rna-binding

PTBP1-RNA-binding inhibitor P6 TFA (PTBP1 α3-helix derived peptide P6 TFA) is a specific stapled peptide inhibitor of the splicing factor PTBP1, which is used to inhibit RNA alternative splicing events regulated by PTBP1. PTBP1-RNA-binding inhibitor P6 TFA exerts its effects by binding to the RNA recognition motif of PTBP1.

Ro 08-2750 is a non-peptide, reversible nerve growth factor (NGF) inhibitor that binds to NGF with an IC50 of approximately 1 µM. It is also a selective MSI RNA-binding activity inhibitor, exhibiting an IC50 of 2.7 μM. Additionally, Ro 08-2750 selectively inhibits NGF binding to p75NTR over TRKA.

Clemizole, an H1 histamine receptor antagonist, inhibits NS4B's RNA binding and hepatitis C virus (HCV) replication.

Clemizole hydrochloride is an antagonist for H1 histamine receptor. According to the research, Clemizole hydrochloride can inhibit hepatitis C virus (HCV) replication and NS4B's RNA binding.

Tat-CIRP, a peptide inhibitor, impedes the protein-protein interaction between myeloid differentiation 2 (MD-2), also known as lymphocyte antigen 96 (LY96), and cold-inducible RNA binding protein (CIRP) by binding to MD-2. This disrupts the MD-2 and CIRP interaction as confirmed in co-immunoprecipitation assays. Notably, in vivo studies reveal that Tat-CIRP, at dosages of 10 and 20 mg/kg, significantly reduces infarct volume in both a mouse model of middle cerebral artery occlusion (MCAO) and a rhesus monkey model of thrombosis-induced stroke. Additionally, it improves motor function, evidenced by decreased time to manipulate and withdraw food with the affected arm in the primate model.

Suramin Sodium Salt (BAY-205) is a sodium salt form of suramin, a polysulphonated naphthylurea with potential antineoplastic activity. Suramin blocks the binding of various growth factors, including insulin-like growth factor I (IGF-I), epidermal growth factor (EGF), platelet-derived growth factor (PDGF), and tumor growth factor-beta (TGF-beta), to their receptors, thereby inhibiting endothelial cell proliferation and migration. This agent also inhibits vascular endothelial growth factor (VEGF)- and basic fibroblast growth factor (bFGF)-induced angiogenesis; retroviral reverse transcriptase; uncoupling of G-proteins from receptors; topoisomerases; cellular folate transport; and steroidogenesis.

Puromycin dihydrochloride (CL13900 dihydrochloride) is a cinnamamide adenosine antibiotic and an inhibitor of protein synthesis. Puromycin dihydrochloride inhibits protein synthesis by binding to RNA and has antitumor and antitrypanosomal activity.

Thailanstatin A is an ultra-potent inhibitor of eukaryotic RNA splicing (IC50 = 650 nM). It inhibits multiple cancer cell lines via non-covalent binding to the SF3b subunit of the U2 snRNA subcomplex of the spliceosome, displaying low-nM to sub-nM IC50s. Thailanstatin A, as a payload for ADCs, is conjugated to the lysines on trastuzumab, yielding linker-less ADC.

AOH1996 belongs to small molecule inhibitors and is a PCNA ligand targeting transcription-replication conflicts, with oral activity, metabolic stability, and tumor selectivity. This compound induces transcription-dependent DNA double-strand breaks and apoptosis, and is used for antitumor therapy.

MY-1B is a covalent inhibitor and an inhibitor of RNA methyltransferase NSUN2 (IC50 = 1.3 μM), featuring stereoselectivity, covalent binding to C271 of NSUN2, and the ability to target PSME1, disrupt proteasome regulatory complexes, and downregulate presentation of specific MHC-I subtypes.

Galidesivir hydrochloride is an inhibitor of viral RNA-dependent RNA polymerase (RdRp). It inhibits SARS-CoV-2 by tightly binding to its RdRp.

Setrobuvir (ANA-598) is an orally active, highly selective non-nucleoside HCV NS5B polymerase inhibitor that inhibits new RNA synthesis and primer extension, with IC₅₀ values ranging from 4 to 5 nM. Setrobuvir exhibits high binding affinity for SARS-CoV-2 RdRp and induces inhibition of RdRp. Setrobuvir is suitable for Antiviral drugs studies.

Carboxy-pyridostatin is a carboxyl-modified derivative of pyridostatin, a classic G-quadruplex ligand, capable of selectively binding to and stabilizing G-quadruplex structures, thereby influencing the DNA conformation in regions related to telomeres and gene regulation. Carboxy-pyridostatin exhibits high molecular specificity for RNA on DNA G4s and can downregulate the ATF-5 protein. Carboxy-pyridostatin inhibits cell proliferation and impedes the formation of stress granules (SGs).

SMN-C2 is a selective regulator of SMN2 gene splicing, a risdiplam analogue, a selective RNA-binding ligand that regulates pre-mRNA splicing and acts by binding to SMN2 pre-mRNA.SMN-C2 has the potential to be used in the study of spinal muscular atrophy (SMA).

Tedizolid (DA-7157)is a novel oxazolidinone-class antibiotic that inhibits bacterial protein synthesis by binding to the 23S ribosomal RNA of the 50S subunit of the ribosome.

EDC hydrochloride (EDC-HCl Crosslinker) is a water-soluble carbodiimide compound. EDC hydrochloride, as a condensing agent, forms peptide bonds through the condensation reaction of carboxyl and amino groups and can be used to synthesize peptides with specific sequences and functions. EDC hydrochloride can covalently bind haptens to carrier proteins to form immune antigens, which are used in vaccine research. EDC hydrochloride can react with the 5 'phosphate group of nucleic acids and is used for the labeling of DNA and RNA. EDC hydrochloride can cross-link proteins with nucleic acids and is used to prepare immune cross-links. EDC hydrochloride, as a crosslinking agent, connects the amine-reactive NHS ester of biomolecules with the carboxyl group, which can be used for protein coupling to create hybrid molecules with new properties and functions.

Lin28 1632 is an inhibitor of RNA binding protein Lin28. It promotes mESC differentiation. Lin281632 is also bromodomain inhibitor.

L-Histidine benzyl ester bistosylate may serve as an activator for HutP, an RNA-binding protein.

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

Erythromycin thiocyanate is a macrolide antibiotic produced by actinomycetes with a broad antibacterial spectrum. It inhibits RNA-dependent protein synthesis by binding to the bacterial 50S ribosomal subunit and blocking transpeptidation and translocation, without interfering with nucleic acid synthesis. It has also shown antitumor and neuroprotective activities in multiple studies.

Lefamulin acetate (BC-3781 acetate) (formally BC-3781 acetate) is a novel pleuromutilin antibiotic and is the first to be used for the systemic treatment of bacterial infections in humans. Lefamulin acetate (BC-3781 acetate) inhibits protein synthesis by binding to the peptidyl transferase center of the 50S bacterial ribosome, preventing the binding of transfer RNA for peptide transfer. Lefamulin acetate (BC-3781 acetate) is an orally active antibiotic for community-acquired bacterial pneumonia (CABP) treatment.

Hycanthone (Etrenol(mesylate)) is a potent drug of antischistosomal. Hycanthone is a DNA intercalator that inhibits RNA synthesis and DNA topoisomerases I and II. Hycanthone inhibits nucleic acid biosynthesis and inhibits APE1 via direct protein binding(KD: 10 nM).

Streptolydigin inhibits RNA synthesis by binding to RNA polymerase and does not inhibit eukaryotic RNA polymerases. Streptolydigin is a 3-acetyltetramic acid antibiotic and a potent bacterial RNA polymerase inhibitor (Ki: 18 μM and a Kd: 15 μM).

Puromycin (NSC-3055) is an antibiotic protein synthesis inhibitor. It inhibits protein synthesis by binding to RNA. It also serves as an anticancer drug by suppressing the growth and metastasis in esophagus cancer cells by Akt phosphorylation. It is an antineoplastic and antitrypanosomal agent and is used in research as an inhibitor of protein synthesis.