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Novel inhibitors

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Cat. No. Product Name Field of Application Chemical Structure
DC12257 Gln-AMS TFA
Gln-AMS (TFA) is a type Ia aminoacyl-tRNA synthetase (AARS) inhibitor. Gln-AMS inhibits glutaminyl-tRNA synthetase (GlnRS) with a Ki of 1.32 µM.
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DC20087 GKI-1
GKI-1 is a Greatwall (GWL) kinase inhibitor with IC50s of 4.9 and 2.5 µM against hGWLFL and hGWL-KinDom, respectively. GKI-1 robustly inhibits ROCK1 with an IC50 of 11 µM, but only weakly affected PKA.
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DC12300 G3-C12 TFA
G3-C12 (TFA) is a galectin-3 binding peptide, with high affinity (Kd) of 88 nM, but shows no affinity for other galectin family members or to other lectins.
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DC12249 E3 ligase Ligand 1 dihydrochloride
E3 ligase Ligand 1 dihydrochloride is a Hippel-Landau (VHL) E3 ligase-binding moiety based on PROTAC technology.
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DC12329 ChX710
ChX710 could prime the type I interferon response to cytosolic DNA, which induces the ISRE promoter sequence, specific cellular Interferon-Stimulated Genes (ISGs), and the phosphorylation of Interferon Regulatory Factor (IRF) 3.
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DC20119 Carnostatine (SAN9812)
Carnostatine (SAN9812) is a specific and highly selective carnosinase (CN1) inhibitor with a Ki of 11 nM.
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DC20034 Boc-MLF TFA
Boc-MLF (TFA) is a peptide, used as a specific formyl peptide receptor (FPR) antagonist, also inhibits the signaling through formyl peptide receptor like 1 (FPRL1) at higher concentrations.
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DC20114 ATWLPPR Peptide TFA
ATWLPPR Peptide TFA, a heptapeptide, acts as a selective neuropilin-1 inhibitor, inhibits VEGF165 binding to NRP-1, used in the research of angiogenesis. ATWLPPR Peptide TFA has potential in reducing the early retinal damage caused by diabetes.
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DC12067 4'-Methylchrysoeriol
4'-Methylchrysoeriol is a potent inhibitor of Cytochrome P450 enzymes, with an IC50 of 19 nM for human P450 1B1-dependent EROD.
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DC10428 (1S,3R,5R)-PIM447 dihydrochloride
(1S,3R,5R)-PIM447 (dihydrochloride) an PIM inhibitor extracted from patent US 20100056576 A1, compound example 72, has IC50 values of 0.095 μM for Pim1, 0.522 μM for Pim2 and 0.369 μM for Pim3.
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DC39041 BMS 247616 (S1 antitumor agent) Featured
S-1 is a novel oral fluorouracil antitumor drug that combines three pharmacological agents: tegafur (FT), a prodrug of 5-fluorouracil (5-FU); 5-chloro-2,4-dihydroxypyridine (CDHP), an inhibitor of dihydropyrimidine dehydrogenase, and potassium oxonate (Ox
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DC43941 Ecamsule.2Na
Ecamsule.2Na is the Sodium salt form of Ecamsule. Ecamsule is an active ingredient of sunscreens that protects the skin from sunburn and erythema.
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DC43942 Polidocanol
Polidocanol (Polyoxyethylene lauryl ether, Polyoxyethyleneglycol Dodecyl Ether, Brij30, Laureth-23, Varithena) is a sclerosant used for treating uncomplicated spider veins and reticular veins in the lower extremities.
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DC43977 L-Palmitoylcarnitine TFA
L-Palmitoylcarnitine TFA, a long-chain acylcarnitine and a fatty acid metabolite, accumulates in the sarcolemma and deranges the membrane lipid environment during ischaemia.
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DC43988 GW806742X hydrochloride
GW806742X hydrochloride, an ATP mimetic and a potent MLKL (Mixed Lineage Kinase Domain-Like protein) inhibitor, binds the MLKL pseudokinase domain with a Kd of 9.3 μM. GW806742X hydrochloride has activity against VEGFR2 (IC50=2 nM). GW806742X hydrochlorid
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DC43996 NAZ2329
NAZ2329, the first cell-permeable inhibitor of R5 subfamily of receptor-type protein tyrosine phosphatases (RPTPs), allosterically and preferentially inhibits PTPRZ (IC50=7.5 µM for hPTPRZ1) and PTPRG (IC50=4.8 µM for hPTPRG) over other PTPs. NAZ2329 bind
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DC43997 Epsilon-V1-2
Epsilon-V1-2 (ε-V1-2), a PKCε-derived peptide, is a selective PKCε inhibitor. Epsilon-V1-2 inhibits the translocationof PKCε, but not α-, β-, and δPKC.
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DC70212 ASH1L inhibitor AS-99
ASH1L inhibitor AS-99 (AS-99) is a first-in-class, potent, selective inhibitor of ASH1L histone methyltransferase with IC50 of 0.79 uM.AS-99 strongly bind to the ASH1L SET domain with Kd values of 0.89 uM.AS-99 displayed no significant inhibition (>100-fold selectivity) at 50 uM against a panel of 20 histone methyltransferases, including NSD1, NSD2, NSD3, and SETD2.AS-99 inhibits the growth of leukemia cells (MV4;11, MOLM13, and KOPN8) harboring different MLL1 translocations with the GI50 values of 1.8-3.6 uM, showed a several fold weaker effect on the proliferation of leukemia cells without MLL1 translocations, such as SET2 and K562, without toxicity in normal cells.AS-99 impairs transcriptional program of MLL fusion proteins and reduces leukemia burden.AS-99 reduced the leukemia burden in the xenotransplantation mouse model of MLL leukemia without affecting blood counts in normal mice.
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DC47225 AS-99 TFA
AS-99 TFA is a first-in-class, potent and selective ASH1L histone methyltransferase inhibitor (IC50= 0.79 µM, Kd= 0.89 µM) with anti-leukemic activity. AS-99 TFA blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo.
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DC47935 NJH-2-057
NJH-2-057 is an EN523 OTUB1 recruiter linked to lumacaftor, a drug used to treat cystic fibrosis that binds ΔF508-CFTR.
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DC71755 Sipagladenant Featured
Sipagladenant (Compound I) is an orally active adenosine receptor A2A inverse agonist. Sipagladenant can be used in frontal lobe dysfunction research.
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DC74523 XY-07-35 Featured
XY-07-35 is a potent, selective HDAC6 proteolysis targeting chimera (PROTAC) degrader with IC50 of 48.5 nM.
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DC43769 2OH-BNPP1 Featured
2OH-BNPP1 is an inhibitor of BUB1 kinase, a Ser/Thr kinase, used for the treatment of cancer.
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DC47754 Disitamab vedotin Featured
Disitamab vedotin (RC48) is an antibody-drug conjugate (ADC) comprising a monoclonal antibody against human epidermal growth factor receptor 2 (HER2) conjugated via a cleavable linker to the cytotoxic agent monomethyl auristatin E. Disitamab vedotin enhances antitumor immunity.
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DC70371 DW0254 Featured
DW0254 (DW-0254,DW 0254) is a small molecules capable of inhibiting RAS-related C3 botulinum toxin substrate (RAC) small GTPase activation in ALL cell lines, directly binds to the hydrophobic pocket of PDE6D (Kd=436 nM, ITC), a RAS chaperone protein.DW0254 demonstrated dose-dependent RAC inhibition, arrest of proliferation and induced apoptosis in human leukemic cell lines (RS4;11 IC50=1.5-1.8 uM), also showed promising anti-leukemic activity in RAS-mutated cells (CCRF-CEM NRAS G12D, IC50=3.3-4.2 uM).DW0254 disrupted the interaction between PDE6D and RAS, disturbing RAS subcellular localization.DW0254 demonstrated anti-leukemic activity, decreased tumor progression in a murine xenograft model.
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DC21021 Peptide P60 Featured
Peptide P60 (FOXP3 inhibitor P60) is a 15-mer synthetic peptide, cell-permeable inhibitor of FOXP3, binds specifically to FOXP3; inhibits murine and human-derived Treg and improves effector T cell stimulation, overcomes the inhibitory effect of FOXP3 on the activity of the transcription factors NF-κB and NFAT, inhibits upregulation of mRNA for Foxp3 and IL-10 on effector T cells and enhances mRNA for IFN-γ after anti-CD3 stimulation; induces a scurfy-like disease in newborn mice, improves vaccine efficacy in mice model of CT26 tumor and HCV infection.
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DC41012 ALK2-IN-4 Featured
ALK2-IN-4 is a potent ALK2 inhibitor extracted from patent WO2020086963A1, compound Formula I free base.
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DC70714 PSB-16671 Featured
PSB-16671 is a novel orthosteric and allosteric activator of GPR84, activates human GPR84 with EC50 of 41.3 nM in cAMP accumulation assays. PSB-16671 is selective versus related fatty acid receptors and the arylhydrocarbon receptor. PSB-16671 shows an EC50 of 5.47 uM in β-Arrestin assays, and allosteric KB value of 634 nM.
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DC22975 GB111-NH2 Featured
GB111-NH2 (Z-Phe-Lys-AOMK) is a novel cysteine cathepsin inhibitor that blocks the activity of cathepsins B, L and S. GB111-NH2 (Z-Phe-Lys-AOMK) inhibits autophagy and increases oxidative stress, specifically trigger macrophage cell death.
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DC65697 HDAC6 inhibitor 4510 Featured
A novel and seletive HDAC6 inhibitor.
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