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PS-1145

SKU: orb1225064

Description

A specific IκB kinase (IKK) inhibitor with IC50 of 88 nM; shows no activity for JNK2, c-Src, p38α, IRAK, Lck, etc.; blocks TNFα-induced NF-κB activation in MM cells through inhibition of IκBα phosphorylation and degradation of IκBα, respectively; blocks the protective effect of IL-6 against Dex-induced apotosis, inhibits both IL-6 secretion from BMSCs triggered by MM cell adhesion and proliferation of MM cells adherent to BMSCs.
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Images & Validation

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PS-1145

Key Properties

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CAS Number431898-65-6
MW322.7484
Purity>98% (HPLC)
FormulaC17H11ClN4O
SMILESC1=CC(=CN=C1)C(=O)NC2=CC(=CC3=C2NC4=C3C=CN=C4)Cl
TargetIκB kinase (IKK)
SolubilityDMSO: ≥ 43 mg/mL

Bioactivity

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In Vivo
Administration of either Bortezomib or PS-1145 (50 mg/kg) results in a significant decrease in serum levels of all 3 cytokines that is nonsignificantly different from those in mice that underwent transplantation with TCD BM alone. PS1145 is injectedintracerebroventricular (icv)as a pretreatment to block hypothalamic inflammation induced by IL-4 in adult male Wistar rats consuming a high-fat diet (HFD) over an 11-day period. The four groups of rats according to icv pretreatment/treatment condition are Veh/Veh, Veh/IL-4, PS1145/Veh, and PS1145/IL-4. Rats in the Veh/IL-4 group display increased weight gain on the HFD compared with the Veh/Veh group (P<0.05 on days 6-9). Importantly, the effect of icv IL-4 administration to increase body fat mass during high-fat (HF)feeding is completely blocked by icv PS1145 pretreatment at a dose that has no independent effect on body composition (on day 8: P<0.001, PS1145/Veh vs. PS1145/IL-4; P = not significant, PS1145/Veh vs. Veh/Veh). In PS1145/IL-4 injected rats, IL-1β mRNA content is decreased by ~75% compared with that of Veh/IL-4-injected rats.
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In Vitro
PS-1145 blocks TNFα-induced NF-κB activation in a dose- and time-dependent fashion in MM cells through inhibition of IκBα phosphorylation. Dexamethasone (Dex), which up-regulates IκBα protein, enhances blockade of NF-κB activation by PS-1145. PS-1145 blocks the protective effect of IL-6 against Dex-induced apotosis. TNFα-induced intracellular adhesion molecule (ICAM)-1 expression on both RPMI8226 and MM.1S cells is also inhibited by PS-1145. Moreover, PS-1145 inhibits both IL-6 secretion from bone marrow stromal cells (BMSCs)triggered by MM cell adhesion and proliferation of MM cells adherent to BMSCs.
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Storage & Handling

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StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

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PS1145 | PS 1145

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Gene Symbol
IκB kinase (IKK)

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PS-1145 (orb1225064)

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1 g
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2 mg
$ 110.00
5 mg
$ 140.00
10 mg
$ 230.00
25 mg
$ 410.00
50 mg
$ 780.00
100 mg
$ 1,100.00
500 mg
$ 2,220.00
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