DNA Damage/DNA Repair

<p>Palifosfamide lysine (ZIO-201) stable, effective vs. sarcomas in vitro. IC50: 2.25-6.75 μM, except OS222 at 31.5 μM.</p>

<p>360A is a stabilizing G-Quadruplex ligand, and also inhibits telomerase activity for telomerase in TRAP-G4 assay(IC50 : 300 nM).</p>

<p>Lomeguatrib (PaTrin-2), a modified guanine base, inhibits the activity of DNA repair protein O(6)-alkylguanine-DNA alkyltransferase (MGMT) .</p>

<p>Nexturastat A is an effective and specific HDAC6 inhibitor (IC50: 5 nM). Its selectivity is &gt;190-fold than other HDACs.</p>

<p>ETP-45658 (ETP45658) is a PI 3-kinase inhibitor (IC50 values are 22, 30, 129 and 710 nM for PI 3-Kα, PI 3-Kδ, PI 3-Kβ and PI 3-Kγ respectively).</p>

<p>Dactolisib (BEZ235) is an orally bioavailable inhibitor of PI3K and mTOR (IC50s: 4 nM/5 nM/7 nM/75 nM, and 20.7 nM for p110α/p110γ/p110δ/p110β and mTOR).</p>

<p>Pimelic diphenylamide 106 (RGFA-8) is a slow, tight-binding inhibitor of class I HDAC, showing no activity against class II HDACs.</p>

<p>TMP269: Class IIa HDAC inhibitor; HDAC4 IC50=157 nM, HDAC5 IC50=97 nM, HDAC7 IC50=43 nM, HDAC9 IC50=23 nM.</p>

<p>Amonafide (NSC-308847, AS1413) causes DNA breaks via topoisomerase II, not topoisomerase I.</p>

<p>A-96649 is a new-type and effective inhibitor. The Ki of A-966492 for PARP1 and PARP2 is 1 nM and 1.5 nM, respectively.</p>

<p>6-azathymine inhibits D-3-aminoisobutyrate-pyruvate aminotransferase; 6-azauracil competes with beta-alanine, uncompetitive with pyruvic acid, Ki ~8.9 mM.</p>

<p>ACY-775 is an effective and specific inhibitor of HDAC6 (IC50: 7.5 nM).</p>

<p>Satraplatin (BMS182751) is an orally available antineoplastic platinum(IV) complex.Satraplatin has a favorable toxicity profile and appears to have clinical</p>

<p>CRT0044876 (7-NO2-ICA) is a potent and selective APE1 inhibitor with IC50 of ~3 μM.</p>

<p>AZD1390: Potent ATM inhibitor (IC50: 0.78 nM), &gt;10,000-fold selectivity vs. PIKK enzymes.</p>

<p>RGFP966 is an HDAC3 inhibitor (IC50: 0.08 μM) and does not affect other HDACs at concentrations up to 15 μM.</p>

<p>RG2833 (RGFP109) (RGFP109), a brain-penetrant HDAC inhibitor, is with IC50 of 60 nM and 50 nM for HDAC1 and HDAC3, respectively.</p>

<p>3,4-Dicaffeoylquinic acid (Isochlorogenic acid B) has antioxidant activity.</p>

<p>Seclidemstat (SP-2577) is an effective LSD1 inhibitor, with a mean IC50 of 127 nM.</p>

<p>Veliparib dihydrochloride (ABT-888 dihydrochloride) is a potent inhibitor of PARP1 and PARP2 with Ki of 5.2 nM and 2.9 nM in cell-free assays, respectively.</p>

<p>Prexasertib dihydrochloride (LY2606368) inhibits CHK1 (Ki: 0.9 nM); IC50: CHK2 8 nM, RSK 9 nM.</p>

<p>6-Thioguanine (2-Amino-6-purinethiol) is an antineoplastic compound which also has antimetabolite action. The drug is used in the therapy of acute leukemia.</p>

<p>SIS17: Potent, selective HDAC11 inhibitor (IC50: 0.83 μM), blocks serine hydroxymethyl transferase 2 demyristoylation, spares other HDACs.</p>

<p>CC-115 is a inhibitor of mTOR/DNA-PK (IC50= 21/ 13 nM).</p>

<p>SRT 1460 is a SIRT1 activator.</p>

<p>Venadaparib, a PARP inhibitor (IC50: 1.4/1.0 nM for PARP1/2), is orally active, selective, not affecting PARP-5, used in tumor studies.</p>

<p>Ochromycinone (STA 21) is a selective STAT3 inhibitor.</p>

<p>5-Methyl-2'-deoxycytidine (5MedCyd) is a pyrimidine nucleoside that when incorporated into single-stranded DNA can act in cis to signal de novo.</p>

<p>5-Fluoro-2'-deoxycytidine (2'-DEOXY-5-FLUOROCYTIDINE) is an inhibitor of DNA methyltransferase (DNMT) .</p>

<p>Bimolane is a topoisomerase II inhibitor.</p>

<p>Amsacrine hydrochloride (acridinyl anisidide hydrochloride) is topoisomerase II inhibitor , is used in the treatment of acute myelogenous leukemia.</p>

<p>Levofloxacin ((-)-Ofloxacin) is a synthetic fluoroquinolone antibiotic that prevents DNA replication. Cost-effective and quality-assured.</p>

<p>ACY-738 demonstrates inhibitory activity against recombinant HDAC6 (IC50: 1.7 nM), with respective average selectivity over class I HDACs being 100-fold.</p>

<p>YU238259 is a novel inhibitor of homology-dependent DNA repair(HDR), but does not inhibit non-homologous end-joining (NHEJ), in cell-based GFP reporter assays.</p>

<p>GeA-69 (GeA69) is a selective and allosteric PARP14 macrodomain 2 (MD2) inhibitor (Kd: 0.86 μM in ITC assays).</p>

<p>Talazoparib (LT-673) is a new-type PARP inhibitor (IC50: 0.58 nM), It similarly binds to PARP1/2 (Kis: 1.2/0.85 nM).</p>

<p>Tunicamycin is a mixture of antibiotics that inhibit N-linked glycosylation by blocking GlcNAc phosphotransferase (GPT).</p>

<p>LY-294002 HCl (NSC 697286) is a stable PI3K inhibitor (IC50: 0.5-0.97 µM) and prevents autophagosome formation.</p>

<p>MDK-7933 (HDAC8-IN-1) is a HDAC8 inhibitor with an IC50 of 27.2 nM in cancer cell lines.</p>

<p>Belinostat (PXD101) is an inhibitor of hydroxamic acid-type histone deacetylase (HDAC, IC50 of 27 nM in HeLa cell extracts),and with antineoplastic activity.</p>

<p>Veliparib (ABT-888) (ABT-888) is an orally bioavailable inhibitor of PARP (Kis: 5.2/2.9 nM for PARP1/2). It enhances apoptosis and autophagy.</p>

<p>SF2523 is a highly selective and potent inhibitor.</p>

<p>SGI-1027 (DNA Methyltransferase Inhibitor II) is an effective and selective inhibitor of DNA methyltransferase (DNMT).</p>

<p>3-Methoxybenzamide (3-MBA) is a competitive inhibitor of poly(ADP-ribose) synthetase.</p>

<p>HDAC-IN-7 (HBI-8000) (Chidamide impurity) is an impurity of Chidamide.</p>

<p>Pirarubicin (Theprubicin), an anthracycline antibiotic, inhibits DNA/RNA synthesis and is used as an antineoplastic.</p>

<p>Potassium acetate (Diuretic salt) with antibacterial and antifungal properties.</p>

<p>TAS-103 dihydrochloride (BMS-247615 dihydrochloride) is a novel anticancer agent targeting both topoisomerase (Topo) I and Topo II.</p>

<p>KU-0060648 is a dual inhibitor of DNA-PK and PI3Kα, PI3Kβ, PI3Kδ with IC50 of 8.6 nM and 4 nM, 0.5 nM, 0.1 nM respectively, less inhibition of PI3Kγ.</p>

<p>Hypericin (Cyclosan) is a natural anthraquinone compound. Hypericin exhibits antimicrobial, antiviral, antitumor, and antidepressant effects. Cost-effective and quality-assured.</p>

<p>PIK-75, a DNA-PK and PI3K inhibitor, suppresses DNA-PK(IC50=2 nM), p110α(IC50=5.8 nM) and p110γ(IC50=76 nM).</p>

<p>RG108 (N-Phthalyl-L-tryptophan) is an DNA methyltransferase inhibitor(IC50=115 nM).</p>

<p>ETP-46464 is an effective and specific ATR inhibitor (IC50: 25 nM).</p>

<p>Brincidofovir (HDP-CDV) is an orally active, lipophilic form of cidofovir.</p>

<p>Neobavaisoflavone: DNA polymerase inhibitor, potential for treating bone loss, anti-inflammatory, reduces ROS, RNS, cytokines in macrophages.</p>

<p>CHDI-390576 is an HDAC inhibitor that inhibits class IIa HDAC 4, HDAC 5, HDAC 7, and HDAC 9, and can be used in cancer research.</p>

<p>MDL-800 is a SIRT6 modulator with antitumor activity for the study of hepatocellular carcinoma and non-small cell lung cancer.</p>

<p>PF-3882845 is an MR antagonist that binds to the progesterone receptor (PR) and is used in the study of endocrine disorders and urogenital disorders.</p>

<p>CBHcy, a dual substrate analog, is a specific BHMT inhibitor that may induce cysteinemia.</p>

<p>IndiMitecan (LMP776) is an inhibitor of topoisomerase I (Top1) with anticancer activities [1].</p>

<p>The test principle applied in this kit is Sandwich enzyme immunoassay. The microtiter plate provided in this kit has been pre-coated with an antibody specific to Mouse PARP2. Standards or samples are added to the appropriate microtiter plate wells then with a biotin-conjugated antibody specific to Mouse PARP2. Next, Avidin conjugated to Horseradish Peroxidase (HRP) is added to each microplate well and incubated. After TMB substrate solution is added, only those wells that contain Mouse PARP2, biotin-conjugated antibody and enzyme-conjugated Avidin will exhibit a change in color. The enzyme-substrate reaction is terminated by the addition of sulphuric acid solution and the color change is measured spectrophotometrically at a wavelength of 450nm ± 10nm. The concentration of Mouse PARP2 in the samples is then determined by comparing the OD of the samples to the standard curve.</p>

<p>RGFP966 is an HDAC3 inhibitor with IC50 of 0.08 μM, exhibits &gt; 200-fold selectivity over other HDAC.</p>

<p>Semustine, a DNA alkylating agent, is a cancer chemotherapy compound that is nephrotoxic in patients with malignant melanoma receiving adjuvant chemotherapy for</p>

<p>Exatecan (DX-8951f) is a DNA topoisomerase I (TOP1) inhibitor with an IC50 value of 2.2 μM (0.975 μg/mL).Exatecan has antitumor activity and may be used in</p>

<p>Cyclophosphamide-d4 is a deuterated compound of Cyclophosphamide. Cyclophosphamide has a CAS number of 50-18-0. Cyclophosphamide is an alkylating agent used in the treatment of several forms of cancer including leukemias, lymphomas and breast cancer.</p>

<p>Mirin is a Mre11-Rad50-Nbs1 (MRN) complex inhibitor and also inhibits Mre11-associated exonuclease activity.Mirin induces cell cycle arrest in G1 phase.</p>

<p>ART0380 is a potent, antitumor, selective, orally available, ATP-competitive ATR kinase inhibitor for the study of ataxia telangiectasia mutated (ATM) cancer.</p>

<p>PNU-159682 is a highly effective metabolite of the anthracycline nemorubicin.</p>

<p>BRD 4354 (ditrifluoroacetate) is a moderately potent inhibitor of HDAC5 and HDAC9 (IC50s: 0.85 and 1.88 μM).</p>

<p>MY-1B is a nitrogen-substituted butenamide stereoprobe that blocks stereoselective enrichment of NSUN2, binding selectively to the C271 of NSUN2.</p>

<p>7-Methyladenine (NSC-7857) can be used as a marker of exposure to exogenous and carcinogenic methylating agents.</p>

<p>Elaidyl-sulfamide is a sulfamoyl analogue of oleoylethanolamide (OEA). ES is a lipid mediator of satiety that acts through the PPARα.</p>

<p>A-20832 blocks strand cleavage in resolvase-driven recombination; doesn't prevent resolvase-res binding or synapse formation, only binds at res site I.</p>

<p>GSK-7227 is a novel PPARδ partial agonist that upregulates target genes in muscle cells, indicating its potential role in modulating muscle metabolism and energy.</p>

<p>LMP744 is a DNA intercalator and Topoisomerase I (Top1) inhibitor with antitumor activity.</p>

<p>A-1062, a resolvase-binding inhibitor, inhibits resolvase binding to the res site.</p>

<p>L-764406 is a partial agonist of human PPAR gamma.</p>

<p>A 9387 is an inhibitor of resolvase protein.</p>

<p>SIRT2-IN-9: selective SIRT2 inhibitor; IC50=1.3μM; halts MCF-7 cell growth; for cancer study.</p>

<p>Lobeglitazone Sulfate (CKD-501) is an anti-inflammatory thiazolidinedione that prevents NLRP3 inflammasome activation and is used in T2DM research.</p>

<p>BVT.13 is used as a selective PPAR-gamma activator.</p>

<p>promotes the reprogramming of human somatic cells to pluripotent stem cells</p>

<p>Aldoxorubicin, an albumin-binding prodrug of Doxorubicin, exhibits potent antitumor effects in cancer lines and mouse models.</p>

<p>Cas9-IN-3 is a potent inhibitor of Cas9 with IC50 of 28 μM. CRISPR/Cas systems have revolutionized gene editing in several species [1].</p>

<p>Exifone (NSC-680919) is a mixed, nonessential activator of HDAC1 that is capable of binding to both free and substrate-bound enzyme, resulting in an increased</p>

<p>BRD0539 is a cell-permeable spCas9 inhibitor that blocks the binding of spCas9 to DNA and inhibits Streptococcus pyogenes Cas9 (SpCas9).</p>

<p>Guadecitabine is a second-generation DNA methyltransferases inhibitor. It is used for research on acute myeloid leukemia and myelodysplastic syndromes.</p>

<p>Naveglitazar racemate is the racemate of Naveglitazar.</p>

<p>Chlornaphazine is an antineoplastic and has been identified as a human carcinogen.</p>

<p>Arazine, a cell-permeable G protein modulator, is an isoprenylcysteine methyltransferase substrate.</p>

<p>NU/ICRF 500 is a novel anthracenyl-amino acid catalytic inhibitor of topoisomerase II.</p>

<p>S-Aristeromycinylhomocysteine is an inhibitor of adenosylmethionine decarboxylase.</p>

<p>GW0072 is a partial agonist of PPARγ.</p>

<p>PPARγ agonist 3, also known as Compound 18a, is a potent and selective agonist of PPARγ.</p>

XR-11576 is a DNA topoisomerase I and II inhibitor for the treatment of solid tumors.

<p>NC182 is a topo II inhibitor that shows selective and potent topo II inhibition on the induction of topo II-dependent DNA fragmentation.</p>

<p>GW2433 is an agonist of PPAR receptor.</p>

<p>Leurubicin is used as a prodrug of doxorubicin.</p>

<p>ICRF-193 is a DNA topoisomerase II inhibitor.</p>

<p>2′-Deoxy-5-nitrocytidine is a DNA Methyltransferase inhibitor that can be used for cancer research[1].</p>