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Inhibitors & Agonists

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Cat. No. Product Name Field of Application Chemical Structure
DC41106 L-Thyroxine sodium
L-Thyroxine sodium (Levothyroxine sodium) is a synthetic hormone for the research of hypothyroidism. DIO enzymes convert biologically active thyroid hormone (Triiodothyronine,T3) from L-Thyroxine (T4).
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DC41105 Prexasertib dimesylate
Prexasertib dimesylate (LY2606368 dimesylate) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib dimesylate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib dimesylate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib dimesylate shows potent anti-tumor activity.
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DC41104 Prexasertib Mesylate Hydrate
Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib Mesylate Hydrate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib Mesylate Hydrate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib Mesylate Hydrate shows potent anti-tumor activity.
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DC41103 Quercetin D5
Quercetin D5 is a deuterium labeled Quercetin. Quercetin, a natural flavonoid, is a stimulator of recombinant SIRT1 and also a PI3K inhibitor with IC50 of 2.4 μM, 3.0 μM and 5.4 μM for PI3K γ, PI3K δ and PI3K β, respectively.
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DC41102 Acalabrutinib D4
Acalabrutinib D4 (ACP-196 D4) is a deuterium labeled Acalabrutinib. Acalabrutinib (ACP-196) is an orally active, irreversible, and highly selective second-generation BTK inhibitor.
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DC41100 Chloroquine dihydrochloride
Chloroquine dihydrochloride is an antimalarial and anti-inflammatory agent widely used to treat malaria and rheumatoid arthritis. Chloroquine dihydrochloride is an autophagy and toll-like receptors (TLRs) inhibitor. Chloroquine dihydrochloride is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC50=1.13 μM).
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DC41099 Chloroquine D5
Chloroquine D5 is deuterium labeled Chloroquine. Chloroquine is an antimalarial and anti-inflammatory agent widely used to treat malaria and rheumatoid arthritis. Chloroquine is an autophagy and toll-like receptors (TLRs) inhibitor. Chloroquine is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC50=1.13 μM).
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DC41097 Rosuvastatin D3
Rosuvastatin D3 (ZD 4522 D3) is a deuterium labeled Rosuvastatin. Rosuvastatin (ZD 4522) is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM. Rosuvastatin potently blocks human ether-a-go-go related gene (hERG) current with an IC50 of 195 nM, delayed cardiac repolarization, and thereby prolonged action potential durations (APDs) and corrected QT interval (QTc) intervals.
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DC41096 Bepridil hydrochloride hydrate
Bepridil hydrochloride hydrate ((±)-Bepridil hydrochloride hydrate) is a non-selective, long-acting Ca+ channel antagonist and Na+, K+ channel inhibitor, with antianginal and type I antiarrhythmic effects. Bepridil hydrochloride hydrate also acts as a cardiac Na+/Ca2+ exchange (NCX1) inhibitor. Bepridil hydrochloride hydrate can be used for the research of cardiovascular disorders.
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DC41094 UNC926 hydrochloride
UNC926 hydrochloride is a methyl-lysine (Kme) reader domain inhibitor that inhibits L3MBTL1 with an IC50 of 3.9 μM.
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DC41093 Apalutamide D4
Apalutamide D4 (ARN-509 D4) is a deuterium labeled Apalutamide. Apalutamide is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM.
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DC41092 Cerdulatinib hydrochloride
Cerdulatinib hydrochloride (PRT062070) is a selective, oral active and reversible ATP-competitive inhibitor of dual SYK and JAK, with IC50s of 32 nM, 0.5 nM, 12 nM, 6 nM and 8 nM for SYK and Tyk2, JAK1, 2, 3, respectively. Cerdulatinib hydrochloride could be used to research autoimmune disease and B-cell malignancies.
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DC41091 VBY-825
VBY-825 is a novel, reversible cathepsin inhibitor with high potency against cathepsins B, L, S and V.
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DC41089 Ribociclib D6
Ribociclib D6 (LEE011 D6) is a deuterium labeled Ribociclib. Ribociclib is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.
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DC41088 Osimertinib D6
Osimertinib D6 (AZD-9291 D6) is a deuterium labeled Osimertinib. Osimertinib is an irreversible and mutant selective EGFR inhibitor with IC50s of 12 and 1 nM against EGFRL858R and EGFRL858R/T790M, respectively.
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DC41087 ICI 89406
ICI 89406 is a selective β1 adrenergic receptor antagonist amenable to labelling with positron emitters, for PET.
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DC41086 Vercirnon sodium
Vercirnon (GSK1605786A) sodium is an orally bioavailable, selective, and potent antagonist of CCR9. Vercirnon sodium inhibits CCR9-mediated Ca2+ mobilization and chemotaxis on Molt-4 cells with IC50 values of 5.4 and 3.4 nM, respectively. Vercirnon sodium is selective for CCR9 over CCR1-12 and CX3CR1-7 (IC50s>10 μM for all). Vercirnon sodium is an equipotent inhibitor of CCL25-directed chemotaxis of both splice forms of CCR9 (CCR9A and CCR9B) with IC50 values of 2.8 and 2.6 nM, respectively.
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DC41085 8-Hydroxy-DPAT hydrobromide
8-Hydroxy-DPAT hydrobromide (8-OH-DPAT hydrobromide) is a potent and selective 5-HT1A agonist with a pIC50 of 8.19. 8-Hydroxy-DPAT hydrobromide has selectivity of almost 1000 fold for a subtype of the 5-HT1 binding site.
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DC41083 Freselestat quarterhydrate
Freselestat quarterhydrate (ONO-6818 quarterhydrate) is a potent and orally active neutrophil elastase inhibitor with a Ki of 12.2 nM. Freselestat quarterhydrate is >100-fold less-active against other proteases such as trypsin, protein-ase 3, pancreatic elastase, plasmin, thrombin, collagenase, cathepsin G, and murine macrophage elastase. Freselestat quarterhydrate has a potent anti-inflammatory activity.
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DC41082 Hoechst 33342 analog trihydrochloride
Hoechst 33342 analog trihydrochloride is an anglog of Hoechst 33342, which is a DNA minor groove binder used fluorochrome for visualizing cellular DNA.
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DC41080 Chroman 1 dihydrochloride
Chroman 1 dihydrochloride is a highly potent ROCK2 inhibitor, with an IC50 of 1 nM. Chroman 1 dihydrochloride also shows inhibitory activities against MRCK, with an IC50 of 150 nM.
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DC41079 Talibegron hydrochloride
Talibegron hydrochloride (ZD2079 hydrochloride) is a potent β3-adrenoceptor agonist with a pD2 of 3.72 on phenylephrine-preconstricted rat mesenteric artery. Talibegron hydrochloride has potent vasorelaxant effect.
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DC41078 Telomestatin
Telomestatin is a very potent telomerase inhibitor and can be isolated from Streptomyces anulatus 3533-SV4. Telomestatin selectively facilitates the formation of intramolecular G-quadruplexes, in particular, that produced from the human telomeric sequence d[T2AG3]4. Telomestatin is an ADC cytotoxin and can be used for cancer research.
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DC41077 (S)-Flurbiprofen
(S)-Flurbiprofen is an active enantiomer of Flurbiprofen, with IC50 values of 0.48 μM and 0.47 μM for COX-1 and COX-2, respectively.
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DC41076 Spergualin trihydrochloride
Spergualin trihydrochloride is a natural product that first identified as an antibiotic from culture filtrates of Bacillus laterosporus BMG162-aF2.
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DC41075 (±)-Naproxen-d3
(±)-Naproxen-d3 ((Rac)-Naproxen-d3) is the deuterium labeled (±)-Naproxen. (±)-Naproxen is a non-steroidal anti-inflammatory drug (NSAID).
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DC41074 Gemigliptin tartrate
Gemigliptin tartrate (LC15-0444 tartrate) is a highly selective, reversible and competitive dipeptidyl peptidase-4 (DPP-4) inhibitor, with an IC50 of 10.3 nM for human recombinant DPP-4. Gemigliptin tartrate exhibits potent anti-glycation properties. Gemigliptin tartrate can be used for the research of advanced glycation end products (AGE)-related diabetic complications.
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DC41073 Avibactam free acid
Avibactam free acid (NXL-104 free acid) is a covalent and reversible non-β-lactam β-lactamase inhibitor which inhibits β-lactamase TEM-1 and CTX-M-15 with IC50s of 8 nM and 5 nM, respectively.
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DC41072 Retosiban
Retosiban (GSK221149A) is a potent and selective oxytocin antagonist with a Ki of 0.65 nM.
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DC41071 (3S,5R)-Fluvastatin D6
(3S,5R)-Fluvastatin D6 is the deuterium labeled (3S,5R)-Fluvastatin sodium. Fluvastatin is a first fully synthetic, competitive?HMG-CoA reductase?inhibitor with an IC50?of 8 nM. Fluvastatin protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway.
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