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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
29 Results for "
DNA replication stress
" in MedChemExpress (MCE) Product Catalog:
Products (29)
29 Results for "DNA replication stress" in MCE Product Catalog:
8
8 Publications Verification
Target:
SphK Dihydroceramide Desaturase 1 (DES1) Apoptosis Reactive Oxygen Species (ROS) mTOR PERK Keap1-Nrf2
Research Areas:
SKI-II is an orally active dual-target inhibitor of SphK1/2 and DES1, with Ki values of 16 µM and 0.3 µM against SphK1 and DES1, respectively. SKI-II activates the PERK-Nrf2 antioxidant pathway by stabilizing Nrf2, and synergizes with Temozolomide (HY-17364) to induce oxidative/endoplasmic reticulum stress and cancer cell death under hypoxic conditions. In vivo, SKI-II inhibits SphK activity, promotes ceramide accumulation and apoptosis, and synergizes with Cisplatin (HY-17394) to reverse drug resistance via the ras/MAPK pathway. SKI-II reduces measles virus replication by inhibiting mTORC1 activity. SKI-II binds to VCP to induce M1 polarization, enhances host tolerance to Staphylococcus aureus infection, and exerts radioprotective effects through Nrf2 activation and accelerated DNA repair. SKI-II can be used in research related to glioblastoma, acute myeloid leukemia, gastric cancer, measles virus infection, Staphylococcus aureus infection, and acute radiation syndrome .
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1 Cited Publications
Cat. No.: HY-W040129
CAS No.: 7059-24-7
Category:
1
Target:
Clemizole hydrochloride is an orally active, blood-brain barrier permeable TRPC5 inhibitor, with an IC50 value of 1.05-1.34 μM against mouse TRPC5. Clemizole hydrochloride blocks TRPC1:TRPC5, TRPC3, TRPC4, TRPC6, TRPC7, hERG, hKCNQ1/hKCNE1 and hKv1.5 channels, and activates TRPA1; it modulates 5HT-2B and HTR2A receptors; it inhibits HCV RNA replication, CrtN enzymatic activity, oxidative stress, neuroinflammation, cell apoptosis and bacterial virulence; it maintains blood-brain barrier (BBB) integrity; it enhances DNA repair capacity; it improves cell viability; and it alters cardiac electrophysiological properties. Clemizole hydrochloride can be used in the research of Dravet syndrome, hepatitis C virus infection, Staphylococcus aureus skin infection, Cisplatin (HY-17394)-induced nephrotoxicity, STXBP1-related diseases, traumatic brain injury and xeroderma pigmentosum type C .
1
1 Cited Publications
Cat. No.: HY-117664
CAS No.: 1633660-76-0
Target:
Research Areas:
PNR-7-02 is a dual Rev1 and human DNA polymerase η (hpol η) inhibitor, with an IC50 value of 8 μM against hpol η. PNR-7-02 binds to hpol η to disrupt the orientation of template DNA and block the catalytic function of hpol η. When used in combination with Cisplatin (HY-17394), PNR-7-02 induces DNA damage and replication stress in cells with intact hpol η function. PNR-7-02 can be used in mechanism studies related to chronic myeloid leukemia and ovarian cancer .
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Target:
Clemizole is an orally active, blood-brain barrier permeable TRPC5 inhibitor, with an IC50 value of 1.05-1.34 μM against mouse TRPC5. Clemizole blocks TRPC1:TRPC5, TRPC3, TRPC4, TRPC6, TRPC7, hERG, hKCNQ1/hKCNE1 and hKv1.5 channels, and activates TRPA1; it modulates 5HT-2B and HTR2A receptors; it inhibits HCV RNA replication, CrtN enzymatic activity, oxidative stress, neuroinflammation, cell apoptosis and bacterial virulence; it maintains blood-brain barrier (BBB) integrity; it enhances DNA repair capacity; it improves cell viability; and it alters cardiac electrophysiological properties. Clemizole can be used in the research of Dravet syndrome, hepatitis C virus infection, Staphylococcus aureus skin infection, Cisplatin (HY-17394)-induced nephrotoxicity, STXBP1-related diseases, traumatic brain injury and xeroderma pigmentosum type C .
Cat. No.: HY-W011725
CAS No.: 2002-35-9
Synonyms: m6dA
Research Areas:
N-6-Methyl-2-deoxyadenosine (m6dA) is an adenine nucleoside analogue. N-6-Methyl-2-deoxyadenosine targets nuclear processes and DNA replication machineries including WER, SATB1, TFAM, Jumu, SSBP1, DNA polymerase η and phage polymerase Gp90 exo −. N-6-Methyl-2-deoxyadenosine acts as a multifunctional epigenetic regulator that modulates transcription, DNA damage response, cell cycle, transposon silencing, stress adaptation, epigenetic crosstalk, and nucleosome organization in both prokaryotes and eukaryotes. N-6-Methyl-2-deoxyadenosine regulates mitochondrial epigenetic inheritance and is required for fear extinction memory in mice. N-6-Methyl-2-deoxyadenosine exhibits dysregulated levels in cancers. N-6-Methyl-2-deoxyadenosine can be used for the research of glioblastoma, triple negative breast cancer, and conditioned fear (fear extinction impairment) .
Cat. No.: HY-171767
CAS No.: 3038446-94-2
Synonyms: JB325
Target:
Research Areas:
SK2188 (JB325) is a selective AURKA PROTAC degrader with a DC50 of 3.9 nM. SK2188 recruits CRBN E3 ubiquitin ligase to target and degrade AURKA, abrogating both its catalytic and non-kinase functions, which leads to the destabilization and degradation of the oncogenic protein MYCN, ultimately inducing replication stress, DNA damage and apoptosis. SK2188 is applicable to research related to neuroblastoma .
Cat. No.: HY-155219
CAS No.: 2379556-15-5
Research Areas:
TH9028 is an inhibitor of MTHFD1, MTHFD2 and MTHFD2L, with IC50 values of 0.5 nM, 11 nM and 27 nM, respectively. TH9028 reduces replication fork speed, induces replication stress, triggers S-phase arrest, initiates apoptosis, impairs thymidine production, and causes erroneous uracil incorporation into DNA. TH9028 can be used in research related to acute myeloid leukemia .
Cat. No.: HY-155798
CAS No.: 2871057-47-3
Target:
Research Areas:
BBI-2779 is a highly selective, orally active CHK1 inhibitor with a CHK1 IC50 of 0.3 nM. BBI-2779 leverages transcription-replication conflicts on extrachromosomal DNA (ecDNA) to induce synthetic lethality, replication stress, DNA damage and cell death in ecDNA-positive tumor cells. BBI-2779 blocks ecDNA-mediated acquired resistance to targeted therapies and inhibits tumor growth in mouse models of gastric cancer. BBI-2779 is applicable to ecDNA-positive cancer-related research .
Cat. No.: HY-105067A
CAS No.: 922174-60-5
Synonyms: GV-1001 hydrochloride
Research Areas:
Infection Neurological Disease Inflammation/Immunology Cancer
Tertomotide hydrochloride (GV-1001 hydrochloride) is a 16-amino acid peptide derived from hTERT, with both cell-penetrating and immunostimulatory activities, and it can cross the blood-brain barrier. Tertomotide hydrochloride binds to STING, HO-1, eHSP70, eHSP90, bradykinin receptor 1, VEGFR-2, NF-κB, p38 MAPK and Smad2. Tertomotide hydrochloride induces type I interferon production, mitochondrial DNA stress and T-cell responses; inhibits HBV replication, angiogenesis, TGF-β signaling pathway, NF-κB activation, endothelial-mesenchymal transition (EndMT) and fibrosis; regulates microglia; and exerts neuroprotective, anti-inflammatory, antioxidant, anti-apoptotic and anti-tumor effects. Tertomotide hydrochloride can be used in research related to hepatitis B virus infection, Alzheimer's disease, non-small cell lung cancer, atherosclerosis and depression .
Cat. No.: HY-W015940
CAS No.: 1455-77-2
Target:
Guanazole is a ribonucleotide reductase (RNR) inhibitor that blocks replicative DNA synthesis by inhibiting deoxyribonucleotide biosynthesis. Guanazole selectively inhibits DNA synthesis in rapidly proliferating tissues, induces replication stress and G2/M phase arrest in Schizosaccharomyces pombe, and exhibits myelosuppressive, immunosuppressive, and anti-L1210 leukemia activities. Guanazole does not induce DNA repair and only shows slight mutagenicity towards Salmonella typhimurium TA102. Guanazole serves as an alternative tool to Hydroxyurea (HY-B0313) for replication checkpoint studies in Schizosaccharomyces pombe. Guanazole can be applied in research related to leukemia and solid tumors .
Cat. No.: HY-147866
CAS No.: 3033492-79-1
Target:
Research Areas:
Antibacterial agent 110 (Compound 4e) is a potent antibacterial agent with a MIC value of 1 μg/mL against P. aeruginosa. Antibacterial agent 110 possesses favorable antibiofilm activity and can destroy cell membranes. Antibacterial agent 110 causes metabolic arrest and intracellular oxidative stress, and obstructs DNA replication .
Cat. No.: HY-144435
ATR-IN-11 (Compound Hit01) is a potent inhibitor of ataxia telangiectasia and Rad3-related (ATR) kinase. ATR kinase is a key regulating protein within the DNA damage response (DDR), responsible for sensing replication stress (RS). ATR-IN-11 is a promising lead compound for subsequent agent discovery targeting ATR kinase. ATR-IN-11 has the potential for the research of cancer disease .
Cat. No.: HY-121777
CAS No.: 1383607-61-1
Target:
Research Areas:
SFOM-0046 arrests cell cycle in S-phase and causes DNA replication stress leading to the phosphorylation of H2AX into γ-H2AX. SFOM-0046 induces DNA damages. SFOM-0046 is a potent anticancer agent .
Cat. No.: HY-163941
Target:
Research Areas:
GSK_WRN2 is a potent and selective covalent WRN helicase inhibitor that suppresses replication stress caused by DNA (TA)n dinucleotide repeat expansions. GSK_WRN2 can be used to study microsatellite instability (MSI) cancers .
Cat. No.: HY-162568
7-tert-Butylfascaplysin (7-TB) is a derivative of Fascaplysin (HY-112328), that can be isolated from Fascaplysinopsis sp.. 7-tert-Butylfascaplysin induces replication stress, leads to toxic DNA double-strand breaks and apoptosis-like cell death, and thus exhibits cytotoxicity in cancer cells in nanomolar levels. 7-tert-Butylfascaplysin exhibits DNA intercalating activity with EC50 of 3.2 μM .
Cat. No.: HY-W040129R
CAS No.: 7059-24-7
Category:
Cat. No.: HY-30234S
CAS No.: 1251554-64-9
Cat. No.: HY-164717
CAS No.: 2922789-15-7
Research Areas:
FORX-428 is an orally active, selective poly (ADP-ribose) glycohydrolase (PARG) inhibitor. FORX-428 reversibly inhibits PARG, thereby blocking PAR chain dissociation, inhibiting DNA repair, inducing tumor cell death, and targeting replication stress in cancer cells. FORX-428 can be used in the research of ovarian cancer and triple-negative breast cancer .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
