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Chemical Structure| 509093-47-4 Chemical Structure| 509093-47-4
Chemical Structure| 509093-47-4
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Product Details of IRAK-1-4 Inhibitor I

CAS No. :509093-47-4
Formula : C20H21N5O4
M.W : 395.41
SMILES Code : O=C(C1=CC=CC([N+]([O-])=O)=C1)NC2=NC3=CC=CC=C3N2CCN4CCOCC4
Synonyms :
IRAK-1/4 Inhibitor I; IRAK-1/4 Inhibitor
MDL No. :MFCD09752602
InChI Key :QTCFYQHZJIIHBS-UHFFFAOYSA-N
Pubchem ID :11983295

Safety of IRAK-1-4 Inhibitor I

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of IRAK-1-4 Inhibitor I

TLR

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description Reference
Malme-3M 2.5 μM 48 h Inhibition of IRAK-1,-4 signaling enhanced cell apoptosis, with more significant effects when combined with vinblastine PMC3677596
A375 2.5 μM 48 h Inhibition of IRAK-1,-4 signaling enhanced cell apoptosis, with more significant effects when combined with vinblastine PMC3677596
NCM460 cells 50 μM 2 h To evaluate the effect of IRAK1/4 inhibitor on DSS-induced IL-8 secretion. Results showed that IRAK1/4 inhibitor had no effect on DSS-induced IL-8 secretion. PMC2688460
SK-OV-3 ovarian cancer cells 10 µM 24 h Evaluate the effect of HS-243 on cancer cell survival, showing that HS-243 alone inhibited cell survival by 13%, and in combination with IL-1β, it inhibited cell survival by 46%. PMC7008364
AN3-CA pancreatic cancer cells 10 µM 24 h Evaluate the effect of HS-243 on cancer cell survival, showing that HS-243 alone inhibited cell survival by 21%, and in combination with IL-1β, it inhibited cell survival by 33%. PMC7008364
THP-1 human macrophages 10 µM 24 h Evaluate the effect of HS-243 on inflammatory responses in macrophages after LPS stimulation, showing that HS-243 significantly inhibited the secretion of IL-8, CD14, GRO-α, MIP-1α, MIP-3α, uPAR, Osteopontin, MMP-9, MCP-1, I-TAC, TIM-3, IP-10, GDF-15, and RANTES. PMC7008364
Human rheumatoid arthritis fibroblast-like synoviocytes (RA-FLS) 10 µM 24 h Evaluate the effect of HS-243 on cytokine/chemokine responses after LPS stimulation, showing that HS-243 significantly inhibited the expression of CCL5, CXCL12, MIF, and IL-18. PMC7008364
Bone marrow-derived dendritic cells (BMDCs) 50 μM 2 h Blocking IRAK1/4 signaling significantly reduced S. pneumoniae-induced IL-23 production and completely abolished the inhibitory effects of morphine on IL-23 production. PMC3060476

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description Reference
NSG mice A375 melanoma xenograft model Intratumoral injection 35 mg/kg Every 2 days for 5 days Combination therapy significantly delayed tumor growth and prolonged survival PMC3677596

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.53mL

0.51mL

0.25mL

12.65mL

2.53mL

1.26mL

25.29mL

5.06mL

2.53mL

References

 

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