LOM612 is a potent activator of FOXO nuclear translocation, with an EC50 value of 1.5 μM in cells.
1-Palmitoyl-2-oleoyl-sn-glycero-3-PE is a phospholipid, and can be used for drug delivery[1].
Etomidate Hcl(R16659 Hcl) is a GABAA receptors agonist, which is a short acting intravenous anaesthetic agent used for the induction of general anaesthesia.Target: GABA ReceptorEtomidate is a potent inhibitor of the adrenal response to surgery. The absence of clinical consequences associated with the blunted response suggests that a major increase in adrenal hormone production may not be necessary during surgery [1]. Etomidate is an intravenous induction agent that is associated with hemodynamic stability during intubation. The agent is therefore attractive for use in critically ill patients who have a high risk of hemodynamic instability during this procedure [2]. Etomidate use was not associated with all cause 28-day mortality or hospital mortality but was associated with significantly higher ICU mortality (91% vs. 64% for etomidate and controls groups, respectively; p = 0.02). Etomidate patients who received subsequent doses of hydrocortisone required lower doses of vasopressors and had more vasopressor-free days but no improvement in mortality [3].Clinical indications: FDA Approved Date: 1983Toxicity: Undesirable side effects of etomidate that may limit its use include pain on injection, myoclonus and adrenocortical suppression lasting 4-6 hours following an induction dose.
Domoic acid ((-)-Domoic acid; L-Domoic acid) is an excitatory neurotransmitter isolated from a form of marine vegetation, Nitzschia pungens[1]. Domoic acid produces neurotoxic effect through activating kainate receptor[2].
Magrolimab (Hu5F9-G4) is a first-in-class humanized anti-CD47 IgG4 antibody with an anti-tumor activity[1].
Psora-4 is a potent and selective inhibitor of Kv1.3 (voltage-gated potassium channels) with an EC50 of 3 nM[1]. Psora-4 has immunosuppressive activity and inhibits proliferation of human and rat myelin-specific effector memory T cells in vitro[2].
5-Amino-2'-deoxyuridine (monohydrochloride) is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
5'-O-TBDMS-Bz-dA is a nucleoside with protective and modification effects.
Catalpanp-1 is a potent anti-microbial agent. Catalpanp-1 has strong antimicrobial effect on yeast, bacteria, fungi and the like[1].
Bathophenanthroline is an agent used for the measurement of iron concentrations in aqueous , serum and urine samples by colorimetry.
Hydroxyalprazolam-d4 is the deuterium labeled Hydroxyalprazolam[1].
Endoxifen Z-isomer hydrochloride is the most important Tamoxifen metabolite responsible for eliciting the anti-estrogenic effects of this drug in breast cancer cells expressing estrogen receptor-alpha (ERα). Endoxifen inhibits hERG tail currents at 50 mV in a concentration-dependent manner with IC50 values of 1.6 μM.IC50 value: 1.6 μM [1]Target: hERG Potassium Channel, Estrogen Receptor/ERREndoxifen is considered a prodrug, since it has a much higher potency for the estrogen receptor than its parent drug. Endoxifen inhibits the hERG channel protein trafficking to the plasma membrane in a concentration-dependent manner with Endoxifen being more potent than Tamoxifen. [1] Endoxifen is also shown to be a more potent inhibitor of estrogen target genes when ERβ is expressed. Additionally, low concentrations of Endoxifen observed in Tamoxifen treated patients with deficient CYP2D6 activity (20 to 40 nM) markedly inhibit estrogen-induced cell proliferation rates in the presence of ERβ, whereas much higher Endoxifen concentrations are needed when ERβ is absent.[2]
Rocbrutinib is a Bruton's tyrosine kinase inhibitor with antineoplastic effect[1].
2-(Pyridin-2-yl)acetic acid-d6 (hydrochloride) is the deuterium labeled 2-(Pyridin-2-yl)acetic acid hydrochloride[1].
SLX-4090, an enterocytic-specific microsomal triglyceride transfer protein (MTP) inhibitor with an IC50 of 8.0 nM. SLX-4090 can be used for the research of dyslipidemia[1].
CPI-169 is a novel and potent EZH2 inhibitor, with IC50s of 0.24 nM, 0.51 nM, and 6.1 nM for EZH2 WT, EZH2 Y641N, and EZH1, respectively.
Mitragynine pseudoindoxyl is a potent MOR agonist. Mitragynine pseudoindoxyl displays reduced hyperlocomotion, inhibition of GI transit and reinforcing properties[1].
PD 119819 is a highly selective benzopyran-4-one brain dopamine autoreceptor agonist. PD 119819, a heterocyclic piperazine, inhibits spontaneous locomotor activity and brain dopamine synthesis[1][2].
6-Iodoamiloride is a potent acid-sensing ion channel 1 (ASIC1) inhibitor with an IC50 of 88 nM. 6-Iodoamiloride inhibits ASIC3-mediated currents from rat dorsal root ganglion neurons with an IC50 of 230 nM[1].
1-Ethyl-L-proline is a proline derivative[1].
Peniciside is a triterpenoid glycoside derived from the fungus Penicillium sp.169[1].
FabH-IN-1 (compound 3f) is an inhibitor of bacterial 3-oxoacyl-[acyl-carrier-protein] synthase 3 (FabH) enzyme which is a broad-spectrum antimicrobial target. FabH-IN-1 is effective against gram-positive and gram-negative. FabH-IN-1 is also a good antioxidant[1].
GSK2850163 is a novel inhibitor of inositol-requiring enzyme-1 alpha (IRE1α) which can inhibit IRE1α kinase activity and RNase activity with IC50s of 20 and 200 nM, respectively.
NH2-PEG6-C1-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Trimyristin--d15 is the deuterium labeled Trimyristin. Trimyristin, an active molluscicidal component of Myristica fragrans Houtt, significantly inhibits acetylcholinesterase (AChE), acid and alkaline phosphatase (ACP/ALP) activities in the nervous tissue of Lymnaea acuminata. IC50s of Trimyristin against AChE, ACP, and ALP are 0.11, 0.16 and 0.18 mM, respectively[1].
Ibudilast(KC-404;AV-411;MN-166) is a relatively nonselective phosphodiesterase inhibitor which has been marketed for treating asthma.Target: PDEIbudilast (3-isobutyryl-2-isopropylpyrazolo[1,5-a]pyridine) is a nonselective inhibitor of cyclic nucleotide phosphodiesterase (PDE). The inhibition of platelet aggregation and vasodilatation by ibudilast may be due to synergistic elevation of intracellular cyclic nucleotides and release of nitric oxide (NO) or prostacyclin from endothelium, rather than direct inhibition of PDE5 or PDE3. Another important property of ibudilast is its antiinflammatory activity possibly associated with potent inhibition of PDE4. Combined with its relaxing effects on bronchial smooth muscle, antiinflammatory actvity of ibudilast could favorably influence pathophysiology of asthma by antagonizing chemical mediators triggering asthmatic attacks [1, 2]. Ibudilast (AV-411) is a non-selective phosphodiesterase inhibitor that is also known to suppress glial cell activation. Preclinical data indicate that ibudilast crosses the blood-brain barrier, is well tolerated, is active on oral administration, reduces glial activation and attenuates pain symptoms in diverse rat models of neuropathic pain. In addition, it enhances acute morphine analgesia and attenuates morphine tolerance and withdrawal. Thus ibudilast may improve opioid efficacy and is a promising therapeutic candidate for neuropathic pain, with a novel mechanism of action [3].
ALK5-IN-32 (compound EX-09) is a selective ALK-5 inhibitor (10 nM
Methyl 2-((3-fluoro-4-(methylcarbamoyl)phenyl)amino)-2-methylpropanoate is an alanine derivative[1].
Pranlukast is a highly potent, selective and competitive antagonist of peptide leukotrienes. Pranlukast inhibits [3H]LTE4, [3H]LTD4, and [3H]LTC4 bindings to lung membranes with Kis of 0.63±0.11, 0.99±0.19, and 5640±680 nM, respectively.
Histone H3 (5-23), derived from histone H3 5-23 amino acids, can be used as a substrate for histone acetyltransferase (HAT) assays[1].