2. Epigenetics Stem Cell/Wnt Protein Tyrosine Kinase/RTK JAK/STAT Signaling
  3. JAK STAT
  4. YYSW001

YYSW001 is a selective and orally acrive JAK1 inhibitor with an IC50 of 6 nM and a Kd of 32.32 μM. YYSW001 blocks JAK1-dependent phosphorylation of STAT6, as well as IL-6-induced phosphorylation of STAT3. YYSW001 suppresses pro-inflammatory cytokine levels, reduces paw swelling, lowers clinical arthritis scores, alleviates joint damage and decreases bone loss. YYSW001 is applicable for the research of rheumatoid arthritis.

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YYSW001

YYSW001 Chemical Structure

CAS No. : 2763672-36-0

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YYSW001 Related Antibodies

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JAK1 JAK2 JAK3 Tyk2 JAK

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STAT3 STAT5 STAT6 STAT1

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Description

YYSW001 is a selective and orally acrive JAK1 inhibitor with an IC50 of 6 nM and a Kd of 32.32 μM. YYSW001 blocks JAK1-dependent phosphorylation of STAT6, as well as IL-6-induced phosphorylation of STAT3. YYSW001 suppresses pro-inflammatory cytokine levels, reduces paw swelling, lowers clinical arthritis scores, alleviates joint damage and decreases bone loss. YYSW001 is applicable for the research of rheumatoid arthritis[1].

IC50 & Target[1]

JAK1

 

STAT3

 

STAT6

 

In Vitro

YYSW001 (2 h) potently inhibits the JAK1-dependent STAT6 pathway in THP-1 cells (IC50 = 0.041 μM), while only exerting weak inhibitory activity against the JAK2-dependent STAT5 pathway in TF-1 cells (IC50 = 5.530 μM)[1].
YYSW001 (72 h) potently inhibits the proliferation of Ba/F3-TEL-JAK1 cells (IC50 = 290.2 nM), while exhibits extremely low activity against Ba/F3-TEL-JAK2, Ba/F3-TEL-JAK3 and Ba/F3-TEL-TYK2 cells[1].
YYSW001 (15 min) inhibits IL-6-induced JAK1-dependent STAT3 phosphorylation in human whole blood cells (IC50 = 7065.0 nM in CD3+ T cells, 3001.0 nM in CD14+ monocytes), and shows extremely weak inhibitory activity against GM-CSF-induced JAK2-dependent STAT5 phosphorylation[1].
YYSW001 exhibits favorable in vitro ADME properties, including excellent liver microsomal stability and plasma stability, extremely low inhibitory activity against CYP3A4 and hERG, moderate permeability, and moderate plasma protein binding rate[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

YYSW001 Related Antibodies

Cell Viability Assay[1]

Cell Line: Ba/F3-engineered cell lines (Ba/F3-TEL-JAK1, Ba/F3-TEL-JAK2, Ba/F3-TEL-JAK3, Ba/F3-TEL-TYK2)
Concentration: serial 2- or 3-fold dilutions (nine gradients)
Incubation Time: 72 h
Result: Exhibited potent inhibitory activity against Ba/F3-TEL-JAK1 cells with an IC50 of 290.2 nM.
Showed negligible inhibition against Ba/F3-TEL-JAK2, Ba/F3-TEL-JAK3, and Ba/F3-TEL-TYK2 cells (IC50 > 10000.0 nM for all three cell lines).
Achieved a cellular JAK1/JAK2 selectivity ratio of 38.6.
Parmacokinetics
Species Dose Route AUC0-t AUC0-∞ Cmax Tmax T1/2 MRT0-∞ V CL F Vd
Rat[1] 3 mg/kg i.v. 3831.25 h·μg/L 4051.12 h·μg/L / / 2.8 h 3.7 h / 0.7 L/h/kg / 3.1 L/kg
Rat[1] 3 mg/kg p.o. 2277.65 h·μg/L 2503.58 h·μg/L 328.61 μg/L 3.0 h 2.8 h 5..8 h 5.0 L/kg 1.2 L/h/kg 61.8 % /
Rat[1] 10 mg/kg p.o. 8543.24 h·μg/L 8861.88 h·μg/L 1323.53 μg/L 3.2 h 2.2 h 5.0 h 3.6 L/kg 1.1 L/h/kg 65.6 % /
Rat[1] 30 mg/kg p.o. 25905.37 h·μg/L 26291.77 h·μg/L 3300.77 μg/L 2.9 h 2.5 h 6.6 h 3.3 L/kg 0.9 L/h/kg 64.9 % /
In Vivo

YYSW001 (3-10 mg/kg; p.o.; twice daily; 14 days) exhibits dose-dependent therapeutic effects in a rat collagen-induced arthritis model[1].
YYSW001 (1-30 mg/kg; p.o.; twice daily; 14 days) exhibits a clear dose-dependent anti-arthritic effect in a rat adjuvant-induced arthritis model[1].
YYSW001 (100-200 mg/kg; p.o.; once daily; 7 days) shows no significant safety concerns in rats[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Sprague-Dawley (SD) rats (collagen-induced arthritis model)[1]
Dosage: 3 mg/kg; 10 mg/kg
Administration: i.g.; twice daily; 14 days
Result: Reversed disease-induced body weight loss.
Significantly reduced hind paw swelling
Decreased clinical arthritis scores.
Suppressed serum levels of pro-inflammatory cytokines IL-6, IL-1β, and TNF-α to near-normal levels.
Substantially preserved joint architecture and reduced bone loss compared to the vehicle group.
Molecular Weight

417.38

Formula

C18H20F5N5O
CAS No.
SMILES

O[C@@H](C1=NC2=CN=C3NC=CC3=C2N1[C@@H]4CN(CC4)CCC(C(F)(F)F)(F)F)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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YYSW001 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

YYSW0012763672-36-0YYSW 001YYSW-001JAKSTATJanus kinaseIL-6STAT3rheumatoid arthritisSTAT6TF-1 cellsratsJAK1Ba/F3-TEL-JAK1 cellsCYP3A4THP-1 cellsInhibitorinhibitorinhibit

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