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Chemical Structure| 919486-40-1 Chemical Structure| 919486-40-1

Structure of AS1517499
CAS No.: 919486-40-1

Chemical Structure| 919486-40-1

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AS-1517499 is a potent STAT6 inhibitor with IC50 of 21 nM.

4.5 *For Research Use Only !

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Product Details of AS1517499

CAS No. :919486-40-1
Formula : C20H20ClN5O2
M.W : 397.86
SMILES Code : O=C(C1=CN=C(NCCC2=CC=C(O)C(Cl)=C2)N=C1NCC3=CC=CC=C3)N
MDL No. :MFCD24038757
InChI Key :OZRMEKAUZBKTTC-UHFFFAOYSA-N
Pubchem ID :10340781

Safety of AS1517499

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Related Pathways of AS1517499

JAK-STAT

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Nthy-ori 3-1 cells 100 nM 30 minutes Inhibit STAT6 phosphorylation, reduce TEC hyperplasia PMC5260978
EPC2-hTERT cells 400 nmol/L 24 hours To evaluate the impact of STAT6 inhibition on the CD73+CD104+ population, AS1517499 was found to prevent cytokine-induced inhibition of CD73 expression PMC8957025
Bone marrow-derived macrophages (BMDMs) 100 nM 48 hours To verify whether BHB promotes M2 macrophage polarization through the STAT6 signaling pathway. Results showed that AS1517499 completely inhibited the enhancement effect of BHB on IL-4-induced M2 macrophage polarization. PMC9011974
Primary fibroblasts 3.387 nM to 200 μM 3 days To analyze the sensitivity of primary fibroblasts to p-STAT6 inhibition, results showed that KFs were more sensitive to AS1517499 PMC10070111
THP-1 cells 800 nM 48 hours To study the effect of AS1517499 on THP-1 cells, results showed that AS1517499 treatment downregulated the expression of p-STAT6 and TGF-β in M0 cells PMC10070111
Raw264.7 macrophages 100 nM 48 hours AS1517499 abolished the induction of PD-L2 expression by TGP in Raw264.7 macrophages, indicating that TGP exerts its effects on macrophage polarization and PD-L2 expression mainly through activating STAT6/PD-L2 signaling pathway. PMC8288191

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
BALB/C mice Ph+ ALL mouse model intraperitoneal injection 50 mg/kg Daily injection for the duration of the experiment Inhibition of p-STAT6 significantly suppressed leukemogenesis in the P190 mouse model PMC9887777
Mice Experimental autoimmune Graves' disease mouse model Intraperitoneal injection 10 mg/kg 5 times Alleviate Graves' disease symptoms, reduce TEC hyperplasia PMC5260978
Mice DSS-induced colitis model Intraperitoneal injection 10 mg/kg/d Once daily, total of four times To verify whether BHB alleviates colitis through the STAT6 signaling pathway. Results showed that AS1517499 completely inhibited the protective effect of BHB against DSS-induced colitis. PMC9011974
BALB/c nude mice Keloid implantation model Subcutaneous injection 5 mg/kg Injected on days 1, 3, 5, 7, and 9, lasting for 9 days To assess the effect of p-STAT6 inhibition on keloid progression, results showed that AS1517499 treatment significantly reduced the volume of implantations, inhibited the proliferation of KFs, and induced apoptosis PMC10070111
Mice Unilateral ureteral obstruction (UUO) model and folic acid nephropathy model Intraperitoneal injection 30 mg/kg/d Once daily for 3 weeks AS1517499 inhibits STAT6 activation, reduces myeloid fibroblast accumulation and activation, reduces M2 macrophage polarization, reduces ECM protein production, and attenuates the development of kidney fibrosis and dysfunction. PMC8426438

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.51mL

0.50mL

0.25mL

12.57mL

2.51mL

1.26mL

25.13mL

5.03mL

2.51mL

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