28, extracted from patent WO2016119700A1.
HY-145336

JAK1/TYK2-IN-1
JAK Cancer

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

JAK1-IN-8	JAK	Cancer Inflammation/Immunology
JAK1-IN-8, a potent *JAK1* inhibitor (IC₅₀<500 nM), compound 28, extracted from patent WO2016119700A1.

JAK1/TYK2-IN-1	JAK	Cancer
JAK1/TYK2-IN-1 is a dual inhibitor of TYK2 and *JAK1* (IC₅₀ = 29 and 41 nM respectively).

HY-143885

JAK1/TYK2-IN-3	JAK	Inflammation/Immunology
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-126294

AZD4604 JAK1-IN-7	JAK	Inflammation/Immunology
AZD4604 (JAK1-IN-7) is a Janus-associated kinase 1 (JAK1) inhibitor extracted from patent WO2018134213A1, Example 63, has an anti-inflammatory effect.

HY-139837

GDC-4379
JAK Inflammation/Immunology

GDC-4379 is a JAK1 inhibitor that can be used for the research of asthma.

GDC-4379	JAK	Inflammation/Immunology
GDC-4379 is a *JAK1* inhibitor that can be used for the research of asthma.

HY-152080

TUL01101	JAK	Inflammation/Immunology
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-112724

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

HY-19569

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

HY-145588A

Povorcitinib phosphate INCB54707 phosphate	JAK	Inflammation/Immunology
Povorcitinib phosphate is a potent and selective inhibitor of *JAK1. Povorcitinib phosphate has the potential for the research of disease selected from cutaneous lupus erythematosus (CLE) and Lichen planus (LP).*

HY-16997

Itacitinib INCB039110	JAK	Cancer
Itacitinib (INCB039110) is an orally active and selective inhibitor of *JAK1* with an IC₅₀ of 2 nM for human JAK1. Itacitinib shows >20-fold selectivity for JAK1 over JAK2 and >100-fold over JAK3 and TYK2; Itacitinib is used in the research of myelofibrosis.

HY-18300

Filgotinib GLPG0634	JAK	Cancer
Filgotinib (GLPG0634) is a selective and orally active *JAK1* inhibitor with IC₅₀ of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, and TYK2, respectively.

HY-145588

Povorcitinib INCB54707	JAK	Inflammation/Immunology
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) (extracted from patent WO2021076124A1).*

HY-19631B

Ilginatinib hydrochloride NS-018 hydrochloride	JAK	Cancer
Ilginatinib hydrochloride (NS-018 hydrochloride) is a highly active and orally bioavailable *JAK2* inhibitor, with an IC₅₀ of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC₅₀, 33 nM), JAK3 (IC₅₀, 39 nM), and Tyk2 (IC₅₀, 22 nM).

HY-108342

PF-00956980	JAK	Inflammation/Immunology
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.

HY-19631A

Ilginatinib NS-018	JAK	Cancer
Ilginatinib (NS-018) is a highly active and orally bioavailable *JAK2* inhibitor, with an IC₅₀ of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC₅₀, 33 nM), JAK3 (IC₅₀, 39 nM), and Tyk2 (IC₅₀, 22 nM).

HY-19631

Ilginatinib maleate NS-018 maleate	JAK	Cancer
Ilginatinib maleate (NS-018 maleate) is a highly active and orally bioavailable *JAK2* inhibitor, with an IC₅₀ of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC₅₀, 33 nM), JAK3 (IC₅₀, 39 nM), and Tyk2 (IC₅₀, 22 nM).

HY-18300S

Filgotinib-d4 GLPG0634-d₄	JAK	Cancer
Filgotinib-d₄ is the deuterium labeled Filgotinib. Filgotinib (GLPG0634) is a selective JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, and TYK2, respectively.

HY-120469

2,6-Dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)benzamide	JAK	Inflammation/Immunology
GDC-046 is a potent, selective, and orally bioavailable TYK2 inhibitor with K_is of 4.8, 0.7, 0.7, and 0.4 nM for TYK2, JAK1, JAK2, and JAK3, respectively.

HY-13827

JAK-IN-1
JAK Inflammation/Immunology

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

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

HY-151385

VVD-118313	JAK STAT IFNAR Interleukin Related	Cancer
VVD-118313 (compound 5a) is a potent, selective *JAK1* inhibitor. VVD-118313 targets an isoform-restricted allosteric cysteine to block JAK1-dependent trans-phosphorylation and cytokine signaling. VVD-118313 can be used for research of cancer.

HY-151385A

(R,R)-VVD-118313	STAT Interleukin Related IFNAR JAK	Cancer
(R,R)-VVD-118313 is the isomer of VVD-118313 (HY-151385). VVD-118313 is a selective *JAK1* inhibitor and blocks JAK1-dependent trans-phosphorylation and cytokine signaling. VVD-118313 can be used for research of cancer.

HY-112442

AZ-3
JAK Cancer

AZ-3 is a potent and selective JAK1 inhibitor with an IC₅₀ of 34 nM.
HY-139649

Ten01
JAK Others

Ten01 has 5.0 nM activity against JAK1 kinase.

AZ-3	JAK	Cancer
AZ-3 is a potent and selective *JAK1* inhibitor with an IC₅₀ of 34 nM.

Ten01	JAK	Others
Ten01 has 5.0 nM activity against *JAK1* kinase.

HY-139807

JAK-IN-14	JAK	Inflammation/Immunology
JAK-IN-14 is a potent and selective *JAK1* inhibitor, with an IC₅₀ of <5 μM. JAK-IN-14 is >8-fold more selective for JAK1 than JAK2 and JAK3 (Patent WO2016119700A1, compound 16).

HY-18300A

Filgotinib maleate GLPG0634 maleate	JAK	Inflammation/Immunology
Filgotinib (maleate) is a selective and orally active *JAK1* inhibitor with IC₅₀ of 10 nM, 28 nM, 810 nM and 116 nM for JAK1, JAK2, JAK3 and TYK2, respectively. Filgotinib (maleate) can be used for rheumatoid arthritis (RA) and Crohn's disease research.

HY-50859

Ruxolitinib sulfate INCB018424 sulfate	JAK Autophagy	Cancer
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-14722C

NVP-BSK805 trihydrochloride	JAK	Cancer
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-14722A

NVP-BSK805 dihydrochloride	JAK	Cancer
NVP-BSK805 dihydrochloride 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-14722

NVP-BSK805	JAK	Cancer
NVP-BSK805 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-15315A

Baricitinib phosphate LY3009104 phosphate; INCB028050 phosphate	JAK	Inflammation/Immunology
Baricitinib phosphate (LY3009104 phosphate; INCB028050 phosphate) is a selective orally bioavailable *JAK1/JAK2* inhibitor with IC₅₀ of 5.9 nM and 5.7 nM, respectively.

HY-50856

Ruxolitinib INCB18424	JAK Autophagy Mitophagy Apoptosis	Cancer
Ruxolitinib (INCB18424) is a potent and selective *JAK1/2* inhibitor with IC₅₀s of 3.3 nM and 2.8 nM in cell-free assays, and has 130-fold selectivity for JAK1/2 over JAK3. Ruxolitinib induces autophagy and kills tumor cells through toxic mitophagy.

HY-10963

Momelotinib Mesylate CYT387 Mesylate	JAK Autophagy	Cancer
Momelotinib Mesylate (CYT387 Mesylate) is an ATP-competitive inhibitor of *JAK1/JAK2* with IC₅₀ of 11 nM/18 nM, appr 10-fold selectivity versus JAK3.

HY-16997A

Itacitinib adipate	JAK	Cancer
Itacitinib adipate is an orally bioavailable and selective *JAK1* inhibitor which has been tested for efficacy and safety in a phase II trial in myelofibrosis.

HY-107429

Abrocitinib PF-04965842	JAK	Inflammation/Immunology
Abrocitinib (PF-04965842) is a potent, orally active and selective *JAK1* inhibitor, with IC₅₀s of 29 and 803 nM for JAK1 and JAK2, respectively. Abrocitinib (PF-04965842) exhibits less active effect on TYK2 (IC₅₀, 1.253 μM), and inhibits phosphorylation of STAT1, STAT3 and STAT5 after stimulation. Effective in autoimmune disease.

HY-10961

Momelotinib CYT387	JAK Autophagy Apoptosis	Cancer
Momelotinib (CYT387) is an ATP-competitive inhibitor of *JAK1/JAK2* with IC₅₀a of 11 nM and 18 nM,respectively. CYT387 shows much less activity against JAK3.

HY-19569A

Upadacitinib tartrate tetrahydrate ABT-494 tartrate tetrahydrate	JAK	Inflammation/Immunology
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-13577A

Oclacitinib maleate PF-03394197 maleate	JAK	Inflammation/Immunology
Oclacitinib maleate (PF-03394197 maleate) is a novel *JAK* inhibitor. Oclacitinib maleate (PF-03394197 maleate) is most potent at inhibiting *JAK1* (IC₅₀=10 nM).

HY-13961

GLPG0634 analog
JAK Cancer

GLPG0634 analog (Compoun 176) is a broad spectrum JAK inhibitor with IC₅₀ values of <100 nM against JAK1, JAK2 and JAK3.

GLPG0634 analog	JAK	Cancer
GLPG0634 analog (Compoun 176) is a broad spectrum *JAK* inhibitor with IC₅₀ values of <100 nM against JAK1, JAK2 and JAK3.

HY-15315

Baricitinib LY3009104; INCB028050	JAK	Inflammation/Immunology
Baricitinib (LY3009104; INCB028050) is a selective and orally bioavailable *JAK1* and *JAK2* inhibitor with IC₅₀s of 5.9 nM and 5.7 nM, respectively.

HY-100895

SAR-20347
JAK Cancer

SAR-20347 is an inhibitor of TYK2, JAK1, JAK2 and JAK3 with IC₅₀s of 0.6, 23, 26 and 41 nM, respectively.
HY-15312

WP1066
STAT JAK Apoptosis Cancer

WP1066 is an inhibitor of JAK2 and STAT3, and also shows effect on STAT5 and ERK1/2, without affecting JAK1 and JAK3.

SAR-20347	JAK	Cancer
SAR-20347 is an inhibitor of TYK2, *JAK1, JAK2* and *JAK3* with IC₅₀s of 0.6, 23, 26 and 41 nM, respectively.

WP1066	STAT JAK Apoptosis	Cancer
WP1066 is an inhibitor of *JAK2* and STAT3, and also shows effect on STAT5 and ERK1/2, without affecting JAK1 and JAK3.

HY-12469

Decernotinib VX-509; VRT-831509	JAK	Inflammation/Immunology
Decernotinib is a potent, orally active *JAK3* inhibitor, with K_is of 2.5, 11, 13 and 11 nM for *JAK3, JAK1, JAK*2, and TYK2, respectively.

HY-10193

AZD-1480
JAK Cancer

AZD-1480 is an ATP-competitive inhibitor of JAK1 and JAK2 with IC₅₀s of 1.3 nM and <0.4 nM, respectively.

AZD-1480	JAK	Cancer
AZD-1480 is an ATP-competitive inhibitor of *JAK1* and *JAK2* with IC₅₀s of 1.3 nM and <0.4 nM, respectively.

HY-10962

Momelotinib sulfate CYT387 sulfate salt	JAK Autophagy Apoptosis	Cancer
Momelotinib sulfate (CYT387 sulfate salt) is an ATP-competitive inhibitor of *JAK1/JAK2* with IC₅₀ of 11 nM/18 nM, 10-fold selectivity versus JAK3 (IC₅₀=155 nM).

HY-50856S

Deuruxolitinib CTP-543; Ruxolitinib d₈; Deuterated Ruxolitinib	JAK	Inflammation/Immunology
Deuruxolitinib, a deuterated Ruxolitinib (HY-50856), modulates the activity of *JAK1/JAK2. Deuruxolitinib can be used for the research hair loss disorders (from patent WO2017192905A1, compound I).*

HY-40354A

Tofacitinib citrate Tasocitinib citrate; CP-690550 citrate	JAK Apoptosis Bacterial Fungal Influenza Virus	Cancer Infection Inflammation/Immunology
Tofacitinib citrate is an orally available *JAK1/2/3* inhibitor with IC₅₀s of 1, 20, and 112 nM, respectively. Tofacitinib citrate has antibacterial, antifungal and antiviral activities.

HY-111750

JAK-IN-3
JAK Inflammation/Immunology

JAK-IN-3 (compound 22) is a potent JAK inhibitor, with IC₅₀ values of 3 nM, 5 nM, 34 nM and 70 nM for JAK3, JAK1, TYK2 and JAK2, respectively.
HY-15270

BMS-911543
JAK Cancer

BMS-911543 is a selective JAK2 inhibitor, with IC₅₀s of 1.1 nM, less selective at JAK1, JAK3 and TYK2 (IC₅₀, 75, 360, 66 nM, respectively).
HY-109053

Delgocitinib
JTE-052
JAK Inflammation/Immunology

Delgocitinib (JTE-052) is a specific JAK inhibitor with IC₅₀s of 2.8, 2.6, 13 and 58 nM for JAK1, JAK2, JAK3 and Tyk2, respectively.

HY-15315S1

Baricitinib-d3 LY3009104-d₃; INCB028050-d₃	JAK	Inflammation/Immunology
Baricitinib-d₃ is the deuterium labeled Baricitinib. Baricitinib (LY3009104; INCB028050) is a selective and orally bioavailable JAK1 and JAK2 inhibitor with IC50s of 5.9 nM and 5.7 nM, respectively.

HY-15315S

Baricitinib-d5 LY3009104-d₅; INCB028050-d₅	JAK	Inflammation/Immunology
Baricitinib-d₅ is the deuterium labeled Baricitinib. Baricitinib (LY3009104; INCB028050) is a selective and orally bioavailable JAK1 and JAK2 inhibitor with IC50s of 5.9 nM and 5.7 nM, respectively.

HY-50858

Ruxolitinib phosphate INCB018424 phosphate	JAK Autophagy Mitophagy	Cancer
Ruxolitinib phosphate (INCB018424 phosphate) is a potent *JAK1/2* inhibitor with IC₅₀s of 3.3 nM/2.8 nM, respectively, showing more than 130-fold selectivity over JAK3.

HY-19568B

Peficitinib hydrochloride ASP015K hydrochloride; JNJ-54781532 hydrochloride	JAK	Inflammation/Immunology
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-19568

Peficitinib ASP015K; JNJ-54781532	JAK	Inflammation/Immunology
Peficitinib (ASP015K) 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-W394903

GS-829845	JAK Drug Metabolite	Cancer
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-15999

Cerdulatinib PRT062070; PRT2070	JAK Syk	Cancer
Cerdulatinib (PRT062070) is a selective Tyk2 inhibitor with an IC₅₀ of 0.5 nM. Cerdulatinib (PRT062070) also is a dual *JAK* and SYK inhibitor with IC₅₀s of 12, 6, 8 and 32 for JAK1, 2, 3 and SYK, respectively.

HY-19568A

Peficitinib hydrobromide ASP015K hydrobromide; JNJ-54781532 hydrobromide	JAK	Inflammation/Immunology
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-107361

Golidocitinib AZD4205	JAK	Cancer
Golidocitinib (AZD4205) is a selective *JAK1* inhibitor, with an IC₅₀ of 73 nM, weakly inhibits JAK2 (IC₅₀>14.7 μM), and shows little inhibition on JAK3 (IC₅₀>30 μM).

HY-101024

PF-06263276	JAK	Inflammation/Immunology
PF-06263276 (PF 6263276) is a potent and selective *pan-JAK* inhibitor, with IC₅₀s of 2.2 nM, 23.1 nM, 59.9 nM and 29.7 nM for JAK1, JAK2, JAK3 and TYK2, respectively.

HY-40354AS

Tofacitinib-d3 citrate Tasocitinib-d₃ (citrate); CP-690550-d₃ (citrate)	JAK Apoptosis Bacterial Fungal Influenza Virus	Cancer Infection Inflammation/Immunology
Tofacitinib-d₃ (citrate) is deuterium labeled Tofacitinib (citrate). Tofacitinib citrate is an orally available JAK1/2/3 inhibitor with IC50s of 1, 20, and 112 nM, respectively. Tofacitinib citrate has antibacterial, antifungal and antiviral activities.

HY-148060

JAK-IN-21
JAK Cancer

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-16755

Solcitinib GSK-2586184; GLPG-0778	JAK	Inflammation/Immunology
Solcitinib is an orally active, competitive, potent, selective *JAK1* inhibitor, with an IC₅₀ of 9.8 nM, and 11-, 55- and 23-fold selectivity over JAK2, JAK3 and TYK2, respectively; Solcitinib is used in the research of moderate-to-severe plaque-type psoriasis.

HY-144032

Tyk2-IN-9	JAK	Inflammation/Immunology
Tyk2-IN-9 (Compound 26) is a selective Tyk-2 inhibitor with IC₅₀s of 0.076 and 1.8 nM for TYK2-JH2 and JAK1-JH2, respectively. Tyk2-IN-9 can be used for the research of inflammatory or autoimmune disease.

HY-143444

JAK-IN-20	JAK	Inflammation/Immunology
JAK-IN-20 is a potent, pan and orally active *JAK* inhibitor with an IC₅₀s of 7 nM, 5 nM, 14 nM for JAK1, JAK2, JAK3, respectively. JAK-IN-20 shows excellent pharmacokinetics and displays anti-inflammatory efficacy in vivo.

HY-144087

TYK2-IN-11	JAK	Inflammation/Immunology
TYK2-IN-11 (Compound 5B) is a selective Tyk-2 inhibitor with IC₅₀s of 0.016 and 0.31 nM for TYK2-JH2 and JAK1-JH2, respectively. TYK2-IN-11 can be used for the research of inflammatory or autoimmune disease.

HY-144031S

Tyk2-IN-8	JAK	Inflammation/Immunology
Tyk2-IN-8 is a selective Tyk-2 inhibitor with an IC50 of 5.7 nM for TYK2-JH2. Tyk2-IN-8 inhibits JAK1-JH1 with IC50 of 3.0 nM. Tyk2-IN-8 can be used for the research of autoimmune disease[1].

HY-102046

FM-381	JAK	Inflammation/Immunology
FM-381 is a potent covalent reversible inhibitor of *JAK3* targeting the unique Cys909. FM-381 has an IC₅₀ of 127 pM for JAK3, with 410, 2700 and 3600-fold selectivity over JAK1, JAK2 and TYK2, respectively.

HY-14435

Pyridone 6	JAK	Cancer
Pyridone 6 is a *pan-JAK* inhibitor, which potently inhibits the JAK kinase family, with IC₅₀s of 1 nM for *JAK2* and TYK2, 5 nM for *JAK3, and 15 nM for JAK1*, while displaying significantly weaker affinities (130 nM to >10 mM) for other protein tyrosine kinases.

HY-112708

Brepocitinib PF-06700841	JAK	Inflammation/Immunology
Brepocitinib (PF-06700841) is a potent dual Janus kinase 1 (JAK1) and TYK2 inhibitor with IC₅₀s of 17 nM and 23 nM, respectively. Brepocitinib also inhibits *JAK2* and *JAK3* with IC₅₀s of 77 nM and 6.49 μM, respectively.

HY-147975

JAK3-IN-12	JAK	Inflammation/Immunology
JAK3-IN-12 (compound 5k) is a highly potent *JAK3* inhibitor with IC₅₀ values of 9.5 nM, 18 nM and 42 nM for JAK3, JAK1 and JAK2, respectively. JAK3-IN-12 can be used for researching rheumatoid arthritis.

HY-112708A

Brepocitinib P-Tosylate PF-06700841 P-Tosylate	JAK	Inflammation/Immunology
Brepocitinib (PF-06700841) P-Tosylate is a potent dual Janus kinase 1 (JAK1) and TYK2 inhibitor with IC₅₀s of 17 nM and 23 nM, respectively. Brepocitinib P-Tosylate also inhibits *JAK2* and *JAK3* with IC₅₀s of 77 nM and 6.49 μM, respectively.

HY-19544

JAK3-IN-1	JAK	Cancer
JAK3-IN-1 is a potent, selective and orally active *JAK3* inhibitor with an IC₅₀ of 4.8 nM. JAK3-IN-1 shows over 180-fold more selective for *JAK3* than JAK1 (IC₅₀ of 896 nM) and JAK2 (IC₅₀ of 1050 nM).

HY-18009

(Z)-LFM-A13	Btk Polo-like Kinase (PLK) JAK	Cancer
LFM-A13 is a potent BTK, *JAK2, PLK* inhibitor, inhibits recombinant BTK, Plx1 and PLK3 with IC₅₀s of 2.5 μM, 10 μM and 61 μM; LFM-A13 shows no effects on JAK1 and JAK3, Src family kinase HCK, EGFR and IRK.

HY-15999A

Cerdulatinib hydrochloride PRT062070 hydrochloride; PRT2070 hydrochloride	Syk JAK	Cancer
Cerdulatinib hydrochloride (PRT062070) is a selective, oral active and reversible ATP-competitive inhibitor of dual SYK and *JAK, with IC₅₀s of 32 nM, 0.5 nM, 12 nM, 6 nM and 8 nM for SYK* and Tyk2, *JAK1, 2, 3, respectively. Cerdulatinib hydrochloride could be used to research autoimmune disease and B-cell malignancies.*

HY-15508

JANEX-1 WHI-P131; JAK3 inhibitor I	JAK	Cancer
JANEX-1 (WHI-P131) is a potent and specific *JAK3* inhibitor (estimated K_i=2.3 μM). JANEX-1 (WHI-P131) shows potent JAK3-inhibitory activity (IC₅₀ of 78 μM), does not inhibit JAK1 and JAK2.

HY-137756

JAK2-IN-6	JAK	Cancer
JAK2-IN-6, a multiple-substituted aminothiazole derivative, is a potent and selective *JAK2* inhibitor with an IC₅₀ of 22.86 μg/mL. JAK2-IN-6 shows no activity against JAK1 and JAK3. JAK2-IN-6 has anti-proliferative effect against cancer cells.

HY-108264

TCS 21311 NIBR3049	JAK PKC GSK-3	Cancer
TCS 21311 (NIBR3049) is a potent, highly selective *JAK3* inhibitor with an IC₅₀ of 8 nM, it displays >100-fold selectivity over JAK1, JAK2 and TYK2. TCS 21311 (NIBR3049) inhibits PKCα, PKCθ, and GSK3β with IC₅₀s of 13, 68, and 3 nM, respectively.

HY-130247

JAK2/FLT3-IN-1	JAK FLT3 Apoptosis	Cancer
JAK2/FLT3-IN-1 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. JAK2/FLT3-IN-1 has anti-cancer activity.

HY-103018

Gusacitinib ASN-002	JAK Syk	Cancer Inflammation/Immunology
Gusacitinib (ASN-002) is an orally active dual *SYK/JAK* kinase inhibitor with IC₅₀ values of 5, 46, 4, 11 and 8 nM for SYK, *JAK1, JAK2, JAK3* and TYK2, respectively. Gusacitinib rapidly and significantly suppressed key inflammatory pathways implicated in atopic dermatitis pathogenesis. Gusacitinib can be used in the research of chronic hand eczema and cancers such as basal cell carcinoma.

HY-10409

Fedratinib TG-101348; SAR 302503	JAK Apoptosis	Cancer
Fedratinib (TG-101348) is a potent, selective, ATP-competitive and orally active *JAK2* inhibitor with IC₅₀s of 3 nM for both *JAK2* and JAK2V617F kinase. Fedratinib shows 35- and 334-fold selectivity over JAK1 and JAK3, respectively. Fedratinib induces cancer cell apoptosis and has the potential for myeloproliferative disorders research.

HY-10409A

Fedratinib hydrochloride hydrate TG-101348 hydrochloride hydrate; SAR 302503 hydrochloride hydrate	JAK Apoptosis	Cancer
Fedratinib hydrochloride hydrate (TG-101348 hydrochloride hydrate) is a potent, selective, ATP-competitive and orally active *JAK2* inhibitor with IC₅₀s of 3 nM for both *JAK2* and JAK2V617F kinase. Fedratinib hydrochloride hydrate shows 35- and 334-fold selectivity over JAK1 and JAK3, respectively. Fedratinib hydrochloride hydrate induces cancer cell apoptosis and has the potential for myeloproliferative disorders research.

HY-130247A

JAK2/FLT3-IN-1 TFA	JAK FLT3 Apoptosis	Cancer
JAK2/FLT3-IN-1 (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. JAK2/FLT3-IN-1 (TFA) has anti-cancer activity.

HY-131014

FM-479	JAK	Inflammation/Immunology
FM-479 is the negative control of FM-381 (HY-102046) and has no activity on JAK3 or other kinases. FM-381 is a potent covalent reversible inhibitor of JAK3* targeting* the unique Cys909. FM-381 has an IC₅₀ of 127 pM for JAK3, with 410, 2700 and 3600-fold selectivity over JAK1, JAK2 and TYK2, respectively.

HY-126242S

Tyk2-IN-7	JAK	Inflammation/Immunology
Tyk2-IN-7 is a TYK2 JH2 inhibitor, binds to TYK2 JH2 domain with IC50 and Ki.app of 0.00053 μM and 0.00007 μM, respectively. Tyk2-IN-7 provides a highly selective alternative to conventional TYK2 orthosteric inhibitors, inhibits TYK2/JAK1/JAK2 kinase domain. Tyk2-IN-7 provides robust inhibition in a mouse IL-12-induced IFNγ pharmacodynamic model as well as efficacy in an IL-23 and IL-12-dependent mouse colitis model[1].

HY-131906

JAK2-IN-7	JAK FLT3 Apoptosis	Cancer
JAK2-IN-7 is a selective *JAK2* inhibitor with IC₅₀s of 3, 11.7, and 41 nM for JAK2, SET-2, and Ba/F3^V617F cells, respectively. JAK2-IN-7 possesses >14-fold selectivity over JAK1, JAK3, FLT3. JAK2-IN-7 stimulates cell cycle arrest in the G0/G1 phase and induces tumor cellapoptosis. Antitumor activities.

HY-145015

Tuspetinib HM43239	FLT3 Apoptosis	Cancer
Tuspetinib (HM43239) is an orally active and selective FLT3 inhibitor with IC₅₀s of 1.1 nM, 1.8 nM and 1.0 nM for FLT3 WT, FLT3 internal tandem duplication (ITD) and FLT3 D835Y kinases, respectively. Tuspetinib inhibits the kinase activity of FLT3 as a reversible type I inhibitor and modulates p-STAT5, p-ERK, SYK, JAK1/2, and TAK1. Tuspetinib inhibits the proliferation and induces the apoptosis of leukemic cells.

HY-13775

XL019	JAK Apoptosis	Cancer
XL019 is a potent, orally active, and selective *JAK2* inhibitor, with IC₅₀s of 2.2, 134.3, and 214.2 nM for JAK2, JAK1 and JAK3, respectively. XL019 shows 50-fold or greater selectivity for JAK2, versus a panel of over 100 serine/threonine and tyrosine kinases, including other members of the JAK family. XL019 potently inhibits STAT3 and STAT5 phosphorylation in cells harboring either JAK2V617F or wild-type JAK2.

HY-151262

JAK-IN-23	JAK STING NF-κB STAT	Inflammation/Immunology
JAK-IN-23 is an orally active double inhibitor of JAK/STAT and NF-κB. JAK-IN-23 can inhibit JAK1/2/3 with IC₅₀ values of 8.9 nM, 15 nM and 46.2 nM, respectively. JAK-IN-23 has potent inhibitory activities against interferon-stimulated genes (ISG) and NF-κB pathways with IC₅₀ values of 3.3 nM and 150.7 nM, respectively. JAK-IN-23 has great anti-inflammatory that decreases the release of various proinflammatory factors. JAK-IN-23 can be used for the research of inflammatory bowel disease (IBD).

HY-119935

JAK3 covalent inhibitor-1	JAK	Inflammation/Immunology
JAK3 covalent inhibitor-1 is a potent and selective janus kinase 3 (JAK3) covalent inhibitor with an IC₅₀ of 11 nM and shows 246-fold selectivity vs other JAKs.

HY-111745

Tyk2-IN-5	JAK	Inflammation/Immunology
Tyk2-IN-5 (compound 6) is a potent, selective and orally active tyrosine kinase 2 (Tyk2) inhibitor that acts on the JH2 structural domain. Tyk2-IN-5 shows a K_i value of 0.086 nM for Tyk2 JH2 and an IC₅₀ value of 25 nM for IFNα. Tyk2-IN-5 efficiently inhibits the production of IFNγ in a pharmacodynamic rat model and is fully efficacious in a rat model of arthritis.

HY-W063968

RO8191 CDM-3008; RO4948191	IFNAR JAK STAT HCV HBV	Infection
RO8191 (CDM-3008), an imidazonaphthyridine compound, is an orally active and potent interferon (IFN) receptor agonist. RO8191 directly binds to IFNα/β receptor 2 (IFNAR2) and activates IFN-stimulated genes (ISGs) expression and *JAK/STAT* phosphorylation. RO8191 shows antiviral activity against both HCV and EMCV with an IC₅₀ of 200 nM for HCV replicon. RO8191 is a cccDNA modulator (CDM) through interferon-like activity and has anti-HBV activity.

HY-15128

9-cis-Retinoic acid Alitretinoin	RAR/RXR Apoptosis Endogenous Metabolite	Cancer Inflammation/Immunology Neurological Disease
9-cis-Retinoic acid (ALRT1057), a vitamin A derivative, is a potent RAR/RXR agonist. 9-cis-Retinoic acid induces apoptosis, regulates cell cycle and has anticancer, anti-inflammatory and neuroprotection activities.

HY-12736

GSK143	Syk PERK	Cancer Inflammation/Immunology
GSK143 is an orally active and highly selective spleen tyrosine kinase (SYK) inhibitor with a pIC₅₀ of 7.5. GSK143 inhibits phosphorylated Erk (pErk: *pIC₅₀*=7.1). GSK143 reduces inflammation and prevents recruitment of immune cells in the intestinal muscularis in mice.

HY-12736A

GSK143 dihydrochloride	Syk PERK	Cancer Inflammation/Immunology
GSK143 dihydrochloride is an orally active and highly selective spleen tyrosine kinase (SYK) inhibitor with a pIC₅₀ of 7.5. GSK143 dihydrochloride inhibits phosphorylated Erk (pErk: *pIC₅₀*=7.1). GSK143 dihydrochloride reduces inflammation and prevents recruitment of immune cells in the intestinal muscularis in mice.

Cat. No.	Product Name

HY-L008

JAK/STAT Compound Library

349 compounds

The Janus kinase (JAK)/signal transducer and activator of transcription (STAT) pathway is central to signaling by cytokine receptors, a superfamily of more than 30 transmembrane proteins that recognize specific cytokines, and is critical in blood formation and immune response. Canonical JAK/STAT signaling begins with the association of cytokines and their corresponding transmembrane receptors. Activated JAKs then phosphorylate latent STAT monomers, leading to dimerization, nuclear translocation, and DNA binding. In mammals, there are four JAKs (JAK1, JAK2, JAK3, TYK2) and seven STATs (STAT1, STAT2, STAT3, STAT4, STAT5a, STAT5b, STAT6). Since the JAK/STAT pathway plays a major role in many fundamental processes, such as apoptosis and inflammation, dysfunctional proteins in the pathway may lead to a number of diseases. For example, alterations in JAK/STAT signalling can result in cancer and diseases affecting the immune system, such as severe combined immunodeficiency disorder (SCID).

MCE provides 349 compounds that can be used in the study of the JAK/STAT signaling pathway and related diseases.

Recombinant Proteins Recommended:

Janus Kinase 1 (JAK1)

Cat. No.	Product Name	Species	Source

HY-P700583

JAK1 Protein, Human (P. pastoris, His)
JAK1; JAK1A; JAK1B; Tyrosine-protein kinase JAK1; Janus kinase 1; JAK-1
Human P. pastoris

Cat. No.	Product Name

HY-18300S

Filgotinib-d4
Filgotinib-d₄ is the deuterium labeled Filgotinib. Filgotinib (GLPG0634) is a selective JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, and TYK2, respectively.

HY-50856S

Deuruxolitinib
Deuruxolitinib, a deuterated Ruxolitinib (HY-50856), modulates the activity of *JAK1/JAK2. Deuruxolitinib can be used for the research hair loss disorders (from patent WO2017192905A1, compound I).*

HY-15315S1

Baricitinib-d3
Baricitinib-d₃ is the deuterium labeled Baricitinib. Baricitinib (LY3009104; INCB028050) is a selective and orally bioavailable JAK1 and JAK2 inhibitor with IC50s of 5.9 nM and 5.7 nM, respectively.

HY-15315S

Baricitinib-d5
Baricitinib-d₅ is the deuterium labeled Baricitinib. Baricitinib (LY3009104; INCB028050) is a selective and orally bioavailable JAK1 and JAK2 inhibitor with IC50s of 5.9 nM and 5.7 nM, respectively.

HY-40354AS

Tofacitinib-d3 citrate
Tofacitinib-d₃ (citrate) is deuterium labeled Tofacitinib (citrate). Tofacitinib citrate is an orally available JAK1/2/3 inhibitor with IC50s of 1, 20, and 112 nM, respectively. Tofacitinib citrate has antibacterial, antifungal and antiviral activities.

HY-144031S

Tyk2-IN-8
Tyk2-IN-8 is a selective Tyk-2 inhibitor with an IC50 of 5.7 nM for TYK2-JH2. Tyk2-IN-8 inhibits JAK1-JH1 with IC50 of 3.0 nM. Tyk2-IN-8 can be used for the research of autoimmune disease[1].

HY-126242S

Tyk2-IN-7

Tyk2-IN-7 is a TYK2 JH2 inhibitor, binds to TYK2 JH2 domain with IC50 and Ki.app of 0.00053 μM and 0.00007 μM, respectively. Tyk2-IN-7 provides a highly selective alternative to conventional TYK2 orthosteric inhibitors, inhibits TYK2/JAK1/JAK2 kinase domain. Tyk2-IN-7 provides robust inhibition in a mouse IL-12-induced IFNγ pharmacodynamic model as well as efficacy in an IL-23 and IL-12-dependent mouse colitis model[1].

Cat. No.	Product Name	Application	Reactivity

HY-P80726

JAK1 (YP7012) Mouse mAb
JAK1; JAK1A; JAK1B; Tyrosine-protein kinase JAK1; Janus kinase 1; JAK-1
WB, ICC/IF, IP Human, Rat

Mouse Monoclonal Antibody to JAK1
HY-P80196

JAK1 Rabbit mAb
WB, IHC-P, FC Human, Mouse, Rat

Rabbit Monoclonal Antibody) to JAK1

HY-P80728

JNK Rabbit mAb AI849689; c Jun N terminal kinase 1; C-JUN kinase 1; c-Jun N-terminal kinase 1; EC 2.7.11.24; JAK 1A; JAK1A; JNK 1; JNK 46; JNK; JNK-46; JNK1A2; JNK21B1/2; MAP kinase 8; MAPK 8; MAPK8; Mitogen activated protein kinase 8; Mitogen-activated protein kinase 8	WB, IP	Human, Mouse, Rat, Hamster
Rabbit Monoclonal Antibody to JNK

HY-P80729

JNK1 (1A4) Mouse mAb AI849689; c Jun N terminal kinase 1; C-JUN kinase 1; c-Jun N-terminal kinase 1; EC 2.7.11.24; JAK 1A; JAK1A; JNK 1; JNK 46; JNK; JNK-46; JNK1A2; JNK21B1/2; MAP kinase 8; MAPK 8; MAPK8; Mitogen activated protein kinase 8; Mitogen-activated protein kinase 8	WB, ICC/IF	Human, Mouse, Rat
Mouse Monoclonal Antibody to JNK1

HY-P80831

Phospho-JNK1 (Thr183/Tyr185) Rabbit mAb AI849689; c Jun N terminal kinase 1; C-JUN kinase 1; c-Jun N-terminal kinase 1; EC 2.7.11.24; JAK 1A; JAK1A; JNK 1; JNK 46; JNK; JNK-46; JNK1A2; JNK21B1/2; MAP kinase 8; MAPK 8; MAPK8; Mitogen activated protein kinase 8; Mitogen-activated protein kinase 8	WB, IP	Human, Rat
Rabbit Monoclonal Antibody to JNK1 (Phospho Thr183/Tyr185)