canonical

ML204 is a novel potent antagonist that selectively modulates native TRPC4/C5 ion channels.

MCC950 (CP-456773) is a NLRP3 inflammasome inhibitor (IC50=7.5-8.1 nM). MCC950 can be used to treat inflammatory diseases, inflammation-related tumors and neurodegenerative diseases.

RU-SKI 43 is a potent and selective hedgehog acyltransferase (Hhat) inhibitor with an IC50 of 850 nM. It exhibits anticancer activity and is a potential treatment for lung adenocarcinomas. RU-SKI 43 reduces Gli-1 activation through smoothening-independent non-canonical signaling and inhibits Akt and mTOR pathway activity.

Kasugamycin hydrochloride hydrate (Ksg (hydrochloride hydrate))(Ksg) specifically inhibits translation initiation of canonical but not of leaderless messenger RNAs. Ksg inhibition is thought to occur by direct competition with initiator transfer RNA

Apramycin(Nebramycin II) is an aminoglycoside antibiotic used in veterinary medicine. IC50 value:Target: Apramycin stands out among aminoglycosides for its mechanism of action which is based on blocking translocation and its ability to bind also to the eukaryotic decoding site despite differences in key residues required for apramycin recognition by the bacterial target. The drug binds in the deep groove of the RNA which forms a continuously stacked helix comprising non-canonical C.A and G.A base pairs and a bulged-out adenine. The binding mode of apramycin at the human decoding-site RNA is distinct from aminoglycoside recognition of the bacterial target, suggesting a molecular basis for the actions of apramycin in eukaryotes and bacteria. [1]. Apramycin, From Wikipedia

FJ9 is an effective Wnt/β-catenin antagonist (Ki = 29 μM) that downregulates canonical Wnt signaling, inhibits HSC (hepatic stellate cell) activation, and reduces MeCP2 protein levels. FJ9 also disrupts the protein-protein interaction between Frz7 and the DVL PDZ domain, induces apoptosis in human cancer cell lines, and inhibits tumor growth in a mouse xenograft model.

Primordazine B is a small molecule that selectively ablates Primordial Germ Cells (PGCs). It functions by specifically inhibiting a process known as Poly(A)-tail Independent Non-canonical Translation (PAINT), without interfering with typical Poly(A) tail-dependent translation (PAT). Primordazine B serves as a valuable tool for investigating translational control mechanisms in specific physiological or pathological contexts, such as gene expression regulation during cell dormancy, viral infection, or stress conditions.

TRPC6-IN-1 is an inhibitor of the Transient Receptor Potential Canonical 6 Channel (TRPC6) (EC50: 4.66 μM).

Hyperforin dicyclohexylammonium salt is a transient receptor canonical 6 channel activator with antidepressant effect. It modulates Ca2+ levels by activating Ca2+-conducting non-selective canonical TRPC6 channels.

JW74 antagonizes LiCl-induced activation of the canonical Wnt signaling pathway (IC50: 420 nM).

Pyr3 is a selective transient receptor potential canonical channel 3 inhibitor. Pyr3 inhibits TRPC3-mediated Ca2+ influx in a dose-dependent manner(IC50 = 700 nM).

UAA crosslinker 1 hydrochloride is an amber codon used to incorporate non-canonical amino acids (ncAAs) into proteins in vivo by leveraging the promiscuous activity of specific wildtype and engineered aminoacyl-tRNA synthetases [1].

UAA crosslinker 1 hydrochloride is an Amber codon-activating agent used for incorporating non-canonical amino acids (ncAAs) into proteins in vivo by leveraging the promiscuous activity of specific wildtype and engineered aminoacyl-tRNA synthetases[1].

SU1261, an IKK inhibitor, exhibits Ki values of 10 nM for IKKα and 680 nM for IKKβ. It effectively inhibits non-canonical NF-κB signaling in U2OS osteosarcoma cells.

TRPC4/5-IN-3 (Compound 32) is an orally active inhibitor of transient receptor potential canonical channels 4 and 5 (TRPC4/5), with IC50 values of 3.6 nM and 5.5 nM, respectively. It inhibits the hERG channel with an IC50 of 6.5 µM. This compound demonstrates good metabolic stability in human, rat, and mouse liver microsomes. In mouse models, TRPC4/5-IN-3 exhibits antidepressant and anxiolytic effects and displays favorable pharmacokinetic properties, with an oral bioavailability of 87%.

3-(5-Methylfuran-2-yl)propanoic acid is a synthetic, non-proteinogenic amino acid characterized by a standard three-carbon propanoic acid backbone with an amino functional group (-NH2) located at the alpha-carbon (C2) and a distinctive 5-methylfuran-2-yl substituent at the beta-carbon (C3), where the furan ring—a five-membered aromatic heterocycle containing an oxygen atom—provides its unique structural and electronic properties, distinguishing it from canonical amino acids.

RS47 (Compound 1a) is a small molecule (Kd = 1.1 μM) that specifically targets RelB, selectively inhibiting the non-canonical NF-κB pathway by disrupting RelB binding to target DNA. It exhibits antitumour activity in vivo and in vitro and may be used in studies of colorectal cancer and B-cell lymphoma.

GDC-0152-acetamide is a pan-antagonist of apoptosis inhibiting proteins (IAPs). It induces the autoubiquitination and subsequent degradation of cIAP1/2, activates the non-canonical NF-κB pathway, and promotes the secretion of TNF-α, leading to apoptosis in tumor cells. GDC-0152-acetamide holds potential for research in ERα-positive breast cancer.

NIK-IN-3 is a potent, orally active inhibitor of NF-κB-inducing kinase (NIK) with an IC50 value of 5.2 nM. It effectively suppresses activation of the non-canonical NF-κB pathway and inhibits the secretion of pro-inflammatory cytokines, including TNF-α, IL-6, IL-1β, and the chemokine CXCL12. NIK-IN-3 demonstrates significant anti-inflammatory effects in LPS-induced sepsis and DSS-induced colitis mouse models. This compound is applicable in inflammation-related research, such as studies on colitis.

AM-0883 is an agonist of TRPC6 (transient receptor potential canonical 6) with a human TRPC6 EC50 of 46 nM. It is applicable for research in cardiac and renal diseases.

CXCR2-IN-3 is a CXCR2 inhibitor with an IC50 of 11.37 μM. It inhibits the CXCR2-Ca2+ signaling pathway, thereby blocking autophagic flux and promoting ROS-mediated apoptosis. Additionally, CXCR2-IN-3 suppresses the CXCR2-NLRP3 canonical pathway, reducing the expression of tumor-promoting markers. This compound induces autophagy-dependent cell death in polyploid giant cancer cells (PGCC) and is applicable in studies related to oral squamous cell carcinoma (OSCC).

GNE-5472 is a potent dual-function ERαPRRTAC degrader featuring an E3 ligase ligand that acts as a pan-IAP antagonist. By antagonizing cIAP1/2, GNE-5472 activates the non-canonical NF-κB pathway, resulting in a significant upregulation of TNFα expression. It inhibits the proliferation of breast cancer cells and induces apoptosis. GNE-5472 is applicable in breast cancer research.

ZD-1-186 is a non-degradable molecular glue that effectively inhibits MYC expression in diffuse large B-cell lymphoma cells and significantly induces the expression of CDKN1A (p21). This compound facilitates the binding of BCL6 to BRD9, a non-canonical BAF complex bromodomain protein involved in sustaining MYC transcriptional activity in certain lymphoma contexts. ZD-1-186 is applicable for research in targeted transcriptional reprogramming.

JW 67 is an inhibitor of canonical Wnt pathway signaling. JW 67 rapidly reduced active β-catenin with a subsequent downregulation of Wnt target genes, including AXIN2, SP5, and NKD1.