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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
51 Results for "
instability
" in MedChemExpress (MCE) Product Catalog:
Products (51)
51 Results for "instability" in MCE Product Catalog:
36
36 Publications Verification
Synonyms: RR82 TFA
Research Areas:
Pyridostatin (RR82) TFA is a G-quadruplex (G4) inducer/stabilizer with a Kd of 490 nM. Pyridostatin TFA also acts as an inhibitor of Zika virus (ZIKV) NS2B-NS3 protease, with an IC50 of 11.0 μM. Pyridostatin TFA interacts with G-quadruplex structures, regulates the expression of SRC and SUB1, and induces replication- and transcription-dependent DNA damage, growth arrest, and genomic instability. Pyridostatin TFA exhibits antiproliferative and antiviral activities. Pyridostatin TFA can be used in studies related to breast cancer, cervical cancer, and Zika virus infection .
36
36 Publications Verification
Cat. No.: HY-15176C
CAS No.: 2517456-88-9
Synonyms: RR82 trihydrochloride
Research Areas:
Pyridostatin (RR82) trihydrochloride is a G-quadruplex (G4) inducer/stabilizer with a Kd of 490 nM. Pyridostatin trihydrochloride also acts as an inhibitor of Zika virus (ZIKV) NS2B-NS3 protease, with an IC50 of 11.0 μM. Pyridostatin trihydrochloride interacts with G-quadruplex structures, regulates the expression of SRC and SUB1, and induces replication- and transcription-dependent DNA damage, growth arrest, and genomic instability. Pyridostatin trihydrochloride exhibits antiproliferative and antiviral activities. Pyridostatin trihydrochloride can be used in studies related to breast cancer, cervical cancer, and Zika virus infection .
14
Novobiocin (Albamycin; Cathomycin) is an orally active antibiotic and Hsp-90 antagonist that also inhibits the Polθ helicase/ATPase domain with IC50 values of 24 μM and 15-17 μM, respectively. Novobiocin binds to Hsp90, GyrB, and POLθ, inhibiting their ATPase activity and ssDNA binding. Novobiocin inhibits molecular chaperone function and DNA repair, and induces apoptosis and genomic instability. Novobiocin exhibits bactericidal and antiparasitic activities. Novobiocin inhibits tumor growth in vivo. Novobiocin is used for research on equine piroplasmosis, ovarian cancer, breast cancer, anthrax, and melioidosis .
14
14 Cited Publications
Synonyms: Albamycin sodium; Cathomycin sodium
13
Target:
Research Areas:
Elrelesertib (AZD1390) is an orally active, brain-penetrant ATM kinase inhibitor with IC50 values of 0.78 nM. Elrelesertib blocks ATM-dependent DNA damage response, inhibits ATM autophosphorylation and downstream Chk2, Rad50 phosphorylation, and accumulates at DNA breaks. Elrelesertib acts as a radiosensitizer, induces apoptosis, genomic instability, G2-M cell cycle arrest, ROS elevation, and mitochondrial membrane potential alteration. Elrelesertib has low efflux liability against P-gp and BCRP. Elrelesertib can be used for the research of central nervous system malignancies, glioblastoma multiforme, glioma, lung cancer brain metastases, and breast cancer .
12
Shield-1 (Shld1) is a specific, cell-permeant and high-affinity ligand of FK506-binding protein-12 (FKBP), and reverses the instability by binding to mutated FKBP (mtFKBP), allowing conditional expression of mtFKBP-fused proteins. Shield-1 can stabilize proteins tagged with a mutated FKBP12-derived destabilization domain (DD) .
1
1 Cited Publications
Synonyms: RO7589831; VVD-133214
Target:
Research Areas:
VVD-214 is a synthetic lethal allosteric inhibitor of WRN helicase with an IC50 of 0.1316 µM. VVD-214 covalently binds to cysteine 727 of WRN and inhibits ATP hydrolysis and helicase activity. VVD-214 is potent in causing double-stranded DNA breaks, nuclear swelling, and cell death in high microsatellite instability (MSI) cancers .
Cat. No.: HY-169422
CAS No.: 3064599-36-3
Synonyms: IDE275
Target:
Research Areas:
GSK4418959 (IDE275) is a selective, reversible and orally active WRN helicase inhibitor. GSK4418959 shows >10,000-fold selectivity over other helicases. GSK4418959 inhibits ATPase and DNA unwinding functions in an ATP-competitive manner. GSK4418959 can be used for the study of microsatellite instability-high (MSI-H) cancer, such as colorectal cancer (CRC) and endometrial cancer (EC) .
Cat. No.: HY-W127709
CAS No.: 519-62-0
Target:
Research Areas:
Chlorophyll b is an orally active tetrapyrrole derivative and pigment. Chlorophyll b can be obtained from photosynthetic organisms such as plants and algae. Chlorophyll b acts as a hydrogen donor and increases Glutathione levels. Chlorophyll b has antioxidant activity and functionally replaces chlorophyll a in photosystem II to participate in photosynthesis. Chlorophyll b reduces Cisplatin (HY-17394)-induced DNA damage, chromosome instability, and oxidative stress. Chlorophyll b is mainly used in the study of plant photosynthesis mechanism .
Cat. No.: HY-170430
CAS No.: 3055558-98-7
Target:
Research Areas:
HGC652 is a molecular glue degrader targeting TRIM21 with a TRIM21-dependent nuclear membrane disruption effect. HGC652 binds to the PRY-SPRY domain of TRIM21 with high affinity (Ka=0.061 μM), mediates the interaction between TRIM21 and NUP98, and redirects E3 ligase activity. By triggering the polyubiquitination and proteasomal degradation of nucleoporins (such as NUP155 and GLE1), HGC652 disrupts nuclear membrane integrity, alters nuclear morphology, induces genomic instability, and thereby induces cancer cell death .
Cat. No.: HY-168555
CAS No.: 3053716-98-3
YJ1206 is an orally active selective CDK12/CDK13 PROTAC degrader. YJ1206 induces DNA damage and genomic instability, activates the AKT pathway, and triggers apoptosis. YJ1206 reduces tumor cell viability, inhibits tumor growth, and attenuates tumor cell dissemination. YJ1206 is applicable to research related to prostate cancer and high-grade serous tubo-ovarian cancer .
Cat. No.: HY-W143531
CAS No.: 133331-77-8
Synonyms: NOV03; SHR8058
Target:
Research Areas:
Perfluorohexyloctane (NOV03), a semifluorinated alkane, reduces tear film instability in Meibomian gland dysfunction and evaporative dry eye disease. Perfluorohexyloctane is a long-term tamponade agent. Perfluorohexyloctane increases tear film breakup time and lipid layer thickness .
Target:
Research Areas:
PIP-199 is a selective inhibitor of RMI (RecQ-mediated genome instability protein) core complex/MM2 interaction, with an IC50 of 36 μM. PIP-199 can be used for the research of sensitizing resistant tumors to DNA crosslinking chemotherapeutics .
Synonyms: NCD
Target:
Research Areas:
Naphthyridine carbamate dimer (NCD) is a molecular glue. Naphthyridine carbamate dimer induces designed structural changes in target functional DNA, thereby regulating its function. As a molecular glue, naphthyridine carbamate dimer stabilizes non-spontaneously formed GG homologous mismatched double-stranded DNA. Naphthyridine carbamate dimer reduces the formation of toxic RNA foci and regulates CGG repeat instability associated with fragile X syndrome and spinocerebellar ataxia type 31. Naphthyridine carbamate dimer can be used in research related to fragile X syndrome and spinocerebellar ataxia type 31 .
Cat. No.: HY-139621
CAS No.: 2916559-62-9
Target:
Research Areas:
Colibactin 742 is a covalently binding DNA-damaging agent targeting DNA, with an IC50 of 5.2 μM against human cervical cancer cells (HeLa). Colibactin 742 covalently binds to DNA, forming interstrand crosslinks (ICLs), activating the Fanconi anemia DNA repair pathway, inducing γH2AX and FANCD2 foci formation and cell cycle arrest, while exacerbating mismatch repair deficiency (MMRd)-related mutations. Colibactin 742 can mimic the genotoxicity of natural Colibactin while avoiding its instability, and is mainly used in colorectal cancer (CRC) related research, including microbial tumorigenesis mechanisms, DNA damage repair pathways, and mutation signature analysis .
Target:
Research Areas:
S-methyl DM1 is a thiomethyl derivative of Maytansine. S-methyl DM1 binds to tubulin with a Kd of 0.93 μM and inhibts microtubule polymerization. S-methyl DM1 potently suppresses microtubule dynamic instability and has anticancer effects .
Cat. No.: HY-P2040
CAS No.: 118399-22-7
Cat. No.: HY-112817
CAS No.: 139307-94-1
Synonyms: 8-Oxo-Deoxyguanosine triphosphate
Target:
Research Areas:
8-Oxo-dGTP (8-Oxo-Deoxyguanosine triphosphate) is an oxidized guanine nucleotide formed by ROS-mediated oxidative modification of dGTP, and it also serves as a key substrate for 8-oxo-dGTP pyrophosphohydrolases (such as hMTH1 and E. coli MutT). 8-Oxo-dGTP acts as a DNA mutagen, inserts into nascent DNA and pairs with adenine and cytosine, inducing A:T to C:G transversion mutations. Furthermore, 8-Oxo-dGTP causes oxidative DNA base modification, strand breakage and S-phase arrest, and ultimately triggers AIF-mediated apoptosis and promotes spontaneous carcinogenesis in mth1-deficient mice. Accumulation of 8-Oxo-dGTP in cells induces genomic instability, but it exhibits a tumor-suppressive effect that reduces tumor incidence in mouse models instead. 8-Oxo-dGTP is widely used in studies related to spontaneous carcinogenesis, Parkinson's disease, Alzheimer's disease, heart failure and tumor mechanisms .
Cat. No.: HY-W199190
CAS No.: 693-07-2
Target:
Research Areas:
2-CEES is a mustard gas analog forms only DNA monoadducts. 2-CEES induces centrosome amplification in human and mouse cells. 2-CEES induces centrosome amplification and chromosome instability .
Cat. No.: HY-169422A
CAS No.: 3064599-37-4
Synonyms: IDE275 (enantiomer)
Target:
Research Areas:
GSK4418959 enantiomer is an enantiomer of GSK4418959 (HY-169422). GSK4418959 (IDE275) is a non-covalent, reversible, selective and orally active WRN helicase inhibitor. GSK4418959 inhibits ATPase and DNA unwinding functions in an ATP-competitive manner. GSK4418959 can be used for the study of microsatellite instability-high (MSI-H) 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
