IQ-1S Free Acid is a selective JNK3 inhibitor with IC50 value of 87 nM, with less potency againstJNK 1/2 with IC50 values of 390/360nM.
HazMat Fee +
There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.
Type
HazMat fee for 500 gram (Estimated)
Excepted Quantity
USD 0.00
Limited Quantity
USD 15-60
Inaccessible (Haz class 6.1), Domestic
USD 80+
Inaccessible (Haz class 6.1), International
USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic
USD 100+
Accessible (Haz class 3, 4, 5 or 8), International
The activating protein 1 (AP-1) and nuclear factor-κB (NF-κB) families of transcription factors are implicated in many pathological processes. C-Jun N-terminal kinases (JNKs) have been shown to regulate the transcriptional activity of AP-1. IQ-1S free acid is a potent inhibitor of pro-inflammatory cytokines without cytotoxic effect. It inhibits NF-κB/AP-1 activity with an IC50 value of 2.3±0.41μM. Treatment of human peripheral blood mononuclear cells with IQ-1S free acid (20μM) significantly inhibited LPS (200ng/ml)-induced production of pro-inflammatory cytokines, including IL-1α, IL-1β, IL-6, IL-10, and TNF-α, compared to DMSO-treated controls. The IC50 values of IQ-1S free acid for TNF-α and IL-6 in human MonoMac-6 cells are 1.3±0.31 and 3.8±0.78μM, respectively. The IC50 values of IQ-1S free acid for TNF-α and IL-6 in human peripheral blood mononuclear cells are 2.6±0.63 and 5.6±1.1μM, respectively. The IC50 values of IQ-1S free acid for NO in murine J774.A1 cells is 3.1±0.87μM. The binding affinity of IQ-1S free acid for JNK1, JNK2, and JNK3 are 0.24, 0.36, and 0.10μM, respectively. IQ-1S free acid also exhibits binding affinity towards CK1δ, PI3Kγ, and MKNK2 with Kd values of 0.38, 0.47, and 0.92μM, respectively. When mice were i.p. administered with IQ-1S free acid at a dose of 12.5 and 30mg/kg, the serum AUC0-12h values were 2.9 and 7.4μM/h, respectively. The i.p. injection of OVA-challenged mice with 12.5mg/kg IQ-1S free acid (every 12 h, a total of 5 injections) significantly suppressed OVA-induced CD4+ T-cell immune response compared to the vehicle-treated group[3].
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