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Fosbretabulin disodium (CA 4DP) is a tubulindestabilizing agent. Fosbretabulin disodium is the Combretastatin A4 proagent that selectively targets endothelial cells, induces regression of nascent tumour neovessels, reduces tumour blood flow and causes central tumour necrosis .
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) .
Fenbendazole is an orally active benzimidazole anthelmintic agent, with a broad antiparasitic range. Fenbendazole is a microtubule destabilizing agent and acts on helminthes primarily by binding to tubulin and disrupting the tubulin microtubule equilibrium. Fenbendazole stabilizes the transcriptional activator HIF-1α. Fenbendazole possesses an efficient anti-proliferative activity and induces apoptosis. Fenbendazole causes cell-cycle arrest and mitotic cell death, and has antitumor activity in mice xenografted with wild-type p53 .
Fenbendazole (Standard) is the analytical standard of Fenbendazole. This product is intended for research and analytical applications. Fenbendazole is an orally active benzimidazole anthelmintic agent, with a broad antiparasitic range. Fenbendazole is a microtubule destabilizing agent and acts on helminthes primarily by binding to tubulin and disrupting the tubulin microtubule equilibrium. Fenbendazole stabilizes the transcriptional activator HIF-1α. Fenbendazole possesses an efficient anti-proliferative activity and induces apoptosis. Fenbendazole causes cell-cycle arrest and mitotic cell death, and has antitumor activity in mice xenografted with wild-type p53 .
Parbendazole is a potent inhibitor of microtubule assembly, destabilizes tubulin, with an EC50 of 530?nM, and exhibits a broad-spectrum anthelmintic activity.
Microtubule destabilizing agent-2 (Compound 21) is an orally active and selective antitumor compound targeting microtubule protein. Microtubule destabilizing agent-2 destabilizesmicrotubule proteins and inhibits microtubule polymers. Microtubule destabilizing agent-2 arrests the G0/G1 phase in human tumor cells. Microtubule destabilizing agent-2 induces Apoptosis by activating the cascade pathway of caspases. Microtubule destabilizing agent-2 has anti-inflammatory activity, as inhibiting TNF-α and IL-6 in vitro. Microtubule destabilizing agent-2 reduces tumors growth in xenograft mice .
Microtubule destabilizing agent-1 (Compound 12b) acts as a microtubule destabilizing agent (MDA) based on hydroxamic acid, could serve as a potential MDA for further investigation. Microtubule destabilizing agent-1 shows favorable metabolism stability, high bioavailability, and potent antitumor activity .
AB-452, a Dihydroquinolizinone (DHQ) analogue, is a potent and orally active HBV RNA destabilizer. AB-452 inhibits PAPD5/7 proteins in vitro with good in vivo efficacy in a chronic HBV mouse model .
KY1220 is a compound that destabilizes both β-catenin and Ras, via targeting the Wnt/β-catenin pathway; with an IC50 of 2.1 μM in HEK293 reporter cells.
Parbendazole (Standard) is the analytical standard of Parbendazole. This product is intended for research and analytical applications. Parbendazole is a potent inhibitor of microtubule assembly, destabilizes tubulin, with an EC50 of 530 nM, and exhibits a broad-spectrum anthelmintic activity.
Kasugamycin (Ksg) is an antibiotic which binds both the 30S and 70S ribosome but not isolated 50S subunits. Kasugamycin mimics mRNA nucleotides to destabilize tRNA binding and inhibit canonical translation initiation .
Thiacloprid, a chloronicotinyl insecticide, is targeted chiefly to control aphid pest species in orchards and vegetables . Thiacloprid destabilizes DNA. Thiacloprid changes the structure and stability of DNA through binding into the minor groove by hydrophobic or hydrogen interactions .
Kasugamycin hydrochloride hydrate (Ksg hydrochloride hydrate) is an antibiotic which binds both the 30S and 70S ribosome but not isolated 50S subunits. Kasugamycin hydrochloride hydrate (Ksg hydrochloride hydrate) mimics mRNA nucleotides to destabilize tRNA binding and inhibit canonical translation initiation .
Kasugamycin hydrochloride (Ksg hydrochloride) is an antibiotic which binds both the 30S and 70S ribosome but not isolated 50S subunits. Kasugamycin hydrochloride (Ksg hydrochloride) mimics mRNA nucleotides to destabilize tRNA binding and inhibit canonical translation initiation .
KY1022 is a small molecule destabilizing Ras via targeting the Wnt/β-catenin pathway. KY1022 can inhibit cellular EMT, metastasis and apoptosis. KY1022 can be used for the research of metastatic colorectal cancer .
UMK57 is a small molecule compound that specifically promotes k-MT attachment error correction to inhibit chromosome missegregation, which can improve chromosome segregation fidelity by destabilizing kinetochore microtubule (k-MT) attachment during mitosis .
9A1P9 is a multi-tail ionizable cationic phospholipid. 9A1P9 induces membrane destabilization. 9A1P9 can be used for CRISPR-Cas9 gene editing in mice .
Suprafenacine is a cell permeable, tubulin-destabilizing molecule which bind microtubules at the colchicine-binding site and inhibit polymerization. Suprafenacine can induce G2/M cell cycle arrest and apoptosis, and can be used for cancer research .
NC9 (Cbz-Lys(Acr)-PEG2-dansyl) is an irreversible transglutaminase (TG) inhibitor. NC9 inhibits osteoblast differentiation and mineralization. NC9 destabilizes microtubules. NC9 can be used for the research of osteoblast differentiation .
Shield-2 is an efficient stabilizing ligand binding to the FKBP (F36V) protein with a dissociation constant of 29 nM. Shield-2 binds tightly to the FKBP mutants destabilizing domains and prevents degradation, thus providing small molecule regulation over intracellular protein levels .
ENMD-1198 (IRC-110160), an orally active microtubule destabilizing agent, is a 2-methoxyestradiol analogue with antiproliferative and antiangiogenic activity. ENMD-1198 is suitable for inhibiting HIF-1alpha and STAT3 in human HCC cells and leads to reduced tumor growth and vascularization.
Thiacloprid (Standard) is the analytical standard of Thiacloprid. This product is intended for research and analytical applications. Thiacloprid, a chloronicotinyl insecticide, is targeted chiefly to control aphid pest species in orchards and vegetables . Thiacloprid destabilizes DNA. Thiacloprid changes the structure and stability of DNA through binding into the minor groove by hydrophobic or hydrogen interactions .
Kasugamycin (hydrochloride) (Standard) is the analytical standard of Kasugamycin (hydrochloride). This product is intended for research and analytical applications. Kasugamycin hydrochloride (Ksg hydrochloride) is an antibiotic which binds both the 30S and 70S ribosome but not isolated 50S subunits. Kasugamycin hydrochloride (Ksg hydrochloride) mimics mRNA nucleotides to destabilize tRNA binding and inhibit canonical translation initiation .
Tubulin inhibitor 14 is a potent NQO2 (quinone oxidoreductase 2) inhibitor with an IC50 of 1.0 μM. Tubulin inhibitor 14 also inhibits tubulin polymerization and the formation of endothelial cell capillary-like tubes. Tubulin inhibitor 14 is a microtubule-destabilizing agent with potential tumor-selectivity and antiangiogenic and vascular disrupting features .
Col003 is a selective and potent inhibitor of Hsp47 and competitively binds to the collagen binding site on Hsp47 (IC50=1.8 μM). Col003 discourages the interaction of Hsp47 with collagen and inhibits collagen secretion by destabilizing the collagen triple helix. Col003 can be used for the investigation of fibrosis
ALC-0315 is an ionisable aminolipid that is responsible for mRNA compaction and aids mRNA cellular delivery and its cytoplasmic release through suspected endosomal destabilization. ALC-0315 can be used to form lipid nanoparticle (LNP) delivery vehicles. Lipid-Nanoparticles have been used in the research of mRNA COVID-19 vaccine .
LCAHA (LCA hydroxyamide) is a deubiquitinase USP2a inhibitor with IC50s of 9.7 μM and 3.7μM in Ub-AMC Assay and Di-Ub Assay, respectively. LCAHA destabilizes Cyclin D1 and induces G0/G1 arrest by inhibiting deubiquitinase USP2a .
M47 is a small molecule that selectively destabilizes Cryptochrome 1 (CRY1) and increases degradation of the CRY1 in the nucleus. M47 enhances apoptosis in Ras-transformed P53-deficient mouse skin fibroblast lines and enhances life span in p53 knockout mice. M47 can be used in research of cancer .
ALC-0315 Excipient is an ionisable aminolipid that is responsible for mRNA compaction and aids mRNA cellular delivery and its cytoplasmic release through suspected endosomal destabilization. ALC-0315 Excipient can be used to form lipid nanoparticle (LNP) delivery vehicles. Lipid-Nanoparticles have been used in the research of mRNA COVID-19 vaccine .
hVEGF-IN-1, a quinazoline derivative, could specifically bind to the G-rich sequence in the internal ribosome entry site A (IRES-A) and destabilize the G-quadruplex structure. hVEGF-IN-1 binds to the IRES-A (WT) with a Kd of 0.928 μM in SPR experiments. hVEGF-IN-1 could hinder tumor cells migration and repress tumor growth by decreasing VEGF-A protein expression .
CHM-1, a microtubule-destabilizing agent, inhibits tubulin polymerization. CHM-1 is a potent and selective antimitotic antitumor activity against human hepatocellular carcinoma. CHM-1 induces growth inhibition and apoptosis via G2-M phase arrest in human hepatocellular carcinoma cells by activation of Cdc2 kinase activity .
NSC15520 is a small molecular inhibitor of Replication Protein A (RPA). NSC15520 specifically recognizes the RPA N-terminal DNA binding domain (DBD), and blocks the interaction of RPA with p53 or RAD9. NSC15520 also inhibtis helix destabilization of a duplex DNA (dsDNA) oligonucleotide, involves in DNA replication, DNA repair, DNA recombination, and DNA damage response signaling .
TRAP1-IN-2 (compound 36) is a selective degrader of TRAP1 downstream proteins without affecting Hsp90's cytoplasmic downstream proteins. TRAP1-IN-2 also inhibits OXPHOS and alters cellular glycolysis metabolism. TRAP1-IN-2 destabilizes TRAP1 tetramers and disrupts mitochondrial membrane potential.
DBPR728 is an acyl prodrug of 6K465 that carries fewer hydrogen bond donors. 6K465 acts as an Aurora kinase inhibitor that destabilizes MYC family cancer proteins and has antitumor efficacy. DBPR728 has the potential to inhibit cancers that overexpress C-MYC and N-MYC, with a 10-fold increase in oral bioavailability compared to 6K465 .
Pyrimidine-indole hybrid is a compound that inhibits ciliogenesis and has the activity of antagonizing the Hedgehog signaling pathway by destabilizing microtubules. Pyrimidine-indole hybrid exerts its biological effects by inhibiting ciliogenesis and deconstructing the stable form of α-tubulin. Pyrimidine-indole hybrid has shown its unique mechanism of action in in vitro cell experiments and zebrafish embryo models, interfering with microtubule dynamics .
AB-161 is an orally active HBV RNA destabilizer and a PAPD5/7 inhibitor, with its primary action focused in the liver. AB-161 treats Hepatitis B Virus (HBV) infection by lowering the levels of Hepatitis B surface antigen (HBsAg), with an EC50 value of 2.2 nM for HBsAg. AB-161 can be used in the field of HBV infection research .
ALC-0315 analogue-2 is an analogue of ALC-0315. ALC-0315 is an ionisable aminolipid that is responsible for mRNA compaction and aids mRNA cellular delivery and its cytoplasmic release through suspected endosomal destabilization. ALC-0315 can be used to form lipid nanoparticle (LNP) delivery vehicles. Lipid-Nanoparticles have been used in the research of mRNA COVID-19 vaccine.
Tubulysin B is a highly cytotoxic peptide and potent microtubuledestabilizing agents isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. Tubulysin B has IC50 values in the picomolar range against many cancer cell lines, including those with multidrug resistant properties .Tubulysin B is a cytotoxic activity tubulysin which inhibits tubulin polymerization and leads to cell cycle arrest and apoptosis .
The Tubulysin family of secondary metabolites was originally isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. These compounds are potent microtubule destabilizers and anti-microtubule toxins (anti-microtubule toxins), with effective IC50 concentrations against multidrug-resistant cancer cell lines. In the picomole range. Tubulysins are ideal candidates for incorporation into small active molecule conjugate (SMDC) delivery systems and are commonly used in ADC synthesis as ADC cytotoxins (ADC Cytotoxin) .
BMH-22, a benzonaphthyridin, is a RNA polymerase I (Pol I) transcription inhibitor independent of p53 function. BMH-22 causes reorganization of nucleolar marker proteins consistent with segregation of the nucleolus. BMH-22 destabilizes RPA194 in a proteasome-dependent manner and inhibits nascent rRNA synthesis and expression of the 45S rRNA precursor. BMH-22 shows potent anticancer activity across many tumor types .
SirReal2 is a potent, isotype-selective Sirt2 inhibitor with an IC50 value of 140 nM and has very little effect on the activities of Sirt3-5. SirReal2 leads to tubulin hyperacetylation in HeLa cells and induces destabilization of the checkpoint protein BubR1. SirReal2 combined with VS-5584 (HY-16585) suppresses tumor growth and extends the survival rate of mice in tumor xenograft model. SirReal2 is is promising for research of cancer, inflammation and neurodegeneration .
DAP-81 is an inhibitory agent targeting Polo-like kinases (Plks), a class of evolutionarily conserved serine/threonine kinases. DAP-81 dose-dependently increases the number of monopolar spindles in treated cells. High-resolution live-cell microscopy revealed that Plk activity is required for the assembly and maintenance of bipolar mitotic spindles. Plk inhibition destabilizes centromeric microtubules while stabilizing other spindle microtubules, leading to the formation of monopolar spindles. Further testing of compounds based on "privileged scaffolds" such as the DAP scaffold may lead to the discovery of new cell division probes and anti-microtubule agents.
Antiproliferative agent-23 is a microtubule-destabilizing agent (MDA) and efficiently disturbes the tubulin-microtubule system. Antiproliferative agent-23 induces apoptosis via a mitochondrion-dependent pathway by downregulating the Bcl-2 protein, upregulating Bax and Cyt c proteins, and activating the caspase cascade. Antiproliferative agent-23 initiates reactive oxygen species (ROS)-mediated endoplasmic reticulum stress in A549/CDDP cells (cisplatin resistant cancer cell line) via the PERK/ATF4/CHOP signaling pathway. Antiproliferative agent-23 has anti-tumor activity .
ALC-0315 is an ionisable aminolipid that is responsible for mRNA compaction and aids mRNA cellular delivery and its cytoplasmic release through suspected endosomal destabilization. ALC-0315 can be used to form lipid nanoparticle (LNP) delivery vehicles. Lipid-Nanoparticles have been used in the research of mRNA COVID-19 vaccine .
ALC-0315 analogue-2 is an analogue of ALC-0315. ALC-0315 is an ionisable aminolipid that is responsible for mRNA compaction and aids mRNA cellular delivery and its cytoplasmic release through suspected endosomal destabilization. ALC-0315 can be used to form lipid nanoparticle (LNP) delivery vehicles. Lipid-Nanoparticles have been used in the research of mRNA COVID-19 vaccine.
ppTG20 is an amphiphilic cell penetrating peptide (KALA) that can be used for gene transfection. ppTG20 can bind to DNA, destabilize membranes, and mediate DNA transfection .
Fosbretabulin disodium (CA 4DP) is a tubulindestabilizing agent. Fosbretabulin disodium is the Combretastatin A4 proagent that selectively targets endothelial cells, induces regression of nascent tumour neovessels, reduces tumour blood flow and causes central tumour necrosis .
Kasugamycin hydrochloride (Ksg hydrochloride) is an antibiotic which binds both the 30S and 70S ribosome but not isolated 50S subunits. Kasugamycin hydrochloride (Ksg hydrochloride) mimics mRNA nucleotides to destabilize tRNA binding and inhibit canonical translation initiation .
Tubulysin B is a highly cytotoxic peptide and potent microtubuledestabilizing agents isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. Tubulysin B has IC50 values in the picomolar range against many cancer cell lines, including those with multidrug resistant properties .Tubulysin B is a cytotoxic activity tubulysin which inhibits tubulin polymerization and leads to cell cycle arrest and apoptosis .
Kasugamycin (hydrochloride) (Standard) is the analytical standard of Kasugamycin (hydrochloride). This product is intended for research and analytical applications. Kasugamycin hydrochloride (Ksg hydrochloride) is an antibiotic which binds both the 30S and 70S ribosome but not isolated 50S subunits. Kasugamycin hydrochloride (Ksg hydrochloride) mimics mRNA nucleotides to destabilize tRNA binding and inhibit canonical translation initiation .
The HNRNPA1 protein is complexly involved in multiple RNA processing functions, packaging pre-mRNA into hnRNP particles, promoting Poly(A) mRNA transport, and regulating splice site selection. Crucially, it binds inhibitoryly to sequences flanking PKM exon 9, favoring the inclusion of exon 10 in pyruvate kinase PKM splicing, thereby generating the PKM M2 isoform. HNRNPA1 Protein, Human (His) is the recombinant human-derived HNRNPA1 protein, expressed by E. coli , with N-6*His labeled tag.
T4 gp32 is a single-stranded DNA-binding protein actively involved in various stages of viral DNA processes, including replication, recombination, and repair. During replication, it covers the lagging strand of single-stranded DNA, supporting the replication fork. T4 gp32 Protein, T4 phage (His, Myc) is the recombinant T4 gp32 protein, expressed by E. coli , with N-His, C-Myc labeled tag. T4 gp32 Protein, T4 phage (His, Myc), has molecular weight of 41.8 kDa.
ALC-0315 is an ionisable aminolipid that is responsible for mRNA compaction and aids mRNA cellular delivery and its cytoplasmic release through suspected endosomal destabilization. ALC-0315 can be used to form lipid nanoparticle (LNP) delivery vehicles. Lipid-Nanoparticles have been used in the research of mRNA COVID-19 vaccine .
ALC-0315 Excipient is an ionisable aminolipid that is responsible for mRNA compaction and aids mRNA cellular delivery and its cytoplasmic release through suspected endosomal destabilization. ALC-0315 Excipient can be used to form lipid nanoparticle (LNP) delivery vehicles. Lipid-Nanoparticles have been used in the research of mRNA COVID-19 vaccine .
ALC-0315 analogue-2 is an analogue of ALC-0315. ALC-0315 is an ionisable aminolipid that is responsible for mRNA compaction and aids mRNA cellular delivery and its cytoplasmic release through suspected endosomal destabilization. ALC-0315 can be used to form lipid nanoparticle (LNP) delivery vehicles. Lipid-Nanoparticles have been used in the research of mRNA COVID-19 vaccine.
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