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Inhibitors & Agonists

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Cat. No. Product Name Field of Application Chemical Structure
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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DC11426 DM1-PEG4-DBCO Featured
DM1-(PEG)4-DBCO (DBCO-PEG4-DM1) is made by DM1 conjugated to DBCO-(PEG)4 linker.DM1 (mertansine), a thiol-containing maytansinoid, is a potent microtubule-disrupting agent.
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DC11456 MeO-Suc-Arg-Pro-Tyr-pNA Featured
MeO-Suc-Arg-Pro-Tyr-pNA is a synthetic colorimetric peptide substrate displaying chymotrypsin-like specificity and is used in the measurement of Kallikreins. It is succinylated at N-terminus and has a nitroanilide tag at the C-terminus.
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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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DC49650 Y1R probe-1 Featured
Y1R probe-1 (Compound 39) is a high-affinity fluorescence probe for the Neuropeptide Y Y1 Receptor. Y1R probe-1 has the potential for the research of cancer disease.
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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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DC46604 CMD178 Featured
CMD178 is a lead peptide that consistently reduced the expression of Foxp3 and STAT5 induced by IL-2/s IL-2Rα signaling. CMD178 also is an inhibitor of STAT5 and inhibit Treg cell development.
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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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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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DCZ-057 Perillene
Perillene is a component of the essential oil, has antibacterial and antitumor effects.
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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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DC72686 SP 600125, negative control Featured
SP 600125, negative control (SPM1) is an alkyl derivative of pyrazoloanthrone, which can be used as a negative control for SP600125.
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DC71376 ABBV-318 Featured
ABBV-318 is a potent Nav1.7/ Nav1.8 blocker, with IC50s of 2.8 μM and 3.8 μM for hNav1.7 and hNav1.8, respectively. ABBV-318 can be used for the research of pain.
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DC47604 GPS491 Featured
GPS491 (EC50 = 0.47 μM) suppresses expression of the HIV-1 structural protein Gag and alters HIV-1 RNA accumulation, decreasing the abundance of RNAs encoding the structural proteins while increasing levels of viral RNAs encoding the regulatory proteins.
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DC21710 SU-909 Featured
SU-909 (SU909, IKKα-IN-48) is a potent, selective IKKα inhibitor with Ki of 0.08±0.07 uM, 10-20-fold selectivity over IKKβ (IC50=1.0±0.28 uM); inhibits FCS-stimulated phosphorylation of p100 in U2OS cells with IC50 of 8.8 uM, inhibits the noncanonical NF-kB pathway without affecting IKKβ-dependent IKappa-Bα loss in the canonical pathway.
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DC43001 VUF11418 Featured
First reported nonpeptidomimetic agonist on the G protein-coupled chemokine receptor CXCR-3
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DC20311 Apraglutide Featured
A peptidic glucagon like peptide 2 (GLP-2) analogue for treatment of type2 diabetes..
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DC72873 MTK458 Featured
MTK458 (MTK-458) is a potent, selective and brain penetrant PINK1 activator, MTK-458 promotes the first step in mitophagy. MTK458 selectively activates PINK1 by stimulating dimerization and stabilization of the PINK1/TOM complex. MTK458 binds to PINK1 and stabilizes an active heterocomplex, thereby increasing mitophagy. MTK458 reduces the PINK1 substrate pS65-Ubiquitin (pUb) in primary neurons and in vivo. MTK458 drives clearance of pathologic α-synuclein in vitro and in vivo, decreases pS129 α-synuclein aggregates and normalized both brain and corresponding plasma pUb levels in both cellular and animal models of α-synuclein aggregation (PD-like pathology).
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DC73665 KCNQ2 activator Ebio1 Featured
Ebio1 is a selective voltage-gated potassium channel KCNQ2 activator. Ebio1 activates KCNQ2 by generating an extended channel gate with greater conductance at a saturation voltage (+50 mV).
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DC21259 LY 3130481 Featured
LY3130481 (CERC611) is a potent, selective, noncompetitive TARP γ8-associated AMPA receptors with IC50 of 65.3 nM (GluA1/TARP γ-8), with no activity for γ-2 (cerebellum) or other TARP members.
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DC41899 Protein E7(43-62) Featured
Protein E7(43-62) is an E7-derived peptide with anti-tumor effects (short peptide spanning the 43th to 62th amino acid residues in the E7 protein).
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DC31174 Doxorubicin Featured
Doxorubicin free base, also called doxorubicin, is an anthracycline antibiotic with antineoplastic activity. Approved API for cancer therapeutic use is doxorubicin HCl. Doxorubicin, isolated from the bacterium Streptomyces peucetius var. caesius, is the h
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