genomic

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.

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.

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].

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

Anti-MRSA agent 2 (compound 14) is a good inhibitor of methicillin-resistant Staphylococcus aureus (MRSA) (MIC: 0.098 μg/ml) with relatively low toxicity to normal cells. anti-MRSA agent 2 is a strong disruptor of bacterial membranes and has a good ability to bind to bacterial genomic DNA.

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

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.

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

AB-506 is a compound that serves as an orally administered inhibitor specifically targeting the hepatitis B virus (HBV) core protein to obstruct HBV replication. It achieves this by binding to the HBV core protein, accelerating capsid assembly, and hindering the encapsidation of HBV pre-genomic RNA (pgRNA). Consequently, AB-506 is utilized in the study of chronic hepatitis B (CHB).

Niraparib hydrochloride (MK-4827 hydrochloride) is an inhibitor of poly (ADP-ribose) polymerase (PARP) with potential antineoplastic activity. Niraparib hydrochloride 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.

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.

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

SGK1-IN-3 is a potent, orally active SGK1 inhibitor. Among them, the serine/threonine kinase SGK1, an activator of the β-linked protein pathway and a powerful stimulator of cartilage degradation, has been found to be upregulated under genomic control in diseased osteoarthritic cartilage. SGK1-IN-3 shows research potential in osteoarthritis.

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.

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.

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.

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.

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