GS 143 is a β-TrCP1 ligase inhibitor. Inhibits IκBα ubiquitination (IC50 = 5.2 μM) without affecting proteasome activity. Blocks LPS-induced expression of inflammatory cytokines in human myelomonocytic cells. Suppresses antigen-induced NFκB expression, inflammation and mucus production in airways of OVA-sensitized mice.
| Molecular Weight | 466.46 |
| Formula | C28H19FN2O4 |
| CAS Number | 916232-21-8 |
| Form | Solid |
| Solubility (25°C) | DMSO 46.65 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related IκB/IKK Products |
|---|
| BMS-066
BMS-066 is an IKKβ/Tyk2 pseudokinase inhibitor, with IC50s of 9 nM and 72 nM, respectively. |
| Ainsliadimer A
Ainsliadimer A is a novel guaiacolide sesquiterpene dimer isolated from Ainsliaea macrocephala.Ainsliadimer A can block the NF-κB signaling pathway by binding to IKK α/β, and possesses anti-tumor and anti-inflammatory activities.Meanwhile, Ainsliadimer A can also Ainsliadimer A can also directly target peroxidase 1 and 2 (PRDX1 and PRDX2) and significantly inhibit their enzymatic activities. In addition, Ainsliadimer A can cause mitochondrial dysfunction by altering the permeability of mitochondrial membrane potential, inhibiting mitochondrial respiration and ATP production, inhibiting cell proliferation, promoting cell cycle arrest in G2/M phase, and inducing apoptosis. |
| IKK2-IN-4
IKK2-IN-4 is a potent IKK-2 inhibitor, with an IC50 of 25 nM. |
| MRT67307 dihydrochloride
MRT67307 dihydrochloride is a dual inhibitor of the IKKε and TBK-1 with IC50s of 160 and 19 nM, respectively. |
| 4′-Hydroxywogonin
4′-Hydroxywogonin has anti-inflammatory activity via TAK1/IKK/NF-κB, MAPKs and PI3/AKT signaling pathways. 4′-Hydroxywogonin inhibits angiogenesis by disrupting PI3K/AKT signaling. 4′-Hydroxywogonin inhibits cell proliferation and induces apoptosis. |
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