HEK293

Shield-1 is a specific, high-affinity, and cell-permeable ligand for FK506-binding protein 12 (FKBP) and reverses instability by binding to mutant FKBP (mtFKBP), allowing conditional expression of mtFKBP fusion proteins.

Rapamycin (AY 22989) is a natural product of macrolides, an mTOR inhibitor with specificity (HEK293 cells: IC50=0.1 nM). Rapamycin has immunosuppressive activity and induces autophagy.

Mavatrep (JNJ-39439335) is a selective antagonist of TRPV1 with Ki of 6.5 nM and can be used for studies about inflammatory pain.

Slingshot inhibitor D3 (JHN76359) is a potent inhibitor of the Protein Phosphatase Slingshot.

Oct3/4-inducer-1 (2-(4-(4-methoxybenzyloxy)phenyl)acetonitrile) is an OCT3/4 inducer that promotes the expression and stabilization of OCT3/4 and enhances its transcriptional activity in a variety of human cells.

JH-II-127 is an oral inhibitor of leucine-rich repeat kinase 2 (LRRK2), targeting WT LRRK2, G2019S LRRK2, and A2016T LRRK2 with IC50 values of 6.6 nM, 2.2 nM, and 47.7 nM, respectively.

EP4 Receptor Antagonist 1 is a highly potent and selective competitive prostanoid EP4 receptor antagonist, effective for cancer immunotherapy. It inhibits both human and mouse EP4 receptors with IC50 values of 6.1 nM and 16.2 nM, respectively, while displaying minimal activity (IC50s >10 μM) against human EP1, EP2, and EP3 receptors.

Ogerin is a selective GPR68 positive allosteric modulator (pEC50: 6.83) that blocks recall in fear conditioning in mice. It exhibits inverse agonist and antagonist activity (Ki, 220 nM) at the A2A receptor and weak antagonist activity (Ki, 736 nM) at the 5-HT2B receptor.

WRG-28 is a potent and selective, allosteric discoidin domain receptor 2 (ddr2) inhibitor(IC50 : 230 nM)

6-OAU (GTPL5846)(GTPL5846; 6-n-octylaminouracil) is a surrogate agonist of GPR84; activates human GPR84 in the presence of Gqi5 chimera in HEK293 cells with an EC50 of 105 nM in the PI assay.

Taprenepag (CP-544326) (CP-544326) is a potent and selective prostaglandin E2 receptor agonist (EC50 = 2.8 nM). Taprenepag has been used in trials studying the treatment of Ocular Hypertension and Glaucoma, Open-Angle.

Mollugin (Rubimaillin) may be a JAK2 inhibitor and inhibits LPS-induced inflammatory responses by blocking the activation of the JAK-STAT pathway. Mollugin as a candidate for a chemotherapeutic agent in OSCCs via the upregulation of the HO-1 and Nrf2 pathways and the downregulation of NF- κ B. Mollugin may be a novel therapeutic candidate for bone loss-associated disorders including osteoporosis, rheumatoid arthritis, and periodontitis. Also, it has anticancer efficacy, can modulate the HER2 pathway in HER2-overexpressing Y cells with a potential role in the treatment and prevention of human breast and ovarian Y with HER2 overexpression.

MS 049 is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC 50 of 34 nM and 43 nM, respectively.

GeA-69 (GeA69) is a selective and allosteric PARP14 macrodomain 2 (MD2) inhibitor (Kd: 0.86 μM in ITC assays).

Ceefourin 1 is a highly selective multidrug resistance protein 4 (MRP4) inhibitor.

I3MT-3 (HMPSNE) (HMPSNE) is a potent, selective and cell membrane permeability inhibitor of 3-mercaptopyruvate sulfur transferase (3MST), which targets the persulfated cysteine residues located at the active site of 3MST.

Sulfopin is a highly selective covalent inhibitor of Pin1 with an apparent Ki of 17nM. Sulfopin blocks Myc-driven tumors in vivo.

IRE1α kinase-IN-1 is a highly selective IRE1α (ERN1) inhibitor, with an IC50 of 77 nM, displaying 100-fold selectivity over the IRE1β isoform. It inhibits ER stress-induced IRE1α oligomerization and autophosphorylation, as well as IRE1α RNase activity (IC50=80 nM).

ML-090 is NOX1-specific inhibitor(IC50 = 90 nM) which is >100 selectivity for NOX1 over NOX2, NOX3, NOX4 (all IC50s >10 μM).

Capsaicin is an active natural component found in chili peppers and acts as a TRPV1 agonist (EC50 = 0.29 μM). It possesses multiple activities, including pain relief, antitumor, anti-inflammatory, antioxidant, and neuroprotective effects, as well as some neurotoxicity. Capsaicin can be used to establish itch models.

KY1220 destabilizes both β-catenin and Ras by targeting the Wnt/β-catenin pathway. It has an IC50 of 2.1 μM in HEK293 reporter cells.

ML67-33 rapidly and reversibly affects K2P2.1 (TREK-1) (EC50s: 36.3 μM and 9.7 μM in cell-free and HEK293 cells, respectively). ML67-33 is a selective activator of temperature- and mechano-sensitive K2P channels.

KN-62 is a potent and specific Ca2+/calmodulin-dependent protein kinase II (CaMKII) inhibitor with Ki of 0.9 μM.

AC1-IN-1 is a selective inhibitor of adenylyl cyclase type 1 (AC1, IC50 = 0.54 µM).