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TLR-signaling Inhibitors
MAPK Pathway Inhibitors
NF-κB Pathway Inhibitors
PI3K Pathway Inhibitors
PRR Inhibitors

Product Lines > Innate Immunity & Inflammation > Signal Transduction Inhibitors

Signal Transduction Inhibitors

InvivoGen offers a selection of known inhibitors of the signaling pathways initiated by pattern recognition receptors (PRRs). These inhibitory molecules intervene in the different steps of PRR activation and signaling cascade, including ligand binding, interaction with adapters, and activation of MAP kinases and NF-κB.

TLR-signaling Inhibitors
Pepinh-MYD: MyD88 inhibitiry peptide
Innate Immunity inhibitors Pepinh-TRIF: TRIF inhibitory peptide

MAPK Pathway Inhibitors
PD98059: MAP kinase kinase inhibitor
SB203580: p38 MAP kinase inhibitor
SP600125: JNK inhibitor
U0126: MEK1-MEK2 inhibitor

NF-kB Pathway Inhibitors
Bay11-7082: IkB-a inhibitor
Celastrol: NF-kB inhibitor

PI3K Pathway Inhibitors
AG490: JAK2 inhibitor
LY294002: PI3K inhibitor
Wortmannin: PI3K inhibitor

PRR Activation & Signaling Inhibitors
2-Aminopurine: PKR inhibitor
Chloroquine: Endosome acidification inhibitor
CLI-095: TLR4 signaling inhibitor
H-89: PKA inhibitor
Polymyxin B: LPS-induced TLR4 activation inhibitor

Contents and Storage

TLR-signaling Inhibitors

Pepinh-MYD and pepinh-TRIF are cell-penetrating peptides that interfere with TLR signaling. They contain the BB loop sequences of the TIR domains of MyD88 or TRIF preceeded by a protein transduction sequence derived from antennapedia which enables the peptide to translocate through the cell membrane [1].
Pepinh-MYD blocks MyD88 signaling by inhibiting its homodimerization through binding [2]. Pepinh-TRIF inhibits TRIF signaling by interfering with TLR-TRIF interaction [3].
Pepinh-MYD was shown to significantly block TLR2- and TLR8-induced NF-κB activation in THP1-Blue™ cells while the efficacy of Pepinh-TRIF was confirmed in Ramos-Blue™ cells induced by the TLR3 ligand poly(I:C).

1. Derossi D. et al., 1994. The third helix of the Antennapedia homeodomain translocates through biological membranes. J. Biol. Chem., 269: 10444-50.
2. Loiarro M. et al., 2005. Peptide-mediated Interference of TIR Domain Dimerization in MyD88 Inhibits Interleukin-1-dependent Activation of NF-{kappa}B. J. Biol. Chem., 280: 15809-14.
3. Toshchakov vU. et al., 2005. Differential Involvement of BB Loops of Toll-IL-1 Resistance (TIR) Domain-Containing Adapter Proteins in TLR4- versus TLR2-Mediated Signal Transduction. J. Immunol., 175: 494 - 500.

Inhibitory activities of Pepinh-MYD and Pepinh-TRIF

Inhibitory activities of Pepinh-MYD and Pepinh-TRIF.
THP1-Blue™ cells and Ramos-Blue™ cells were pretreated with 50 μM Pepinh-Control, Pepinh-MYD or Pepinh-TRIF for 6 hours.Then THP1-Blue™ cells were stimulated with Pam3CSK4 (100 ng/ml) or R848 (10 μg/ml) and Ramos-Blue™ cells with poly(I:C) (100 ng/ml).After 24h incubation, NF-kB activation was assessed by measuring the levels of SEAP in the supernatant using the QUANTI-Blue™ assay.

Product	Description	Endotoxin Level	Working Conc.	TDS	Qty	Cat. Code	Price	Order
Pepinh-MYD NEW	MyD88 inhibitory peptide	Endotoxin-free	50 - 100 µM	PDF	2 mg	tlrl-pimyd	check
Pepinh-TRIF NEW	TRIF inhibitory peptide	Endotoxin-free	50 - 100 µM	PDF	2 mg	tlrl-pitrif	check

MAPK Pathway Inhibitors

Product	Description	Endotoxin Level	Working Conc.	TDS	MSDS	Qty	Cat. Code	Price
PD98059	MAP Kinase Kinase Inhibitor	Endotoxin-free	50 - 100µM	PDF	PDF	10 mg	tlrl-pd98	check
SB203580	p38/RK MAP Kinase Inhibitor	Endotoxin-free	1 - 20µM	PDF	PDF	5 mg	tlrl-sb20	check
SP600125	JNK inhibitor	Endotoxin-free	10-500 µM	PDF	PDF	10 mg	tlrl-sp60	check
U0126	MEK1 and MEK2 Inhibitor	Endotoxin-free	10 - 50µM	PDF	PDF	5 mg	tlrl-u0126	check

NF-κB Pathway Inhibitors

Product	Description	Endotoxin Level	Working Conc.	TDS	MSDS	Qty	Cat. Code	Price	Order
Bay11-7082	IκB-α inhibitor	Endotoxin-free	1 - 10 µM	PDF	PDF	10 mg	tlrl-b82	check
Celastrol	NF-κB inhibitor	Endotoxin-free		PDF	PDF	1 mg	ant-cls	check

PI3K Pathway Inhibitors

Product	Description	Endotoxin Level	Working Conc.	TDS	MSDS	Qty	Cat. Code	Price
AG490	JAK2 inhibitor	Endotoxin-free	1-100 µM	PDF	PDF	10 mg	tlrl-ag4	check
Wortmannin	PI3K inhibitor	Endotoxin-free	0.1-2.5 µM	PDF	PDF	5 mg	tlrl-wtm	check
LY294002	PI3K Inhibitor	Endotoxin-free	50 - 100µM	PDF	PDF	5 mg	tlrl-ly29	check

PRR Activation & Signaling Inhibitors

Product	Description	Endotoxin Level	Working Conc.	TDS	MSDS	Qty	Cat. Code	Price
2-AminoPurine	PKR Inhibitor	Endotoxin-free	1 - 10 mM	PDF	PDF	250 mg	tlrl-apr	check
Chloroquine	Inhibitor of Endosomal Acidification	Endotoxin-free	10 µM	PDF	PDF	250 mg	tlrl-chq	check
CLI-095	TLR4 signaling inhibitor	Endotoxin-free	50 nM - 1 µM	PDF	PDF	1 mg	tlrl-cli95	check
H-89	PKA inhibitor	Endotoxin-free	10-50 µM	PDF	PDF	5 mg	tlrl-h89	check
Polymyxin B	Inhibitor of LPS-induced TLR4 activation	Endotoxin-free	10 µg/ml	PDF	PDF	100 mg	tlrl-pmb	check

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Note that the sequence of available ORFs provided by InvivoGen can differ from a given reference Genbank record due to genetic variations and/or alternative splicing. Customers should verify that the version of a gene sold by InvivoGen is suitable for the customer needs.

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