permeate

JNK3 Inhibitor-4, a potent 2-aryl-1-pyrimidinyl-1H-imidazole-5-yl acetonitrile derivative, demonstrates a strong inhibitory effect on JNK3 with an IC 50 value of 1.0 nM. It exhibits exceptional selectivity against JNK3 when compared to other protein kinases, including isoforms JNK1 (IC 50 = 143.9 nM) and JNK2 (IC 50 = 298.2 nM). Additionally, JNK3 Inhibitor-4 benefits from neuroprotective properties and is predicted to permeate the blood-brain barrier effectively.

HPi1 is a selective and orally active antimicrobial against Helicobacter pylori (IC50: 0.24 μM and a MIC of 0.08-0.16 μg mL). HPi1 is inactive against other Xaliproden, including the gut commensals, Lactobacillus reuteri, Lactobacillus casei, and Bifidoba

Lauroyl-L-carnitine (chloride) (Lauroyl-L-carnitine Hydrochloride), an acylcarnitine and surfactant, has been used to permeate porcine intestinal cells to deliver the polar fluorescent probe fluorescent yellow.

Ppc-1 is a chemical compound known for its inhibitory effects on the Gram-negative periodontopathogen Porphyromonas gingivalis. It acts as a mitochondrial uncoupler, enhancing mitochondrial oxygen consumption without affecting ATP production. Additionally, Ppc-1 serves as a cell-permeate inhibitor of interleukin-2 (IL-2). This compound exhibits various beneficial activities, including anti-obesity, antibacterial, and anti-inflammatory properties.

SL 0101-1 (SL0101) is a selective, efficient, reversible and ATP-competitive inhibitor of p90 ribosomal S6 kinase (RSK) that can permeate cell membranes, with an IC50 value of 89 nM for RSK.SL 0101-1 (SL0101) is also a potent RSK1 2 inhibitor with a Ki value of 1 μM. SL 0101-1 (SL0101) is also a potent RSK1 2 inhibitor with a Ki value of 1 μM.

SORT1-IN-3 (compound 5) is a SORT1 inhibitor characterized by its ability to permeate the blood-brain barrier.

SORT1-IN-4 (compound 6) is a SORT1 inhibitor with the ability to permeate the blood-brain barrier.

SMARt751 targets the transcriptional regulator VirS, inhibiting its ability to bind DNA, which in turn enhances the expression of the mymA operon and activates Ethionamide. This activation increases the antimicrobial efficacy of Ethionamide against Mycobacterium tuberculosis, and overcomes its resistance. Furthermore, SMARt751 augments Ethionamide's antibacterial activity in mouse models and reduces its effective dose. Additionally, SMARt751 can permeate the blood-brain barrier.

Diclofenac methyl ester is a hydrophobic prodrug form of the non-steroidal anti-inflammatory drug (NSAID) diclofenac . It is more soluble than diclofenac acid in isopropylmyristate. Diclofenac methyl ester does not permeate human epidermal membranes in vitro.

DCN-83, a potent anti-leishmanial compound, exhibits its highest efficacy against the amastigote form, achieving an IC50 value of 0.71 μM. It also possesses the ability to permeate the blood-brain barrier, impacting the central nervous system [1].

T-518, an orally active and selective HDAC6 inhibitor with an IC50 value of 36 nM for human HDAC6, can permeate the blood-brain barrier and is applicable in tauopathy research [1].

IGGi-11me, a prodrug that can permeate membranes, is derived from IGGi-11, the inaugural inhibitor targeting the noncanonical activation of heterotrimeric G-protein signaling. By binding to G-protein α-subunits (Gαi), IGGi-11 specifically disrupts their interaction with GIV Girdin, thereby obstructing noncanonical G-protein signaling in tumor cells and hindering the proinvasive characteristics of metastatic cancer cells.

GPR17 Modulator-1 (Compound 2-046) is a regulator of the G protein-coupled receptor 17 (GPR17), displaying an IC50 of less than 10 nM against hGPR17 in CHO cells. This compound exhibits moderate pharmacokinetic properties in mice and possesses the ability to permeate the blood-brain barrier (BBB).

IP6K-IN-2 (compound 29c) is an IP6K inhibitor that demonstrates oral bioavailability and the ability to permeate the blood-brain barrier (IC 50 : 15.8 nM), making it suitable for research on central nervous system diseases.