modification

N-Succinimidyl-S-acetylthioacetate (SATA) is a protein modification agent that introduces thiol-groups into protein molecules and adds sulfhydryl groups in a protected form to proteins and other amine-containing molecules for later reaction with sulfhydryl reactive crosslinkers such as Sulfo-SMCC, Sulfo-MBS, etc.

Cemdisiran, an investigational N-acetylgalactosamine-conjugated RNAi (RNA interference) agent with terminal sugar modification, is a small interfering RNA (siRNA) designed to specifically target and suppress the C5 mRNA, thereby reducing the liver's production of the complement component C5 [1].

Triparanol (NSC-65345) interferes with posttranslational modification of Hedgehog signaling molecules as well as the sterol sensing domain of its receptor PTCH1, leading to down-regulation of Hedgehog signaling. Triparanol suppresses human tumor growth and is an antilipemic agent with high ophthalmic toxicity.

VRT-532 (CFpot-532) is an effective modulator of CFTR and is commonly used in studies of cystic fibrosis (CF) caused by CFTR defects. Modification of CFTR by this small molecule modulator can increase arylsulfatase B (ARSB), which is necessary to reduce the accumulation of sulphate glycosaminosaccharide (gag), thus reducing the accumulation of 4-chondroitin sulfate in cystic fibrosis.

Chlorpropamide (Diabinese) is a sulfonylurea hypoglycemic agent used in the treatment of non-insulin-dependent diabetes mellitus not responding to dietary modification.

Clindamycin Phosphate is the phosphate salt form of clindamycin, a semi-synthetic, chlorinated broad-spectrum antibiotic produced by chemical modification of lincomycin. Clindamycin phosphate (Clindamycin 2-dihydrogen phosphate) is used in topical preparations.

5-Methylcytosine is a methylated nucleotide base found in eukaryotic DNA. It is an epigenetic modification formed by the action of DNA methyltransferases.

1-Thioglycerol (alpha-Thioglycerol) is an antioxidant thioglycerol that scavenges free radicals and reduces oxidative stress as a media component, and is used as a matrix in fast atom bombardment mass spectrometry (FAB-MS) and liquid secondary ion mass spectrometry (LSIMS).

Tetradecylthioacetic acid is a synthetic fatty acid with a sulfur substitution in the β-position. This modification renders TTA unable to undergo complete β-oxidation and increases its biological activity, including activation of peroxisome proliferator activated receptors (PPARs) with preference for PPARα.

T6A (N6-Threonylcarbamoyladenosine) is a ubiquitously conserved nucleoside, which is essential for modification. T6A is found in the tRNA responsible for transporting the ANN codon.

N6-Methyladenosine is a methylated adenine residue, glycoside is an endogenous uridine product of transfer RNA degradation. It is the most prevalent internal modification of messenger RNA present in all higher eukaryotes and can modify viral RNA with antiviral activity.

Fmoc-Gly-Thr(psi(Me,Me)pro)-OH is a polypeptide composed of glycine and threonine containing a (psi(Me,Me)pro) modification.

2-Hexylthiophene, a weakly basic heteroaromatic compound, can enhance the molar absorption coefficient of ruthenium sensitizers by undergoing modification.

NCC007 is a novel CKIα and CKIδ dual inhibitors by structural modification of N9 and C2 position of longdaysin.

EN6-mediated ATP6V1A modification decouples the v-ATPase from the Rags, leading to inhibition of mTORC1 signaling, increased lysosomal acidification and activation of autophagy. EN6 clears TDP-43 aggregates, a causative agent in frontotemporal dementia, in a lysosome-dependent manner. EN6 is a small-molecule in vivo activator of autophagy that covalently targets cysteine 277 in the ATP6V1A subunit of the lysosomal the vacuolar H+ ATPase (v-ATPase).

IDH1 Inhibitor 2 (compound 13) is a potent IDH1 inhibitor through direct covalent modification of His315, with an IC50 of 110 nM.

3-Methyluridine is a modified nucleoside of cellular RNA.

BPK-29, a ligand specifically targeting the atypical orphan nuclear receptor NR0B1, disrupts its protein interactions through covalent modification at C274, thereby impairing the anchorage-independent growth of KEAP1-mutant cancer cells.

LS2265, a fenofibrate derivative with a taurine modification, effectively induces the proliferation of peroxisomes in rat liver cells.

AA147 (ATF6-activator-147) is a small molecule endoplasmic reticulum (ER) proteostasis regulator. The selectively activates ATF6 arm of the unfolded protein response (UPR) .It acts as a prodrug that preferentially triggers ATF6 signaling through a mechanism involving localized metabolic activation and selective covalent modification of ER resident proteins that regulate ATF6 activity.

Leptomycin B (LMB) is a potent inhibitor of the nuclear export of proteins and is a potent antifungal antibiotic blocking the eukaryotic cell cycle. Leptomycin B inactivates CRM1 exportin 1 by covalent modification at a cysteine residue.

Leptomycin B (GMP) refers to the GMP grade reagents of Leptomycin B. Leptomycin B (LMB) is a potent inhibitor of the nuclear export of proteins and is a potent antifungal antibiotic blocking the eukaryotic cell cycle. Leptomycin B inactivates CRM1 exportin 1 by covalent modification at a cysteine residue.

KB02-JQ1 is a potent and specific proteolysis targeting chimera (PROTAC) that specifically degrades BRD4, acting as a molecular glue. It does not degrade BRD2 or BRD3. The mechanism of action involves covalent modification of the E3 ligase DCAF16, thereby promoting BRD4 degradation. Importantly, KB02-JQ1 demonstrates enhanced stability and durability in facilitating protein degradation within biological systems. The compound forms a complex with the ubiquitin E3 ligase ligand KB02 through a linker, resulting in the formation of KB02-JQ1[1].

5-Methyl-5,6-dihydrouridine, a minor constituent in the chromosomal RNA of the rat ascites tumor, can be utilized for nucleic acid modification.