2. NF-κB
  3. IKK
  4. (Rac)-PF-184 hydrate

(Rac)-PF-184 hydrate is a potent inhibitory factor-κB kinase 2 (IKK-2) inhibitor with an IC50 of 37 nM. (Rac)-PF-184 hydrate has anti-inflammatory effects.

For research use only. We do not sell to patients.

(Rac)-PF-184 hydrate Chemical Structure

(Rac)-PF-184 hydrate Chemical Structure

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Based on 1 publication(s) in Google Scholar

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(Rac)-PF-184 hydrate Related Antibodies

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Description

(Rac)-PF-184 hydrate is a potent inhibitory factor-κB kinase 2 (IKK-2) inhibitor with an IC50 of 37 nM. (Rac)-PF-184 hydrate has anti-inflammatory effects[1].

IC50 & Target[1]

IKK-2

37 nM (IC50)

In Vitro

(Rac)-PF-184 has slow dissociation kinetics with a T1/2 of 6.7 h from rhIKK-2, very low oral bioavailability (5%), high intravenous clearance (59 ml/min/kg), and high P450 metabolism in human liver microsomes[1].
(Rac)-PF-184 binds tightly to endogenous IKK-2 and shows extended inhibition of kinase activity and cytokine production[1].
(Rac)-PF-184 shows a concentration-dependent inhibition on LPS- and IL-1β-induced production of inflammatory mediators in a variety of human disease-relevant cells[1].
(Rac)-PF-184 (0.001-10 µM; 1 h) inhibits IL-1β-induced TNF-α in a concentration-dependent manner with maximal efficacies of 94% and relative potencies of 163 nM[1].
(Rac)-PF-184 inhibits LPS-induced cytokine production from rat alveolar macrophages and blocked p65 nuclear translocation[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

(Rac)-PF-184 hydrate Related Antibodies
In Vivo

(Rac)-PF-184 (0.3-2.5 mg; i.t.; once) blocks neutrophil infiltration and BAL cell cytokine production[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Fasted male Sprague-Dawley rats (350 g) placed into a chamber connected to a large volume nebulizer filled with 20 ml of 1 mg/mL solution of LPS[1]
Dosage: 0.3-2.5 mg
Administration: Nano suspension and administered intratracheally in a volume of 100 µL, 60 min before aerosolized LPS
Result: Resulted in a comparable attenuation of total cell and PMN cell infiltration 4 h after LPS exposure. Dose-dependently inhibited cell infiltration with EC50 values of 1 mg. Dose-dependently suppressed BAL fluid TNF- and PGE2 levels comparable with cell infiltration. Inhibited p65 translocation. Showed long-lasting activity.
Molecular Weight

659.64

Formula

C32H34ClFN6O5
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=NN(C2=C1CCC3=C2C=C(NC(C4=CC(N5CC(CO)(C(CO)(C5)C)C)=NC=C4Cl)=O)C=C3)C6=CC=C(C=C6)F)N.[2.25].O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation

Purity: ≥98.0%

COA (252 KB)

Handling Instructions (2659 KB)
References
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(Rac)-PF-184 hydrate Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

(Rac)-PF-184IKKIκB kinaseI kappa B kinaseLPSIL-1βanti-inflammatoryPBMCneutrophilsA549endothelial cellBALp65Inhibitorinhibitorinhibit

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(Rac)-PF-184 hydrate
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