(s) p38 mapk inhibitor iii

(S)-p38 MAPK inhibitor III is a methylsulfanylimidazole that inhibits p38 MAP kinase (IC50 = 0.90 μM in vitro). It is cell-permeable, potently blocking the release of TNF-α and IL-1β from human peripheral blood mononuclear cells (IC50s = 0.37 and 0.044 μM, respectively).

Cdk1 2 Inhibitor III is a selective inhibitor of Cdk1 2 with an IC50 value of 2.1 μM against CDK1 cyclin B.

p38 MAPK inhibitor is a potent inhibitor of p38 MAP kinase (IC50 = 35 nM). It inhibits senescence induced by the oncogene RAS.

VPS34 inhibitor 1 (Compound 19, PIK-III analogue) (PIK-III analogue) is a potent and selective inhibitor of VPS34( IC50 : 15 nM)

P-gp inhibitor 1 inhibits reversing P-glycoprotein-mediated multidrug resistance with an EC50 of 57.9 nM (K562 A02 cells).

p38-α MAPK-IN-1 is a MAPK14 (p38-α) inhibitor with an IC50 of 2300 nM in the EFC displacement assay and 5500 nM in the HTRF assay.

PDGFR Tyrosine Kinase Inhibitor III (PDGF Receptor Tyrosine Kinase Inhibitor III) is a multikinase inhibitor that inhibits PDGFR, EGFR, FGFR, PKA, and PKC and can be used for research on amyotrophic lateral sclerosis [1].

Tubulin Inhibitor 38 (Compound 14), a tetrazole-based agent, demonstrates significant antiproliferative effects by inducing mitotic arrest and blocking the cell cycle at the G2/M phase, ultimately triggering apoptosis. Administered at 100 nM for 24 hours, it shows considerable cytotoxicity and selectivity within HeLa, MCF7, and U87 MG cell lines [1].

p38 MAPK-IN-2 is a potent inhibitor of p38 kinase.

Compound 8a, also known as P-gp inhibitor 14, demonstrates high affinity as a P-gp inhibitor and effectively reverses P-gp-mediated multidrug resistance (EC 50 = 48.74 nM). Additionally, this compound exhibits a weak inhibitory effect on CYP3A4 activity [1].

P-gp Inhibitor 17 (compound 2g), a potent inhibitor, directly interacts with the transmembrane domain of P-gp. This compound is useful for studying P-gp-mediated multidrug resistance in tumor cells [1].

Human PD-L1 inhibitor III [Human PD-L1 inhibitor] is a bioactive compound designed to inhibit the programmed death-ligand 1 (PD-L1) protein in humans.

P-gp Inhibitor 15 (compound 7a), a nonsubstrate inhibitor of P-glycoprotein (Pgp), inhibits Pgp-ATPase activity and interferes with Pgp-mediated Rhodamine123 efflux. Additionally, this compound enhances the inhibitory effect of Paclitaxel on tumor progression in the KBV xenograft tumor model in nude mice [1].

Ftase Inhibitor III, derived from a phenotypic screen, functions as an anion-dependent inhibitor of Farnesyltransferase.

p38 MAPK inhibitor IV is an ATP-competitive inhibitor of p38 MAP kinases with IC50 values of 0.13, 0.55, 5.47, and 8.63 μM for p38α, p38β, p38x, and p38δ, respectively, in vitro.[1] It also inhibits LPS-induced TNF-α and IL-1β cytokine production (IC50s = 22 and 44 nM, respectively) in human peripheral blood mononuclear cells.

HSP47 inhibitor III suppressed collagen type I expression in human and mouse cells and suppressed the viability and migration of lung fibroblasts.

p38 MAPK-IN-3 (Compound 2c) is a potent inhibitor of p38α MAPK, exhibiting antitumor properties through the promotion of apoptosis and the enhancement of reactive oxygen species (ROS) production [1].

p38 MAPK-IN-1 displays sustained levels, low clearance, and good bioavailability. p38 MAPK-IN-1 is a novel effective and selective inhibitor of p38 MAPK (IC50: 68 nM).

S-(p-Nitrobenzyl)glutathione acts as a competitive inhibitor of glutathionase. Rat kidney microsomes convert this compound into associated cysteine derivatives. It serves as a research tool in investigating the catabolism of glutathione by the glutathionase system [1] [2].

Caspase-9 Inhibitor III (Ac-LEHD-cmk), a caspase-9 inhibitor, demonstrates protective effects against ischemia-reperfusion-induced myocardial injury.

P-gp Inhibitor 3, an effective P-glycoprotein (P-gp) inhibitor, activates P-gp ATPase to inhibit P-gp's efflux function. It demonstrates a relatively stronger multidrug resistance (MDR) reversal ability, thereby enhancing the anti-tumor efficacy of Paclitaxel.

P-gp Inhibitor 22 effectively inhibits P-glycoprotein (P-gp) and its efflux function, promoting apoptosis and the accumulation of MCF-7 ADR cells in the S phase [1].

p38 MAP Kinase Inhibitor Ⅵ is a potent p38 MAP Kinase inhibitor with anti-inflammatory activity.

Compound 40, NH2-c[X-R-L-S-X]-K-G-P-(D-2Nal), a macrocyclic analogue of Ape13, acts as a potent APJ agonist with a Ki of 5.7 nM. It demonstrates favorable Gα12-biased signaling and possesses an enhanced in vivo half-life [1].

(S,R)-WT IDH1 Inhibitor 2 is a selective and potent mutant IDH1 inhibitor that inhibits R132G (IC50: 2.9 nM), R132C (IC50: 3.8 nM), R132H (IC50: 4.6 nM) and WT IDH1 (IC50: 46 nM) with 100-fold higher selectivity than IDH2. 100-fold higher selectivity than IDH2. (S,R)-WT IDH1 Inhibitor 2 is investigated in acute myeloid leukemia (AML) and other cancers for its ability to induce intracellular 2-HG reduction, failure of myeloid differentiation block, and induction of granulocyte differentiation at the level of leukemia mother cells and more immature stem cells.

P38-α MAPK-IN-5 is a potent inhibitor of p38α, demonstrating inhibitory concentrations (IC50) of 0.1 nM for p38α, 0.2 nM for p38β, 944 nM for p38γ, and 4100 nM for p38δ. It exhibits anti-inflammatory properties and holds potential for research in asthma and chronic obstructive pulmonary disease (COPD).

p38-α MAPK-IN-4 (Compound 69) is a selective inhibitor of p38α MAPK, with an IC50 of 1.5 μM, and effectively mitigates the onset of mechanical allodynia (MA) in vivo [1].

(S,E)-2-Methyl-6-(p-tolyl)hept-3-en-2-ol is a useful organic compound for research related to life sciences and the catalog number is T125520.

Super-chelating agent & MRI contrast agent

P-gp Inhibitor 2 is a powerful P-glycoprotein (P-gp) inhibitor, effective in reversing Doxorubicin resistance with an IC50 of 0.22 µM in human colorectal carcinoma cells overexpressing P-gp (SW600 Ad300).

P-gp inhibitor 4 is a selective P-glycoprotein modulator with an EC 50 of 94 nM. P-gp inhibitor 4 increases drug transport across gastro-intestinal barrier and recovers doxorubicin toxicity in multidrug resistant cancer cells .

P-gp Inhibitor 13, a P-glycoprotein antagonist, can counteract paclitaxel resistance in A2780 T cells, proving valuable for advanced acute myeloid leukemia research [1].

HIV-1 inhibitor-38 (Compound 91) is a potent HIV-1 activity inhibitor and shows significant potential as a novel latency reversing agent, making it a promising candidate for further development [1].

β-Secretase Inhibitor III is a highly selective inhibitor of BACE1 with a Ki value of 0.13 nM.

P-gp inhibitor 5 is a potent P-glycoprotein (P-gp) inhibitor, reducing P-gp activity by a factor of 2.5 and 3.0 at 1.25 μM and 2.5 μM, respectively. It exhibits anti-proliferative effects on certain cancer cells and restores cellular sensitivity to Vincristine and Paclitaxel, reversing the multidrug resistant (MDR) phenotype of ABCB1 Flp-InTM-293 and KBvin.

Lck Inhibitor III, a potent inhibitor of Lck, exhibits an IC50 value of 867 nM. Additionally, this compound effectively inhibits IL-2 synthesis in Jurkat cells, demonstrating an IC50 of 1.270 μM.

Compound 39 (NH2-c[X-R-L-S-X]-K-G-P-(D-1Nal)) is a potent agonist of the APJ receptor, possessing a K i value of 0.6 nM. It is capable of activating Gαi1, with an EC 50 of 0.8 nM, and of recruiting β-arrestin2, with an EC 50 of 31 nM. Furthermore, this compound demonstrates extended effects on cardiac function [1].

Compound 135, also known as p38 Kinase Inhibitor 4, is a potent inhibitor of p38 [1].

p38 Kinase Inhibitor 5 (AA6) is a powerful inhibitor of p38 kinase, exhibiting an IC50 of 403.57 nM. This compound demonstrates significant anti-inflammatory activity [1].

Compound 3a (p38-α MAPK-IN-6) is an inhibitor of the p38α mitogen-activated protein kinase [1].