instability

Elimusertib (BAY-1895344) is a potent, highly selective, and orally available ATR inhibitor with an IC50 of 7 nM, demonstrating significant anti-tumor efficacy as a monotherapy and strong combination potential with targeted alpha therapy Radium-223 dichloride.

Terodiline is a seconal amine with anticholinergic and calcium antagonistic properties that blocks the hERG current (IC50: 375 nM).Terodiline is cardiotoxic and has been used in the study of disorders caused by urethral muscle instability.

Niraparib, also know as MK-4827, is an inhibitor of poly (ADP-ribose) polymerase (PARP) with potential antineoplastic activity. MK4827 inhibits PARP activity, enhancing the accumulation of DNA strand breaks and promoting genomic instability and apoptosis. The PARP family of proteins detect and repair single strand DNA breaks by the base-excision repair (BER) pathway.

KIF18A-IN-2 is an inhibitor of mitotic kinesin Kif18A with IC50 of 28 nM and can be used in studies about chromosomal instability-associated vulnerabilities.

Ascorbyl propyl hyaluronate is a perfect combination of hyaluronic acid and vitamin C, to overcome the instability of vitamin C, is to improve wrinkles, moisturize, calm the skin, whitening quality raw materials.

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.

2-CEES is a mustard gas analogue that only forms DNA monoadducts. It induces centromere amplification in both human and mouse cells and can lead to chromosome instability.

Tolterodine ((R)-(+)-Tolterodine) is a novel and selective muscarinic-type receptor (mAChR) antagonist used in the treatment of detrusor instability and overactive bladder syndrome.

Pamiparib is a highly potent and selective PARP inhibitor. BGB-290 selectively binds to PARP and prevents PARP-mediated repair of single-strand DNA breaks via the base-excision repair (BER) pathway. This enhances the accumulation of DNA strand breaks, pro

Niraparib hydrochloride (MK-4827 hydrochloride) is an inhibitor of poly (ADP-ribose) polymerase (PARP) with potential antineoplastic activity. By inhibiting PARP activity, niraparib hydrochloride increases DNA strand breaks, leading to genomic instability and apoptosis. The PARP family of proteins detects and repairs single-strand DNA breaks via the base-excision repair (BER) pathway.

5-Hydroxymethyl-2'-deoxycytidine is an oxidized derivative of 5-methyl-2'-deoxycytidine (5-mdC) in DNA, causing DNA damage reactions, chromosomal aberrations, replication fork damage, and loss of cell viability.5-Hydroxymethyl-2'-deoxycytidine is an oxidized derivative of 5-methyl-2'-deoxycytidine in DNA. Hydroxymethyl-2'-deoxycytidine replication fork instability is associated with the presence of poly(ADP-ribose) polymerase 1 (PARP1) on chromatin.

Perivine (Perivin) may resolve the instability of the retinoblastoma-associated proteins (RbAp48) complex and thus be used in Alzheimer's disease therapy. Perivine, vobasine, coronaridine and dichomine show hypotensive and muscle relaxant activity.

LasR-IN-3, a chemical compound, acts as an inhibitor of LasR in Pseudomonas aeruginosa. It induces structural instability in LasR and causes complete dissociation of its functioning dimeric form [1].

Antitubercular agent-13 (Compound 3d) is an antitubercular compound with MIC values of 0.007 μg mL against MTB H37Rv and 1.851 μg mL against MDR-MTB 16833, respectively, and exhibits metabolic instability [1].

AGG-523 is an aggrecanase specific inhibitor that has been shown to attenuate increases in synovial fluid ARG-aggrecan levels following surgically-induced joint instability in the rat MT model. Pharmacologic inhibition of aggrecanase activity in humans using AGG-523 may be an effective treatment for slowing cartilage degradation following joint injury.

Pamiparib, also known as BGB-290, is a highly potent and selective PARP inhibitor with favorable drug metabolism and pharmacokinetic properties. BGB-290 selectively binds to PARP and prevents PARP-mediated repair of single-strand DNA breaks via the base-excision repair (BER) pathway. This enhances the accumulation of DNA strand breaks, promotes genomic instability, and eventually leads to apoptosis. BGB-290 may both potentiate the cytotoxicity of DNA-damaging agents and reverse tumor cell chemo- and radioresistance.

Streptonigrin is an aminoquinone antitumor and antibacterial antibiotic produced by Streptomyces flocculus. Streptonigrin inhibits β-Catenin Tcf signaling and shows cytotoxicity in β-catenin-activated cells. Streptonigrin induces delayed chromosomal instability involving interstitial telomeric sequences in Chinese hamster ovary cells. Note: Streptonigrin from natural resource is (-)-rotation, has CAS#3930-19-6 and is a R-isomer.

2-Arachidonoylglycerol (2-AG) is identified as a more potent endogenous cannabinoid ligand compared to its analogue, 1-Arachidonoylglycerol (1-AG), exhibiting 10 to 100 times the ligand binding affinity and agonist activity at the CB1 receptor, thus making it a natural ligand. However, 2-AG's chemical instability leads to rapid isomerization to 1-AG (also referred to as 1(3)-AG) both in vitro and in vivo. This isomerization process, where 1-AG becomes a frequent contaminant in synthetic 1-AG preparations, significantly decreases their cannabinergic potency. Furthermore, 1-AG is characterized as a weak CB1 receptor agonist with potential for other pharmacological effects.

GSK_WRN2 is a potent, selective covalent inhibitor of the WRN helicase, which targets replication stress caused by the amplification of DNA (TA)n dinucleotide repeats. It can be utilized in research focusing on microsatellite instability (MSI) cancers.

PIP-199 is a selective inhibitor of the RMI (RecQ-mediated genome instability protein) core complex MM2 interaction, with an IC50 of 36 μM. PIP-199 can be used to study DNA crosslink repair mechanisms and could serve as a sensitizing agent for chemoresistant tumors [1].

10-Deacetylcephalomannin exhibits activity against PS leukemia in vivo; however, its instability leads to an equilibrium mixture with its cytotoxic C-7 epimer. Additionally, 10-Deacetylcephalomannine demonstrates growth inhibitory effects on human cancer cell lines, including cervical HeLa adenocarcinoma.

Pregeijerene is a C12 terpene. This compound acts as a plant volatile induced by herbivores, playing a crucial role in signaling between plants and nematodes, particularly notable for its thermal instability.

Chlorophyll b is an orally active tetrapyrrole derivative and pigment that can be obtained from photosynthetic organisms such as plants and algae. It acts as a hydrogen donor and enhances glutathione levels. Chlorophyll b possesses antioxidant activity and functionally replaces chlorophyll a in photosystem II to participate in photosynthesis. It reduces DNA damage, chromosome instability, and oxidative stress induced by Cisplatin (HY-17394). Chlorophyll b is primarily used in research on plant photosynthesis mechanisms.