genomic

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.

Glecaprevir (ABT-493) is a small-molecule inhibitor that functions as an HCV NS3/4A protease inhibitor (IC50=3.5–11.3 nM) and also inhibits SARS-CoV-2 3CLpro (IC50=4.09 μM). It possesses oral bioavailability and antiviral activity, and is used for the treatment of hepatitis C as well as potential anti-coronavirus research.

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.

Isothiafludine (NZ-4) is an orally active anti-HBV compound that acts by blocking the encapsulation of pre-genomic RNA (pgRNA) and interfering with nucleosome capsid assembly, and is used in the study of HBV infections.

GSK4418959 (IDE275) is a non-covalent, reversible, selective, and orally active inhibitor of the Werner syndrome helicase (WRN helicase). GSK4418959 inhibits both ATPase and DNA unwinding activities of WRN helicase in an ATP-competitive manner. GSK4418959 is a valuable chemical tool for the study of microsatellite instability-high (MSI-H) cancers, where WRN helicase plays an essential role in maintaining genomic stability.

ZIM, a norbornene derivative of 4-Aminoantipyrine, effectively induces DNA damage, leading to genomic and chromosomal alterations, cell death, and phagocytosis activation. Its properties highlight its potential as a chemotherapeutic agent in cancer research.

GLP-26 disrupts the encapsidation of pre-genomic RNA, causes nucleocapsid disassembly and reduces cccDNA pools. GLP-26 is a HBV capsid assembly modulators (CAM), inhibits HBV DNA replication in Hep AD38 system (IC50=3 nM), and reduces cccDNA by >90% at 1

TEI-9647 is a 1α,25-dihydroxy vitamin D3-26,23-lactone (1α,25-lactone) analog and is an effective VDR/vitamin D-responsive element (DRE)-mediated genomic actions antagonist.

PF-3837 is an inhibitor of the Mps1 kinase, with a Ki value of 0.33 nM and an IC50 value of 5.5 nM. It disrupts cell cycle checkpoints by inhibiting the catalytic activity of Mps1, thereby reducing genomic stability and leading to cancer cell apoptosis (Apoptosis). PF-3837 is utilized in the study of breast cancer.

5-Methylcytosine hydrochloride plays a critical role in regulating gene expression, promoting genomic imprinting, and inhibiting transposon factors. It is also closely associated with translation fidelity and tRNA recognition.

SGK1-IN-3 hydrochloride (compound 3a) is an efficacious, orally bioavailable SGK1 inhibitor. The serine/threonine kinase SGK1 acts as an activator of the β-catenin pathway and strongly stimulates cartilage degradation, being upregulated under genomic control in diseased osteoarthritic cartilage. SGK1-IN-3 hydrochloride holds potential for osteoarthritis research.

Anti-MRSA agent 28 is an antimicrobial compound effective against multidrug-resistant Gram-positive strains, with a minimum inhibitory concentration (MIC) of 0.06-0.125 μg/mL. It targets DNA polymerase IIIC to reduce the amount of genomic DNA, achieving an IC50 of 3.80 μg/mL. Anti-MRSA agent 28 exhibits potent antibacterial activity and aids in reducing inflammation, making it suitable for use against Gram-positive strains and in treating infectious diseases.

MU262 is a structurally novel polycyclic heterocyclic small-molecule compound and a MUS81 inhibitor with an IC₅₀ value of 0.87 μM, which directly inhibits MUS81 catalytic activity through non-interfering DNA binding, inducing genomic instability in tumor cells and specifically inhibiting the HR/BIR repair pathways. MU262 can serve as a chemical biology tool for studying MUS81 function and as a lead compound for developing anticancer therapies that exploit DNA repair defects in cancer cells.

AChE/BuChE-IN-7 is a dual-action inhibitor with an IC50 value of 0.15 μM for acetylcholinesterase (AChE) and 0.7 μM for butyrylcholinesterase (BuChE), with a selectivity index (SI) of 4.7. It exhibits antioxidant activity, reducing H2O2-induced cytotoxicity, and shows genomic stability and extended systemic bioavailability. AChE/BuChE-IN-7 is applicable for research into neurological disorders, such as Alzheimer's disease.

JPC0661 is a direct and allosteric inhibitor of ΔFOSB. It inhibits the binding of ΔFOSB/JUND and ΔFOSB to DNA with a micromolar IC50 value (9-52 μM), and directly suppresses ΔFOSB-mediated transcription in vitro with an IC50 of 0.82 μM. In vivo, JPC0661 notably reduces the occupancy of ΔFOSB at genomic AP1 sites. JPC0661 disrupts the formation of the ΔFOSB/JUND-DNA complex by binding to a novel groove outside the ΔFOSBDNA binding cleft. JPC0661 is applicable in Alzheimer's disease research.

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.

HM-cytosine (5hmC) is a naturally occurring component of mammalian genomic DNA and is thought to be the sixth base of DNA [1]. HM-cytosine is an intermediate metabolite for demethylation of active DNA [2]. HM-cytosine is an ep

The methylation of lysine residues on histones plays a central role in determining euchromatin structure and gene expression. The histone methyltransferase (HMTase) G9a can mono- or dimethylate lysine 9 on histone 3 (H3), contributing to early embryogenesis, genomic imprinting, and lymphocyte development. BIX01294 (hydrochloride hydrate) is a selective inhibitor of G9a HMTase (IC50 = 1.7 μM). It less effectively inhibits the HMTase G9a-like protein (GLP; IC50 = 38 μM) and has no effect on other known HMTases. BIX01294 has been used in combination with the calcium channel activator BayK8644 to facilitate the generation of induced pluripotent stem cells from somatic cells in vitro.

TEI-9648, an analogue of Vitamin D3 Lactone, acts as a potent and specific antagonist to the vitamin D receptor (VDR). This compound effectively blocks the genomic actions mediated by VDR and the Vitamin D responsive element (VDRE) of 1α,25(OH)2D3. Furthermore, TEI-9648 prevents the differentiation of HL-60 cells induced by 1α,25(OH)2D3, indicating its utility in bone metabolism studies[1][2].

XMD16-5 is a TNK2 inhibitor. TNK2 genomic amplification has been associated with late-stage or metastatic lung and prostate Ys. Overexpression of TNK2 promoted metastasis in a mouse model of breast Y. TNK2 signaling is disrupted in breast, prostate and ga

LL-37 is a cationic and α-helical antimicrobial peptide expressed in human bone marrow, testis, granulocytes, and gingival epithelium and is upregulated in psoriatic lesions. It inhibits growth of Gram-positive E. coli D21 and Gram-negative B. megatarium in a concentration-dependent manner and LL-37 expression is induced in A549 epithelial cells, alveolar macrophages, neutrophils, and monocyte-derived macrophages following M. tuberculosis infection. LL-37 binds sheep erythrocytes coated with S. minnesota Re-LPS and induces agglutination with a minimal agglutinating concentration (MAC) of 12.1 μg/ml. It is a chemoattractant for, and can induce calcium mobilization in, human monocytes, neutrophils, and T cells that naturally express formyl peptide receptor-like 1 (FPRL1) and FPRL1-transfected HEK293 cells. LL-37 (10-15 μM) pretreatment of dengue virus type 2 (DENV-2) reduces its infectivity as well as levels of viral genomic RNA and NS1 antigen. In vivo, LL-37 inhibits cecal ligation and puncture-induced caspase-1 activation and pyroptosis of peritoneal macrophages, reduces levels of the inflammatory cytokines IL-1β, IL-6, and TNF-α, and improves survival in polybacterial septic mice.

Anti-MRSA agent 2 (compound 14) is a potent inhibitor of methicillin-resistant Staphylococcus aureus (MRSA) (MIC: 0.098 μg/ml), exhibiting relatively low toxicity to normal cells. It strongly disrupts bacterial membranes and effectively binds to bacterial genomic DNA.

Anti-MRSA agent 3 inhibits methicillin-resistant Staphylococcus aureus (MRSA) activity significantly (MIC: 0.098 μg/ml) with low toxicity to normal cells. anti-MRSA agent 3 has a high binding affinity for bacterial genomic DNA and a strong ability to disrupt bacterial cell walls and membranes.