One of the most relevant brands among our more than 25 partners is TargetMol

AS-605240 (potassium) is an orally active PI3Kγ inhibitor with an IC50 of 8 nM and a Ki of 7.8 nM. It inhibits MCP-1 and CSF1-induced PKB phosphorylation with IC50 values of 0.181 µM and 0.550 µM, respectively. In mouse models of peritonitis induced by RANTES (CCL5) and thioglycolate, AS-605240 (potassium) reduces neutrophil recruitment, showing EC50 values of 9.1 mg/kg and 10 mg/kg. Additionally, AS-605240 (potassium) ameliorates arthritis induced by αCII-IA in mice.

Rho GTPase inhibitor 1 (compound 7) is a potent inhibitor of Rho GTPase. It exhibits high affinity for Cdc42, Rac1, and RhoA, with dissociation constants (KDs) of 151 μM, 352 μM, and 232 μM, respectively. Additionally, Rho GTPase inhibitor 1 reduces cell migration in glioblastoma cell lines.

PKM2-IN-10 is a PKM2 inhibitor. It effectively suppresses the proliferation of A549 and HCC1833 cell lines with IC50 values of 3.36 μM and 9.20 μM, respectively. PKM2-IN-10 demonstrates antitumor activity in human non-small cell lung cancer (NSCLC) and mouse lung adenocarcinoma models. It is applicable for research in lung cancer.

(H)S(OMe)-DFR-kbt (compound 9) is a potent selective inhibitor of TMPRSS2, with a Ki value of 0.13 nM. It is utilized in research related to SARS-CoV-2.

BET bromodomain inhibitor is a potent BET inhibitor.

Norethisterone enanthate (NSC-9564) is a long-acting parenteral progestogen with antigonadotropic effects.

FLY26 is a selective partial antagonist of GluN2B, with an IC50 value of 0.64 μM. FLY26 inhibits the GluN2B subunit of NMDA receptors, reducing calcium ion influx and reactive oxygen species (ROS) production. It also activates the BDNF/TrkB/CREB neuroprotective signaling pathway, mitigating excitotoxicity and mitochondrial dysfunction. FLY26 holds potential for treating neurological deficits caused by cerebral ischemia-reperfusion injury.

KIM-161 is a PIK3CA inhibitor. It demonstrates significant antiproliferative activity, with IC50 values of 1.428 and 1.562 µM against PI3KCA-mutant breast cancer cell lines MCF7 and T47D, respectively. KIM-161 induces apoptosis and cell cycle arrest by inhibiting the PI3K/AKT/mTOR signaling pathway, leading to ROS production. It is applicable for research on breast cancer and its PI3KCA-mutant subtypes.

Insecticidal agent 24 is an orally active pyridinyl spiroindoline lead compound. It demonstrates antimalarial activity with Pf NF54IC50 of 0.08 μM. Insecticidal agent 24 also inhibits hERG activity with an IC50 of 6.5 μM. In a humanized immunodeficient NSG mouse model of malaria infection, it effectively reduces parasitemia.

BChE-IN-40 (compound D40) is a potent butyrylcholinesterase inhibitor with an IC50 of 0.59 μM. It demonstrates significant anti-inflammatory effects, with an IC50 of 4.55 μM in inhibiting nitric oxide production. Additionally, BChE-IN-40 exhibits excellent permeability across the blood-brain barrier.

Isoxaflutole (RP-201772) is a low toxic herbicide and has been marketed as a substitute for atrazine.

AD015 is a dual inhibitor of angiotensin-converting enzyme (ACE) and neprilysin (NEP), effectively inhibiting NEP, nACE, and cACE with IC50 values of 0.009, 0.019, and 0.0008 μM, respectively.

LC-SF-14 is a selective dual inhibitor of SHP2 and FGFR, with IC50 values of 71.6 nM and 8.9 nM, respectively. It blocks FGFR2-FRS2α-SHP2-MAPK signaling and ERK phosphorylation, and also inhibits the proliferation of KATOIII cancer cells (IC50: 9.2 nM). Furthermore, LC-SF-14 exhibits antitumor activity in SNU-16 xenograft mouse models, making it suitable for research on FGFR2-driven gastric cancer.

HDAC/PSMD14-IN-1 is a derivative of gambogic acid. It serves as an orally active dual inhibitor targeting PSMD14 and HDAC1, with IC50 values of 238.7 nM and 141.2 nM, respectively. The compound exhibits significant cytotoxicity against ESCC cell lines (IC50: 30-250 nM) and effectively reverses epithelial-mesenchymal transition (EMT). Additionally, HDAC/PSMD14-IN-1 can induce apoptosis. In KYSE30 cell xenograft models in mice, it displays antitumor activity. HDAC/PSMD14-IN-1 is useful for researching esophageal cancer treatment.

<p>ASN-1377642 is an NK1 receptor antagonist with a Ki value of 251 nM. It demonstrates antitumor activity in breast cancer cells with high expression of NK1R-Tr.</p>

Flucetosulfuron is a sulfonylurea herbicide

AMTG-DA1 is a ligand for the gastrin-releasing peptide receptor (GRPR), and it can be utilized in cancer research.

CCR1 antagonist13 is a selective small molecule antagonist of CCR1.

<p>Mrgx2 antagonist-3 (Compound B-40) is a highly selective antagonist of the MrgX2 receptor, with an IC50 range of 0.042-2.5 nM. It blocks downstream G protein signaling and β-arrestin recruitment, inhibiting Mrgx2 receptor-mediated calcium influx and cell degranulation. Mrgx2 antagonist-3 shows potential for research in inflammation-associated diseases and pruritus, such as chronic urticaria and allergic asthma.</p>

Carbonic anhydrase inhibitor33 (11D) is a dual inhibitor that targets both CA (carbonic anhydrase) IX/XII and CDK6. It exhibits Ki values of 19.7 nM for hCA IX and 26.1 nM for hCA XII. Additionally, Carbonic anhydrase inhibitor33 (11D) can induce G1 phase cell cycle arrest and apoptosis, making it relevant for research in non-small cell lung cancer (NSCLC).