9月
Aftin-4；化合物Aftin4Aftin 4|||Aftin4；Aftin 4|||Aftin4 (2024/9/8)
簡介：aftin-4, an amyloid forty-two inducer, activates γ-secretase, promoting the generation of amyloid-β-1-42 (aβ1-42) from amyloid-β protein precursor. aftin-4(aftin4) increased aβ-1-42, but not aβ-1-40 in mouse hipppocampus, accompanied by learning deficits and mitochondrial ultrastructural changes similar to those found in the brains of patients with ad. aftin-4(aftin4) can thus be used to induce a rapid, acute alzheimer´s disease-like toxicity in the rodent brain.
WM-8014；化合物MOZ-IN-3MOZ-IN-3；MOZ-IN-3 (2024/9/8)
簡介：wm-8014 (moz-in-3) is an inhibitor of moz(ic50=55 nm), a member of histone acetyltransferases.
CBL0137 hydrochloride；化合物CBL0137 hydrochlorideCBL0137|||CBLC137|||Curaxin 137|||CBL-C137 hydrochlori (2024/9/8)
簡介：cbl0137 hydrochloride (curaxin-137 hydrochloride) activates p53 and inhibits nf-kb (ec50: 0.37/0.47 μm) in the cell-based p53 and nf-kb reporter assays, respectively. it also suppresses histone chaperone fact.
ML385；化合物ML385ML385 (2024/9/8)
簡介：ml385 is an nrf2 inhibitor (ic50=1.9 μm) with novelty and specificity. ml385 has anti-inflammatory activity by modulating anti-oxidative stress through the inhibition of nrf2. ml385 also exhibits anti-tumor activity.
VAS2870；化合物VAS2870VAS2870 (2024/9/8)
簡介：vas2870 is an inhibitor of nadph oxidase (nox).
KPT9274；化合物KPT9274KPT-9274|||KPT 9274|||PAK4-IN-1；KPT-9274|||KPT 9274|||PAK4-IN-1 (2024/9/8)
簡介：kpt9274 (pak4-in-1) is a non-competitive dual inhibitor of pak4 and nampt(ic50= ~120 nm). it is an orally bioavailable small molecule.
SR-18292；化合物SR18292SR 18292；SR 18292 (2024/9/8)
簡介：sr-18292 is an inhibitor of ppar gamma coactivator-1α (pgc-1α), which increases pgc-1α acetylation, suppresses gluconeogenic gene expression and reduces glucose production in hepatocytes.
SB756050；化合物SB756050SB-756050|||SB 756050；SB-756050|||SB 756050 (2024/9/8)
簡介：sb756050 is a specific tgr5 agonist.
DAMGO；化合物DAMGODagol|||DAGO|||RX-783006；Dagol|||DAGO|||RX-783006 (2024/9/8)
簡介：damgo (dago) is an opioid receptor agonist with the ability to affect the locomotive activity in rodents. possible analgesic agent due to μ-opiod receptor interaction.
Palifosfamide；帕利伐米ZIO-201|||Isophosphamide mustard|||Isophosphoramide mustard；ZIO-201|||Isophosphami (2024/9/8)
簡介：palifosfamide (isophosphamide mustard) lysine (zio-201) is a stable form of palifosfamide. palifosfamide lysine has broad activity in sarcoma lines in vitro. the ic50 ranges from 2.25 to 6.75 μm for most cell lines except os222 (ic50=31.5 μm).
Sitravatinib；化合物SitravatinibMG516|||MGCD516；MG516|||MGCD516 (2024/9/8)
簡介：sitravatinib (mgcd516) is an inhibitor targeting multiple rtks involved in driving sarcoma cell growth, including c-met, c-kit, pdgfrα/β, pdgfr, and axl.
Syk Inhibitor II；化合物Syk Inhibitor IISyk Inhibitor II (2024/9/8)
簡介：syk inhibitor ii, a cell-permeable, atp-competitive, pyrimidine-carboxamide compound, selectively and reversibly inhibits syk (ic50 = 41 nm).
ML355；化合物ML355ML355 (2024/9/8)
簡介：ml355, a specific, effective 12-lipoxygenase(12-lox) inhibitors(ic50=0.34 μm), possess favorable adme properties.
SPDB；化合物SPDBSPDB (2024/9/8)
簡介：spdb is a small fragment linked to dm4 conjugates. it conjugates to antibodies utilizing disulfide linkers: anti-egfr-spdb-dm4 has been widely used.
CeMMEC1化合物CeMMEC1CeMMEC1 HCl (2024/9/8)
簡介：cemmec1 is an inhibitor of brd4, and also has a great affinity for taf1(ic50=0.9 μm).
ALW-II-41-27；化合物ALW-II-41-27Eph receptor tyrosine kinase inhibitor；Eph receptor tyrosine kinase inhi (2024/9/8)
簡介：alw-ii-41-27 (eph receptor tyrosine kinase inhibitor), an eph receptor tyrosine kinase inhibitor, is used for cancer therapy.
A-196；化合物A196A 196；A 196 (2024/9/8)
簡介：a-196 is a potent and selective inhibitor of suv420 h1 and suv420 h2 with ic50 values of 0.025 and 0.144 μm, respectively; more than 100-fold selective over other histone methyltransferases and non-epigenetic targets.
PF-04929113 Mesylate；化合物PF-04929113 MesylatePF-04929113 (Mesylate)|||SNX-5422 Mesylate；PF-04929113 ( (2024/9/8)
簡介：pf-04929113 mesylate (snx-5422 mesylate), a prodrug of snx-2112, is an orally available hsp90 inhibitor (kd: 41 nm) and also induces her-2 degradation (ic50: 37 nm).
Betrixaban；貝曲西班PRT054021；貝曲西班|||PRT054021 (2024/9/8)
簡介：betrixaban (prt054021) is a non-vitamin k oral anticoagulant whose action is driven by the competitive and reversible inhibition of the factor xa [1]. it was selected among all lead compounds due to its low herg channel affinity while sustaining its factor xa inhibition capacity [3]. betrixaban, now developed by portola pharmaceuticals inc., is prescribed as a venous thromboembolism (vte) prophylactic for adult patients with moderate to severe restricted motility or with other risks for vte [2].
SPI-112；化合物SPI 112SPI-112 (2024/9/8)
簡介：spi-112, the spi-112 methyl ester analog, can inhibit cellular shp2 ptp activity. spi-112 bound to shp2 by surface plasmon resonance (spr) and displayed competitive inhibitor kinetics to shp2.
YU238259；化合物YU238259YU238259 (2024/9/8)
簡介：yu238259 is a novel inhibitor of homology-dependent dna repair(hdr), but does not inhibit non-homologous end-joining (nhej), in cell-based gfp reporter assays.
USP7/USP47 inhibitor；化合物USP7/USP47 inhibitorUSP7/47 inhibitor-1；USP7/47 inhibitor-1 (2024/9/8)
簡介：usp7/usp47 inhibitor (usp7/47 inhibitor-1) is a selective ubiquitin-specific protease 7/47 (usp7/usp47) inhibitor, with ec50s of 0.42 μm and 1.0 μm, respectively.
PCI 29732；化合物PCI29732PCI29732|||PCI-29732；PCI29732|||PCI-29732 (2024/9/8)
簡介：pci 29732 is a selective and irreversible btk inhibitor with ic50 of 8.2 nm in a fret based biochemical enzymology assay.
IPTG；異丙基-beta-D-硫代半乳糖吡喃糖苷Isopropyl β-D-thiogalactoside；異丙基-beta-D-硫代半乳糖吡喃糖苷|||Isopropyl β-D-thiogala (2024/9/8)
簡介：iptg (isopropyl β-d-thiogalactoside) is a non-metabolizable galactose analog that induces expression of the lac operon.
GNE-617；化合物GNE617GNE617；GNE617 (2024/9/8)
簡介：gne-617, a specific nampt inhibitor(ic50=5 nm), shows potency in xenograft models of cancer.
EPZ020411 2HCl (1700663-41-7(free base))；化合物EPZ020411 2HClEPZ020411 2HCl (1700663-41-7(free base)) (2024/9/8)
簡介：epz020411 is an effective and specific small molecule prmt6 inhibitor (ic50=10 nm).
Quinine dihydrochloride；鹽酸奎寧Quinine bimuriate；鹽酸奎寧|||Quinine bimuriate (2024/9/8)
簡介：quinine dihydrochloride (quinine bimuriate) is a primary alkaloid of various species of cinchona (rubiaceae). it is also an antimalarial and muscle relaxant (skeletal).
c-Kit-IN-1；化合物c-Kit-IN-1PDGFR inhibitor 1|||DCC-2618；PDGFR inhibitor 1|||DCC-2618 (2024/9/8)
簡介：c-kit-in-1 (dcc-2618) is an effective inhibitor of c-met and c-kit (ic50s<200 nm).
CaCCinh-A01；化合物CaCCinh-A01CaCCinh-A01 (2024/9/8)
簡介：caccinh-a01 is an inhibitor of the calcium-activated chloride channel (cacc, 10 μm) and tmem16a (ic50: 2.1 μm).
CP 376395；化合物CP 376395CP-316311；CP-316311 (2024/9/8)
簡介：cp 376395 (cp-316311) is an effective and specific corticotropin-releasing factor 1 (crf1) receptor antagonist.
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