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Merbarone (NSC 336628) is an orally active inhibitor of topoisomerase II. Merbarone acts primarily by blocking topoisomerase II-mediated DNA cleavage without stabilizing topo II-DNA covalent complexes. Merbarone is an anticancer agent .
Beclin1-ATG14L interaction inhibitor 1 (com 19) is a selective Beclin1-ATG14L interaction inhibitor. This protein interaction mechanism specifically targets complex I of the lipid kinase VPS34 without affecting complexII. Because the integrity of VPS34 complexII depends on the Beclin 1-UVRAG interaction. Beclin1-ATG14L interaction inhibitor 1 can disrupt the formation of VPS34 complex I and inhibit autophagy, but does not affect complexII-related vesicle transport .
Lacto-N-triose II is a core structural unit of human milk oligosaccharides (HMOs). Lacto-N-triose II owns nutraceutical potentials and can be used in the production of complex HMOs .
DACA inhibits two essential nuclear enzymes in vitro, DNA topoisomerase I and DNA topoisomerase (topo) II. DACA stabilises topo I, topo II alpha, and topo II beta cleavable complexes in human leukaemia CCRF-CEM cells .
2-Thenoyltrifluoroacetone is a chelating agent. 2-Thenoyltrifluoroacetone can be used for the complexation of various metal ions including Mn(II), Co(III), Ni(II), et al.. 2-Thenoyltrifluoroacetone possesses antitubercular and cytotoxic activities. 2-Thenoyltrifluoroacetone is also used as common inhibitor of mitochondrial electron flux and to analyze the endothelial cell dysfunction. Besides, copper (II) complex of 2-Thenoyltrifluoroacetone has anticancer activity against K562 .
Filipin complex is a potent polyene macrolide antifungal antibiotic. Filipin complex inserts into membranes and sequester cholesterol into complexes and inhibits PRRSV entry. The Filipin complex consists of about 75.8% Filipin III (HY-N6718), 10.8% Filipin IV, 9.1% Filipin II, and 1.2% Filipin I .
Topoisomerase II inhibitor 16 (compound CT3) is a selective, orally active, brain-penetrant and irreversible trypanosomal topoisomerase II inhibitor by stabilizing double-stranded DNA:enzyme cleavage complexes. Topoisomerase II inhibitor 16 has the potential for Chagas disease research .
Cu(II)GTSM, a cell-permeable Cu-complex, significantly inhibits GSK3β. Cu(II)GTSM inhibits Amyloid-β oligomers (AβOs) and decreases tau phosphorylation. Cu(II)GTSM also decreases the abundance of Amyloid-β trimers. Cu(II)GTSM is a potential anticancer and antimicrobial agent .
Cu(II)-Elesclomol is a Cu 2+complex of Elesclomol (HY-12040). Cu(II)-Elesclomol induces cuproptosis. Cu(II)-Elesclomol also inducesapoptosis, causes a G1 cell cycle block and induces DNA double strand breaks in K562 cells. Cu(II)-Elesclomol also weakly inhibits DNA topoisomerase I. Cu(II)-Elesclomol has anticancer activity .
Cobalt phthalocyanine is a catalyst of redox reaction, catalyzes aerobic regenerations of aldehydes and ketones from aldoximes and ketoximes. Cobalt phthalocyanine can be used in the development of electrocatalysts .
24RBPyBC is a dinucleating macrocyclic ligand, it contains phenolate pyridine, bipyridine, and amino groups form dinuclear Fe(II) and Fe(III) complexes .
Antiproliferative agent-10 (compound 8) is an anti-tumour ruthenium(II)-tris-pyrazolylmethane complex that inhibits the growth of cancer cells by inhibiting mitochondrial calcium uptake .
Antiproliferative agent-10 (compound 1) is an anti-tumour ruthenium(II)-tris-pyrazolylmethane complex that inhibits the growth of cancer cells by inhibiting mitochondrial calcium uptake .
Bathophenanthrolinedisulfonic acid disodium salt is used as a colorimetric reagent for the detection of iron. It is widely used for the determination of iron in aqueous solutions without the use of extraction solvents. It is used as a precursor for the preparation of the anion Europium(III) disulfonated bathophenanthroline tris(dibenzoylformic acid) complex and ruthenium II tris(rubphenanthroline disulfonate). It plays a crucial role in the catalytic oxidation of 2-hexanol by enabling it to form a water-soluble complex with palladium.
Netropsin dihydrochloride is a small-molecule MGB (minor-groove binder), inhibits the catalytic activity of isolated topoisomerase and interferes with the stabilization of the cleavable complexes of topoisomerase II and I in nuclei . Netropsin dihydrochloride exhibits antiviral activity against the vaccinia virus .
Fluxapyroxad is a synthetic broad-spectrum fungicide for the control of fungal diseases. It works by inhibiting succinate dehydrogenase in complexII of the mitochondrial respiratory chain, resulting in inhibition of spore germination, germ tubes and mycelia growth within the fungus target species .
CJJ300 is a transforming growth factor-β (TGF-β) inhibitor with an IC50 of 5.3 µM. CJJ300 inhibits TGF-β signaling by disrupting the formation of the TGF-β-TβR-I-TβR-II signaling complex .
Aclacinomycin A (Aclarubicin) is an orally active and potent anthracycline antitumor antibiotic. Aclacinomycin A is an inhibitor of topoisomerase I and II. Aclacinomycin A inhibits synthesis of nucleic acid, especially RNA. Aclacinomycin A might inhibit the 26S protease complex as well as the ubiquitin-ATP-dependent proteolysis .
Aclacinomycin A (Aclarubicin) hydrochloride is an orally active and potent anthracycline antitumor antibiotic. Aclacinomycin A hydrochloride is an inhibitor of topoisomerase I and II. Aclacinomycin A hydrochloride inhibits synthesis of nucleic acid, especially RNA. Aclacinomycin A hydrochloride might inhibit the 26S protease complex as well as the ubiquitin-ATP-dependent proteolysis .
ROS-ERS inducer 1 is a type II ICD (immunogenic cell death) inducer. ROS-ERS inducer 1 is a Pt(II)-N-heterocyclic carbene (Pt(II)-NHC) complex derived from 4,5-diarylimidazole. ROS-ERS inducer 1 successfully induces endoplasmic reticulum stress (ERS) accompanied by reactive oxygen species (ROS) generation and finally lead to the release of damage-associated molecular patterns (DAMPs) in HCC cells. ROS-ERS inducer 1 displays much higher anticancer activities than Cisplatin .
MnTBAP chloride is a superoxide dismutase (SOD) mimetic and peroxynitrite scavenger. MnTBAP chloride is a manganic porphyrin complex and has anti-oxidative property. MnTBAP chloride mediates anti-inflammatory effects through upregulation of BMPR-II and inhibition of the NFκB signaling. MnTBAP chloride has the potential for the fibrotic response in chronic kidney diseases (CKDs) research .
H-Ser-Tyr-OH is a dipeptide consisting of glutamic acid, glycine and histidine. H-Ser-Tyr-OH can form a copper(II) complex with copper ions to form a strong free radical scavenging activity. H-Ser-Tyr-OH also increases the intracellular uptake of the delta opioid receptor ligand deltorphin .
Antifungal agent 92 (Compound 21) is a potent antifungal agent with an EC50 of 4.4 μM against Sclerotinia sclerotiorum. Antifungal agent 92 can induce abnormal mitochondrial morphology, loss of mitochondrial membrane potential, and reactive oxygen species (ROS) accumulation in Sclerotinia sclerotiorum. Antifungal agent 92 is a moderate promiscuous inhibitor of mitochondrial complexesII and III .
Antiproliferative agent-11 (compound 7) is an antiproliferative and selective Ruthenium(II)-Tris-pyrazolylmethane complex. Antiproliferative agent-11 shows antiproliferative activity towards MCF-7, HeLa, 518A2, HCT116 and RD with IC50s of 6, 10, 6.8, 6.7 and 6 μM, respectively. Antiproliferative agent-11 can be used for the research of cancer .
Phenoxodiol (Idronoxil), a synthetic analog of Genestein, activates the mitochondrial caspase system, inhibits XIAP (an apoptosis inhibitor), and sensitizes the cancer cells to Fas-mediated apoptosis. Phenoxodiol also inhibits DNA topoisomerase II by stabilizing the cleavable complex. Phenoxodiol induces cell cycle arrest in the G1/S phase of the cell cycle and upregulates p21 WAF1 via a p53 independent manner .
HL-PEG2k is a second near-infrared Ru(II) polypyridyl complex. HL-PEG2k exhibits a wavelength bathochromic shift, enhanced photothermal conversion efficiency (41.77%), and an antineoplastic effect against glioma. HL-PEG2k displays a superior biocompatibility and thus can be a potential theranostic platform to combat the growth and recurrence of tumors .
Thiosemicarbazide is a vitamin B6 antagonist with anti-acne activity. Thiosemicarbazide is also a well-known source in the synthesis of heterocycles, and its derivatives have potential anticancer activity. Thiosemicarbazide (TSC: HL1) reacts with metal salts, urea (U), to prepare Co(II) and Cu(I) metal complexes. Thiosemicarbazide is also used in the fields of media communications and optical storage, and in the spectrophotometric detection of metals .
Cuprizone is a copper chelating agent that forms a deep blue copper ketone complex with copper (II). The copper ketone reaction can be used in colorimetric tests for the presence of trace copper. Cuprizone can be used to induce some schizophrenia-like behavior in mice. Cuprizone acts on copper enzymes, including SOD1, cytochrome oxidase, and DβH, thereby causing oxidative stress and increasing DA levels in certain brain regions such as the medial prefrontal cortex (PFC) .
ND-011992 is a reversible, selective quinazoline-type inhibitor targeting quinone reductases and quinol oxidases. ND-011992 inhibits respiratory complex I and bo3 oxidase in addition to bd-I and bd-II oxidases in E. coli strain BL21*Δcyo with the IC50 of 0.12, 2.47, 0.63 and 1.3 μM, respectively. ND-011992 can be used for tuberculosis study .
TRV120027 TFA, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages ß-arrestins while blocking G-protein signaling . TRV120027 TFA induces acute catecholamine secretion through cation channel subfamily C3 (TRPC3) coupling, promotes the formation of a macromolecular complex composed of AT1R–β-arrestin-1–TRPC3–PLCγ at the plasma membrane. TRV120027 TFA inhibits angiotensin II–mediated vasoconstriction and increases cardiomyocyte contractility. TRV120027 TFA has the potential for the acute decompensated heart failure (ADHF) treatment .
TRV120027, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages ß-arrestins while blocking G-protein signaling . TRV120027 induces acute catecholamine secretion through cation channel subfamily C3 (TRPC3) coupling, promotes the formation of a macromolecular complex composed of AT1R–β-arrestin-1–TRPC3–PLCγ at the plasma membrane. TRV120027 inhibits angiotensin II–mediated vasoconstriction and increases cardiomyocyte contractility. TRV120027 has the potential for the acute decompensated heart failure (ADHF) treatment .
NHEJ inhibitor-1 (Compound C2) is a trifunctional Pt(II) complex, alleviates the non-homologous end connection (NHEJ)/homologous recombination (HR)-related double strand breaks (DSBs) repairs to evade Cisplatin-resistance in non-small cell lung cancer (NSCLC). NHEJ inhibitor-1 inhibits the damage repair proteins Ku70 and Rad51 to make tumors re-sensitive to Cisplatin。NHEJ inhibitor-1 also induces ROS generation and MMP deduction .
SEC inhibitor KL-2 (KL-2), a peptidomimetic lead compound, is a potent, selective super elongation complex (SEC) inhibitor and disrupts the interaction between the SEC scaffolding protein AFF4 and P-TEFb, resulting in impaired release of Pol II from promoter-proximal pause sites and a reduced average rate of processive transcription elongation. SEC inhibitor KL-2 exhibits an dose-dependent inhibitory effect on AFF4-CCNT1 interaction with a Ki of 1.50 μM .
SEC inhibitor KL-1 (KL-1), a peptidomimetic lead compound, is a potent, selective super elongation complex (SEC) inhibitor and disrupts the interaction between the SEC scaffolding protein AFF4 and P-TEFb, resulting in impaired release of Pol II from promoter-proximal pause sites and a reduced average rate of processive transcription elongation. SEC inhibitor KL-1 exhibits an dose-dependent inhibitory effect on AFF4-CCNT1 interaction with a Ki of 3.48 μM .
Rheb inhibitor NR1 is a Rheb inhibitor with an IC50 of 2.1 µM in the Rheb-IVK assay. Rheb inhibitor NR1 can directly bind Rheb in the switch II domain and selectively inhibit the activation of mechanistic target of rapamycin complex 1 (mTORC1). Rheb inhibitor NR1 inhibits the phosphorylation of mTORC1 driven T389pS6K1 and increases the phosphorylation of S473pAKT in a dose-dependent manner. Rheb inhibitor NR1 does not influence mTORC2 activity . (Rheb-IVK: Rheb-dependent mTORC1 kinase activity)
MRTX1133 is a noncovalent, potent, and selective KRAS G12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD against KRAS G12D of 0.2 pM. MRTX1133 prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRAS G12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells. MRTX1133 has single digit nanomolar activity in cellular assays and marked in vivo efficacy in tumor models harboring KRAS G12D mutations .
The transforming growth factor beta (TGF-β) signaling pathway is involved in many cellular processes in both the adult organism and the developing embryo including cell growth, cell differentiation, apoptosis, cellular homeostasis and other cellular functions. The TGF-β superfamily comprises TGF-βs, bone morphogenetic proteins (BMPs), activins and related proteins. Signaling begins with the binding of a TGF beta superfamily ligand to a TGF beta type II receptor. The type II receptor is a serine/threonine receptor kinase, which catalyzes the phosphorylation of the Type I receptor. The type I receptor then phosphorylates receptor-regulated SMADs (R-SMADs) which can now bind the coSMAD (e.g. SMAD4). R-SMAD/coSMAD complexes accumulate in the nucleus where they act as transcription factors and participate in the regulation of target gene expression. Deregulation of TGF-β signaling contributes to developmental defects and human diseases, including cancers, some bone diseases, chronic kidney disease, etc.
MCE designs a unique collection of 223 TGF-beta/Smad signaling pathway compounds. TGF-beta/Smad Compound Library acts as a useful tool for TGF-beta/Smad-related drug screening and disease research.
Filipin complex is a potent polyene macrolide antifungal antibiotic. Filipin complex inserts into membranes and sequester cholesterol into complexes and inhibits PRRSV entry. The Filipin complex consists of about 75.8% Filipin III (HY-N6718), 10.8% Filipin IV, 9.1% Filipin II, and 1.2% Filipin I .
Bathophenanthrolinedisulfonic acid disodium salt is used as a colorimetric reagent for the detection of iron. It is widely used for the determination of iron in aqueous solutions without the use of extraction solvents. It is used as a precursor for the preparation of the anion Europium(III) disulfonated bathophenanthroline tris(dibenzoylformic acid) complex and ruthenium II tris(rubphenanthroline disulfonate). It plays a crucial role in the catalytic oxidation of 2-hexanol by enabling it to form a water-soluble complex with palladium.
LLO (190-201) (Listeriolysin O 190 peptide) is a biological active peptide. (This peptide is a major histocompatibility complex class II (MHC-II)-restricted peptide, LLO190 (NEKYAQAYPNVS), from the listeriolysin O protein of Listeria monocytogenes, which generates an LLO190-specific Th response. This peptide subsequently challenge recombinant L. monocytogenes expressing the MHC-I-restricted epitope of ovalbumin (Ova257, SIINFEKL).)
Valylhistidine is a dipeptide consisting of valine and histidine (Val-His). Valylhistidine forms a dipeptide complex with Cu(II) that mimics superoxide dismutase, but lacks activity .
CLIP (86-100) is amino acids 86 to 100 fragment of class II-associated invariant chain peptide (CLIP). CLIP is a small self-peptide and cleavage product of the invariant chain that resides in the HLA-II antigen binding groove and is believed to play a critical role in the assembly and transport of MHC class II alphabetaIi complexes through its interaction with the class II peptide-binding site .
CLIP (86-100) TFA is amino acids 86 to 100 fragment of class II-associated invariant chain peptide (CLIP). CLIP is a small self-peptide and cleavage product of the invariant chain that resides in the HLA-II antigen binding groove and is believed to play a critical role in the assembly and transport of MHC class II alphabetaIi complexes through its interaction with the class II peptide-binding site .
InsB (9-23) is an insulin B-chain peptide that binds to a class II histocompatibility complex (MHC) allele called I-Ag7. InsB (9-23) can be used to treat a number of autoimmune related diseases like Type 1 diabetes .
H-Ser-Tyr-OH is a dipeptide consisting of glutamic acid, glycine and histidine. H-Ser-Tyr-OH can form a copper(II) complex with copper ions to form a strong free radical scavenging activity. H-Ser-Tyr-OH also increases the intracellular uptake of the delta opioid receptor ligand deltorphin .
TRV120027 TFA, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages ß-arrestins while blocking G-protein signaling . TRV120027 TFA induces acute catecholamine secretion through cation channel subfamily C3 (TRPC3) coupling, promotes the formation of a macromolecular complex composed of AT1R–β-arrestin-1–TRPC3–PLCγ at the plasma membrane. TRV120027 TFA inhibits angiotensin II–mediated vasoconstriction and increases cardiomyocyte contractility. TRV120027 TFA has the potential for the acute decompensated heart failure (ADHF) treatment .
TRV120027, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages ß-arrestins while blocking G-protein signaling . TRV120027 induces acute catecholamine secretion through cation channel subfamily C3 (TRPC3) coupling, promotes the formation of a macromolecular complex composed of AT1R–β-arrestin-1–TRPC3–PLCγ at the plasma membrane. TRV120027 inhibits angiotensin II–mediated vasoconstriction and increases cardiomyocyte contractility. TRV120027 has the potential for the acute decompensated heart failure (ADHF) treatment .
Filipin complex is a potent polyene macrolide antifungal antibiotic. Filipin complex inserts into membranes and sequester cholesterol into complexes and inhibits PRRSV entry. The Filipin complex consists of about 75.8% Filipin III (HY-N6718), 10.8% Filipin IV, 9.1% Filipin II, and 1.2% Filipin I .
Netropsin dihydrochloride is a small-molecule MGB (minor-groove binder), inhibits the catalytic activity of isolated topoisomerase and interferes with the stabilization of the cleavable complexes of topoisomerase II and I in nuclei . Netropsin dihydrochloride exhibits antiviral activity against the vaccinia virus .
Lacto-N-triose II is a core structural unit of human milk oligosaccharides (HMOs). Lacto-N-triose II owns nutraceutical potentials and can be used in the production of complex HMOs .
Aclacinomycin A (Aclarubicin) hydrochloride is an orally active and potent anthracycline antitumor antibiotic. Aclacinomycin A hydrochloride is an inhibitor of topoisomerase I and II. Aclacinomycin A hydrochloride inhibits synthesis of nucleic acid, especially RNA. Aclacinomycin A hydrochloride might inhibit the 26S protease complex as well as the ubiquitin-ATP-dependent proteolysis .
The CDK8-CCNC-MED12 protein is an important component of the mediator complex, acting as a bridge for gene transcription regulation, transmitting information from gene-specific regulatory factors to RNA polymerase II. It is recruited to the promoter, assembles a preinitiation complex, and promotes transcription. CDK8-CCNC-MED12 Protein, Human (Sf9) is the recombinant human-derived CDK8-CCNC-MED12 protein, expressed by Sf9 insect cells , with tag free.
The CDK8-CCNC-MED12 protein is an important component of the mediator complex, acting as a bridge for gene transcription regulation, transmitting information from gene-specific regulatory factors to RNA polymerase II. It is recruited to the promoter, assembles a preinitiation complex, and promotes transcription. CDK8-CCNC-MED12 Protein, Human (Sf9, GST, FLAG, His) is the recombinant human-derived CDK8-CCNC-MED12 protein, expressed by Sf9 insect cells , with N-6*His, N-Flag, N-GST labeled tag.
CDK19 plays a key role in cellular homeostasis and developmental programming. CDK19 can interact with p53 to inhibit p53-mediated transcription of p21, and regulates the proliferation of hematopoietic stem cells and acute myeloid leukemia cells. Besides, CDK19 is the paralog of CDK8. CDK8 and CDK19 can cooperate with each other in stimulating NFκB-induced transcription and Dengue virus replication. CDK19-CCNC-MED12 Protein, Human (Sf9) is the recombinant human-derived CDK19-CCNC-MED12 protein, expressed by Sf9 insect cells , with tag free. ,
Cytokeratin 5 Antibody is an unconjugated, approximately 62 kDa, rabbit-derived, anti-Cytokeratin 5 monoclonal antibody. Cytokeratin 5 Antibody can be used for: WB, IHC-P, IF-Tissue, IF-Cell, FC expriments in human, mouse, rat background without labeling.
MRTX1133 is a noncovalent, potent, and selective KRAS G12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD against KRAS G12D of 0.2 pM. MRTX1133 prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRAS G12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells. MRTX1133 has single digit nanomolar activity in cellular assays and marked in vivo efficacy in tumor models harboring KRAS G12D mutations .
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