iq 1

IQ-1S free acid (IQ-1S) is an effective and specific c-Jun N-Terminal Kinase Inhibitor. IQ-1S inhibits murine delayed-type hypersensitivity. IQ-1S can reduce inflammation and cartilage loss associated with CIA and can serve as a small-molecule modulator for mechanistic studies of JNK function in rheumatoid arthritis. IQ-1S is highly specific for JNK and that its neutral form is the most abundant species at physiologic pH.

IQ 1 has multiple roles, such as maintaining the multifunctionality of mouse ESCs, decreasing Wnt-stimulated phosphorylation, blocking PP2A/Nkd interactions, and so on.

IQ-1S is an inhibitor of NF-κB/activating protein 1 (AP-1) with an IC50 of 1.8 μM. It exhibits high binding affinity to all three JNKs, with Kd values for JNK3, JNK2, and JNK1 being 87 nM, 360 nM, and 390 nM, respectively.

LIQ1 is a flavonoid derivative and a potent allosteric inhibitor of pyruvate kinase M2 (PKM2) with an IC50 of 0.39 μM and a Kd of 4.5 μM, targeting the Arg43 in the poly-arginine pocket. It demonstrates efficacy in an LPS-induced mouse endotoxemia model by preventing PKM2 nuclear translocation and inhibiting its interaction with HIF-1α, thus suppressing IL-1β transcription. LIQ1 is applicable in endotoxemia research.

TIQ-15 is an effective and selective CXCR4 antagonist. It has good drug-like properties.

SIQ17, an EGFR inhibitor, blocks the ATP-binding site with an IC50 of 0.62 nM, demonstrating more effective EGFR-TK inhibitory activity than the known inhibitor Erlotinib (IC50 of ∼20 nM). SIQ17 is applicable in cancer research [1].

Camstatin TFA, a 25-residue fragment derived from the IQ motif of PEP-19, effectively binds to calmodulin and inhibits neuronal nitric oxide (NO) synthase, demonstrating its functional activity [1].

Me-IQ (Methyl-IQ) is a heterocyclic amine that exhibits both carcinogenic and mutagenic properties. It displays significantly higher mutagenic activity in liver microsomal preparations compared to those from the lungs in uninduced mice and rabbits [1] [2].