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Results for "

activated intermediate

" in MedChemExpress (MCE) Product Catalog:

22

Inhibitors & Agonists

1

Inhibitory Antibodies

7

Natural
Products

1

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-113492
    5(S)15(S)-DiHETE

    		Interleukin Related Cardiovascular Disease Inflammation/Immunology
    5(S)15(S)-DiHETE is an “activated” intermediate, inhibits platelet aggregation with an IC50 of 1.3 μM. 5(S)15(S)-DiHETE enhances the rate of either LXA4 or LXB4 biosynthesis .
    5(S)15(S)-DiHETE
  • HY-13519
    TRAM-34
    Maximum Cited Publications
    18 Publications Verification

    		 Potassium Channel Neurological Disease
    TRAM-34 is a highly selective blocker of intermediate-conductance calcium-activated K + channel (IKCa1) (Kd=20 nM).
    TRAM-34
  • HY-48564
    TAM558 intermediate-5

    		ADC Cytotoxin Cancer
    TAM558 intermediate-54 is an intermediate in the synthesis of TAM558 (HY-148127).TAM558 is the payload molecule used in the synthesis of OMTX705.OMTX705 is a humanized anti-fibroblast activation protein (FAP) antibody that binds to the cytolysin TAM470 (HY-148128) and has anti-tumor activity .
    TAM558 intermediate-5
  • HY-78869
    Mutated EGFR-IN-1

    Osimertinib analog

    		 EGFR Cancer
    Mutated EGFR-IN-1 (Osimertinib analog) is a useful intermediate for the inhibitors design for mutated EGFR, such as L858R EGFR, Exonl9 deletion activating mutant and T790M resistance mutant.
    Mutated EGFR-IN-1
  • HY-125665
    Pheophorbide A

    		Apoptosis Cardiovascular Disease Cancer
    Pheophorbide A is an intermediate product in the chlorophyll degradation pathway. Pheophorbide A can be used as a photosensitizer. Pheophorbide A is a lymphatic vascular activator. Pheophorbide A has antitumor activity. Pheophorbide A can be used for human lymphatic vascular insufficiencies research .
    Pheophorbide A
  • HY-400687
    TAM558 intermediate-1

    		Others Cancer
    TAM558 intermediate-1 is an intermediate in the synthesis of TAM558 (HY-148127).TAM558 is the payload molecule used in the synthesis of OMTX705.OMTX705 is a humanized anti-fibroblast activation protein (FAP) antibody that binds to the cytolysin TAM470 (HY-148128) and has anti-tumor activity .
    TAM558 intermediate-1
  • HY-400688
    TAM558 intermediate-2

    		Others Cancer
    TAM558 intermediate-24 is an intermediate in the synthesis of TAM558 (HY-148127).TAM558 is the payload molecule used in the synthesis of OMTX705.OMTX705 is a humanized anti-fibroblast activation protein (FAP) antibody that binds to the cytolysin TAM470 (HY-148128) and has anti-tumor activity .
    TAM558 intermediate-2
  • HY-400689
    TAM558 intermediate-3

    		Others Cancer
    TAM558 intermediate-34 is an intermediate in the synthesis of TAM558 (HY-148127).TAM558 is the payload molecule used in the synthesis of OMTX705.OMTX705 is a humanized anti-fibroblast activation protein (FAP) antibody that binds to the cytolysin TAM470 (HY-148128) and has anti-tumor activity .
    TAM558 intermediate-3
  • HY-400690
    TAM558 intermediate-4

    		Others Cancer
    TAM558 intermediate-4 is an intermediate in the synthesis of TAM558 (HY-148127).TAM558 is the payload molecule used in the synthesis of OMTX705.OMTX705 is a humanized anti-fibroblast activation protein (FAP) antibody that binds to the cytolysin TAM470 (HY-148128) and has anti-tumor activity .
    TAM558 intermediate-4
  • HY-156194
    FLAP-IN-1

    		FLAP Cardiovascular Disease
    FLAP-IN-1 (Intermediate 14) is a 5-lipoxygenase-activating protein (FLAP) inhibitor with an IC50 value of 654 nM. FLAP-IN-1 can be used in cardiovascular disease research .
    FLAP-IN-1
  • HY-103308
    TRAM-39

    		Potassium Channel Neurological Disease
    TRAM-39 is a selective blocker of intermediate conductance Ca2+-activated K+ (IKCa) channels. TRAM-39 inhibits KCa3.1 channel with an IC50 value of 60 nM. TRAM-39 can be used for the research of ataxia, epilepsy, memory disorders, schizophrenia and Parkinson’s disease .
    TRAM-39
  • HY-110105
    NS8593 hydrochloride

    		Potassium Channel Neurological Disease
    NS8593 hydrochloride is a potent and selective small conductance Ca 2+-activated K + channels (SK channels) inhibitor. NS8593 hydrochloride reversibly inhibits SK3-mediated currents with a Kd value of 77 nM. NS8593 hydrochloride inhibits all the SK1-3 subtypes Ca 2+-dependently (Kds of 0.42, 0.60, and 0.73 μM, respectively, at 0.5 μM Ca 2+), and does not affect the Ca 2+-activated K + channels of intermediate and large conductance (hIK and hBK channels, respectively) .
    NS8593 hydrochloride
  • HY-126585
    SAICAR
    1 Publications Verification

    		 Endogenous Metabolite Cancer
    SAICAR is an intermediate of de novo purine nucleotide biosynthesis, activates pyruvate kinase isoform M2 (PKM2) in an isozyme-selective manner, with an EC50 of 0.3 mM. SAICAR stimulates PKM2 and promotes cancer cell survival in glucose-limited conditions .
    SAICAR
  • HY-P99752
    Nemvaleukin alfa

    ALKS 4230; RDB-1450

    		 Interleukin Related Inflammation/Immunology Cancer
    Nemvaleukin alfa (ALKS 4230) is a IL-2 fusion protein that selectively binds to intermediate-affinity IL-2R. Nemvaleukin alfa is an activator of NK and effector T cells. Nemvaleukin alfa can be used for research of cancer .
    Nemvaleukin alfa
  • HY-126585S
    SAICAR-d1

    		Endogenous Metabolite Metabolic Disease
    SAICAR-d is the deuterium labeled SAICAR. SAICAR is an intermediate of de novo purine nucleotide biosynthesis, activates pyruvate kinase isoform M2 (PKM2) in an isozyme-selective manner, with an EC50 of 0.3 mM. SAICAR stimulates PKM2 and promotes cancer cell survival in glucose-limited conditions[1][2].
    SAICAR-d1
  • HY-113037
    Farnesyl pyrophosphate

    Farnesyl diphosphate

    		 TRP Channel Endogenous Metabolite Neurological Disease
    Farnesyl pyrophosphate (Farnesyl diphosphate), a 15-carbon isoprenoid, is a metabolic intermediate of the mevalonate (MVA) pathway. Farnesyl pyrophosphate is a TRPM2 (TRP Channel) agonist, activates TRPM2 opening for ion influx. Farnesyl pyrophosphate is a key branch substrate for cholesterol synthesis, ubiquinones synthesis, protein farnesylation decoration, and geranyl-geranyl pyrophosphate (GGPP) synthesis .
    Farnesyl pyrophosphate
  • HY-113037C
    Farnesyl Pyrophosphate ammonium

    Farnesyl diphosphate ammonium

    		 TRP Channel Endogenous Metabolite Neurological Disease
    Farnesyl Pyrophosphate ammonium salt, a 15-carbon isoprenoid, is a metabolic intermediate of the mevalonate (MVA) pathway. Farnesyl pyrophosphate ammonium salt is a TRPM2 (TRP Channel) agonist, and activates TRPM2 opening for ion influx. Farnesyl pyrophosphate ammonium salt is a key branch substrate for cholesterol synthesis, ubiquinones synthesis, protein farnesylation decoration, and geranyl-geranyl pyrophosphate (GGPP) synthesis .
    Farnesyl Pyrophosphate ammonium
  • HY-141581
    Lyso-PAF C-18

    		Platelet-activating Factor Receptor (PAFR) Endogenous Metabolite Cardiovascular Disease
    Lyso-PAF C-18 is an intermediate for the synthesis of C18-PAF (HY-130345). It has an easily substituted "Lyso-PAF" structure and is easy to purify and has high yield. C18-PAF is a ligand for platelet-activating factor and PAF G protein-coupled receptor (PAFR) and has renovasodilator properties and antihypertensive lipid properties .
    Lyso-PAF C-18
  • HY-120059
    NS4591

    		Others Neurological Disease
    NS4591 is a modulator of calcium-activated potassium channels with activity that enhances small (SK) and intermediate (IK) conductivity. NS4591 doubled IK-mediated currents in whole-cell patch-clamp experiments at a concentration of 45 +/- 6 nM, and doubled SK3-mediated currents at a concentration of 530 +/- 100 nM. NS4591 inhibits the number of action potentials generated by suprathreshold depolarizing pulses in acutely isolated bladder primary afferent neurons. NS4591 also reduced carbakol-induced detrusor ring contraction in the rat bladder, demonstrating sensitivity to apamin .
    NS4591
  • HY-117993
    MIND4

    		Others Neurological Disease
    MIND4 is a novel thiozoline that was found to inhibit the deacetylase SIRT2 and to have neuroprotective activity in in vitro brain slices and Drosophila models of Huntington's disease (HD). A systems biology approach revealed another SIRT2-independent property of MIND4, namely as an inducer of nuclear factor erythroid 2 p45-derived factor 2 (NRF2) activity. Structure-activity relationship studies further identified a potent NRF2 activator (MIND4-17) that lacks SIRT2 inhibitory activity. MIND compounds induce NRF2 activation responses in both neuronal and non-neuronal cells and reduce the generation of reactive oxygen and nitrogen intermediates. These agent-like thiozolines offer exciting opportunities for the development of multi-target agents with potential synergistic therapeutic benefits for HD and related disorders.
    MIND4
  • HY-B1247
    Protoporphyrin IX
    10+ Cited Publications

    		 Endogenous Metabolite Others
    Protoporphyrin IX is a final intermediate in the heme biosynthetic pathway, which acts as a radiation sensitizer enhancing ROS generation even in a hypoxic state and inducing DNA damage. Protoporphyrin IX also acts as a photo sensitizer undergoing photobleaching that occurs through direct degradation by light irradiation. Protoporphyrin IX is formed and accumulated following 5-aminolevulinic acid (5-ALA) (HY-W000450) administration in the tumor cells of rats. Protoporphyrin IX causes selective improvement of basal cell carcinoma when activated red fluorescence of a peak wavelength at 405 nm. Protoporphyrin IX is promising for research of sonodynamic and photodynamic agents for a wide range of cancers, such as bladder cancer and nodular basal cell carcinoma .
    Protoporphyrin IX
  • HY-118097
    GW0072

    		Others Cancer
    Targeted molecular dynamics simulations of the entry of GW0072, a macromolecular ligand with flexible ionic properties, into the ligand-binding domain of the nuclear receptor PPARc were performed. Starting from the apo-form, where the ligand is located outside the receptor, the simulation ultimately locks the ligand into the binding pocket, yielding a structure very close to the holo-form. The results show that the entry process is mainly guided by hydrophobic interactions, and that the entry and exit pathways are very similar. We suggest that the TMD approach may be useful in distinguishing ligands generated by in silico docking. To address the question of the ligand entry process, we report targeted molecular dynamics (TMD) simulations of the binding of the GW0072 ligand to the ligand-binding domain (LBD) of the peroxisome proliferator-activated receptor gamma (PPARc). PPARc is a member of the nuclear receptor superfamily and an important agent target for many diseases. We chose to study this complex because (i) GW0072 is a large ionic, highly flexible ligand that includes aliphatic chains and polar groups, and (ii) previous simulations have defined a possible escape pathway for this ligand. Starting from the apo-form of the receptor (PDB.ID 1PRG, chain A), with the ligand located outside, TMD simulations converged on a holo-form complex that is close to the target structure (PDB.ID 4PRG, chain A), defining a permeation pathway into the binding pocket that is very similar to the escape pathway. However, during the entry of GW0072 into the receptor (Fig. 5), the helices are very mobile, and once the ligand is placed in the pocket, AF-2 becomes more rigid during the remainder of the simulation (Fig. S1 in the Supplementary Materials). This finding is in good agreement with the observations of Oberfield et al. [12], suggesting that despite the absence of direct interaction with the ligand, the presence of the ligand in the binding site stabilizes an intermediate conformation of AF-2, which may be responsible for the property of GW0072 as a partial agonist.
    GW0072

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