dsb

Pyridostatin (RR82) is a synthetic small-molecule stabilizer of G-quadruplexes, a secondary structure of DNA that usually exists in the end of the chromosome or the telomeres.

Pyridostatin Trifluoroacetate Salt is a G-quadruplexe stabilizer with Kd of 490 nM in a cell-free assay, which targets a series of proto-oncogenes including c-kit, K-ras and Bcl-2.

PFM01 is an inhibitor of MRE11 endonuclease. PFM01 can regulate double-strand break repair (DSBR) by nonhomologous end-joining (NHEJ) versus homologous recombination (HR).

NSC 617145 (NSC617145) is an inhibitor of WRN helicase that inhibits the ATPase, but not exonuclease, activity of WRN helicase in a concentration-dependent manner.

IC 86621 is a selective and reversible ATP-competitive inhibitor of DNA-PK with an IC50 of 120 nM. IC 86621 increases DNA double-strand break(DSB)-induced antitumor activity with an EC50 of 68 µM for DNA-PK mediated cellular DSB repair.

NDSB-211 is a surfactant with small hydrophobic ends and mildly solubilizes proteins for protein extraction and analysis.

NDSB-256 (3-(Benzyldimethylammonio)propane-1-sulfonate) is a non-detergent sulfobetaine that prevents protein aggregation and increases the isomerization rate in a concentration-dependent manner.

NDSB-201 is a pyridine derivative with sulfonate groups and an amphoteric surfactant that prevents protein aggregation and precipitation without causing protein denaturation, commonly used as a buffer in biochemical experiments.

EcDsbB-IN-9 is a specific EcDsbB inhibitor, targeting disulfide bond forming enzyme DsbB of Gram-negative bacteria.

EcDsbB-IN-12 (4,5-dichloro-2-[(2-chlorophenyl)methyl]pyridazin-3-one) targets disulfide bond forming enzyme,and is a novel potent specific inhibitor of EcDsbB.

NDSB-195 is a useful organic compound for research related to life sciences. The catalog number is TF0078 and the CAS number is 160255-06-1.

NDSB-221 is a useful organic compound for research related to life sciences. The catalog number is TF0121 and the CAS number is 160788-56-7.

NDSB 256-4T is a non-detergent sulfobetaine compound. It inhibits protein aggregation and aids in protein folding by interacting with early folding intermediates.

Gimeracil (Gimestat) is a competitive, reversible inhibitor of dihydropyrimidine dehydrogenase.

DMNB (6-Nitroveratraldehyde) is DNA-dependent protein kinase (DNA-PK) inhibitor with IC50 of 15 μM, an enzyme involved in the non-homologous end-joining (NHEJ) pathway of double-stranded DNA break (DSB) repair in human cells.

ERK1/2 inhibitor 11 (compound L6) is a dual inhibitor of ERK1/2 that promotes the accumulation of DSBs and the degradation of ERK1/2 expression. This compound decreases BCL-2 levels and induces DNA damage by inhibiting PARP and ERK1/2. Additionally, ERK1/2 inhibitor 11 activates caspase 3 to induce apoptosis.

CDK9/EZH2-IN-1 is a dual-target inhibitor of CDK9 and EZH2 with IC50 values of 83.9 nM and 108.6 nM, respectively. It induces apoptosis and causes DNA double-strand breaks (DSB). Additionally, CDK9/EZH2-IN-1 inhibits the proliferation of MKN45, MDA-MB-453, and SW620 cancer cells, with respective IC50 values of 136.3 nM, 171.3 nM, and 315.7 nM.

HDAC6-IN-63 (Compound 7) is an orally active inhibitor of HDAC6 with an IC50 of 145 nM. It suppresses the expression of Sp1 and RAD51, inducing caspase-dependent apoptosis. HDAC6-IN-63 exhibits antitumor activity and enhances the sensitivity of Etoposide and Gemcitabine by inhibiting homologous recombination and non-homologous end joining (NHEJ) pathways involved in DNA double-strand break (DSB) repair, promoting synergistic cell death in NSCLC cells. This compound is applicable for chemotherapy research in cancers such as NSCLC.

Topoisomerase II inhibitor 6 (Compound 5), a tryptanthrin derivative, is a potent and selective topoisomerase II inhibitor that blocks the CCRF-CEM cell cycle in the G2 phase and induces DNA double-strand breaks (DSB). It exhibits antiproliferative activity on various tumor cell lines and has potential for cancer research [1].

Simmiparib (SMOCL-9112) is a novel and potent PARP1 and PARP2 inhibitor, a derivative of Olaparib.Simmiparib induces DNA double-strand breaks (DSBs) and cell cycle arrest in homologous recombination repair (HR)-deficient cells, thereby contributing to apoptosis.Simmiparib has been used for study Parkinson's disease, Alzheimer's disease, breast cancer, and melanoma.

CBP-93872 is a G2 checkpoint inhibitor. CBP-93872 specifically abrogates the DNA double-stranded break (DSB)-induced G2 checkpoint through inhibiting maintenance. CBP-93872 is an inhibitor of maintenance of the DSB-specific G2 checkpoint and thus might be a strong candidate as the basis for a drug that specifically sensitizes p53-mutated cancer cells to DSB-inducing DNA damage therapy.

Amonafide L-malate is the malate salt of amonafide, an imide derivative of naphthalic acid, with potential antineoplastic activity. Amonafide intercalates into DNA and inhibits topoisomerase II, resulting in DNA double-strand breaks (DSB) and inhibition of DNA replication and RNA synthesis.

NHEJ Inhibitor-1 (Compound C2), a trifunctional Pt(II) complex, mitigates non-homologous end joining (NHEJ)/homologous recombination (HR)-related double strand break (DSB) repairs, combating Cisplatin resistance in non-small cell lung cancer (NSCLC). It achieves this by inhibiting the damage repair proteins Ku70 and Rad51, thus re-sensitizing tumors to Cisplatin. Additionally, this compound prompts the generation of reactive oxygen species (ROS) and reduces mitochondrial membrane potential (MMP) [1].

DiPT-4, a dual TOP1/PARP1 inhibitor, effectively induces DNA double-strand breaks (DSBs), cell cycle arrest, and apoptosis in cancer cells, with potential to circumvent drug resistance [1].