9月
PCSK9-IN-14；化合物 PCSK9-IN-14PCSK9-IN-14 (2024/9/14)
簡(jiǎn)介：pcsk9-in-14, also known as compound ia-8, is a potent inhibitor of pcsk9 [1].
Saquinavir；沙奎那韋Ro 31-8959；Ro 31-8959|||沙奎那韋 (2024/9/14)
簡(jiǎn)介：saquinavir (ro 31-8959) is a potent hiv protease inhibitor, is an antiretroviral drug used together with other medications to treat or prevent hiv/aids.
IpOHA；化合物 IpOHAIpOHA (2024/9/14)
簡(jiǎn)介：ipoha is a potent inhibitor of plant kari and functions as an antimycobacterial agent, demonstrating a k_i value of 97.7 nm against mycobacterium tuberculosis (mt) [1].
p38 Kinase inhibitor 4；化合物 p38 Kinase inhibitor 4p38 Kinase inhibitor 4 (2024/9/14)
簡(jiǎn)介：compound 135, also known as p38 kinase inhibitor 4, is a potent inhibitor of p38 [1].
A1/A3 AR antagonist 3；化合物 A1/A3 AR antagonist 3A1/A3 AR antagonist 3 (2024/9/14)
簡(jiǎn)介：a1/a3 ar antagonist 3 is a dual a1r/a3r antagonist that demonstrates high affinity within the low-micromolar to nanomolar range, and is potentially useful in the research of chronic heart diseases [1].
Tankyrase-IN-5；化合物 Tankyrase-IN-5Tankyrase-IN-5 (2024/9/14)
簡(jiǎn)介：tankyrase-in-5 (compound 30f), structurally related to msc2504877, effectively inhibits tankyrase isoforms tnks1 and tnks2, with half-maximal inhibitory concentrations (ic50s) of 2.3 nm and 7.9 nm, respectively [1].
TNF-α-IN-10；化合物 TNF-α-IN-10TNF-α-IN-10 (2024/9/14)
簡(jiǎn)介：tnf-α-in-10 (compound 8a) acts as an inhibitor of il-6 and tnf-α, demonstrating anti-inflammatory activity [1].
Androgen receptor-IN-5；化合物 Androgen receptor-IN-5Androgen receptor-IN-5 (2024/9/14)
簡(jiǎn)介：androgen receptor-in-5 is a potent inhibitor of the androgen receptor with anticancer properties. it additionally suppresses the synthesis of il-17a, il-17f, and inf-γ.
CaSR antagonist-1；化合物 CaSR antagonist-1CaSR antagonist-1 (2024/9/14)
簡(jiǎn)介：casr antagonist-1 is a potent inhibitor of the calcium-sensing receptor (casr) with an inhibitory concentration (ic50) of 50 nm, suitable for the investigation of diseases related to dysregulated bone or mineral homeostasis, including osteoporosis [1].
BACE1-IN-13；化合物 BACE1-IN-13BACE1-IN-13 (2024/9/14)
簡(jiǎn)介：bace1-in-13 (compound 36), an orally active inhibitor of bace1, exhibits high potency with an ic50 of 2.9 nm and demonstrates greater efficacy in haβ42 cells (ic50 = 1.3 nm). it is considered safe for the cardiovascular system and induces a sustained reduction of aβ42 in both mouse and dog animal models [1].
GSK3839919A；化合物 GSK3839919AGSK3839919A (2024/9/14)
簡(jiǎn)介：gsk3839919a is a potent allosteric inhibitor of hiv-1 integrase [1].
ALK2-IN-5；化合物 ALK2-IN-5ALK2-IN-5 (2024/9/14)
簡(jiǎn)介：alk2-in-5, a pyrazolopyrimidine compound, serves as an inhibitor of alk2 and fgfr, targeting disorders linked with their activity, including cancer [1].
Ozenoxacin；奧澤沙星T-3912；奧澤沙星|||T-3912 (2024/9/14)
簡(jiǎn)介：ozenoxacin (t-3912) is a quinolone antibacterial. it shows potent activities against the main microorganisms isolated from soft tissue and skin infections.
JNJ-64264681；化合物 JNJ-64264681JNJ-64264681 (2024/9/14)
簡(jiǎn)介：jnj-64264681 is a potent, orally active, selective, and irreversible covalent inhibitor of bruton´s tyrosine kinase (btk). this compound demonstrates favorable pharmacokinetic properties and is applicable in the research of cancer and autoimmune diseases [1].
GSK217；化合物 GSK217GSK217 (2024/9/14)
簡(jiǎn)介：gsk217 is a potent and selective inhibitor of the bromo and extraterminal domain (bet) second bromodomain (bd2) with high solubility, utilized in oncology and immune inflammation research [1].
GSK737；化合物 GSK737GSK737 (2024/9/14)
簡(jiǎn)介：gsk737 is a dual inhibitor of brd4 bd1 and bd2, exhibiting pic50 values of 5.3 and 7.3, respectively. it demonstrates low clearance, along with favorable solubility and permeability in rats [1].
BET-IN-14；化合物 BET-IN-14BET-IN-14 (2024/9/14)
簡(jiǎn)介：bet-in-14 is a pan bet inhibitor with an ic50 of 5.35 nm, demonstrating oral activity and anticancer properties [1].
SEQ-9；化合物 SEQ-9SEQ-9 (2024/9/14)
簡(jiǎn)介：seq-9 is an orally active inhibitor targeting the mycobacterium tuberculosis (mtb) 23s bacterial ribosome, demonstrating an inhibitory concentration (ic50) around 170 nm against unmethylated mtb ribosomes and showing potent effects on a2296 methylated ribosomes. this compound is utilized in researching bacterial infections and drug resistance [1].
QR-6401；化合物 QR-6401QR-6401 (2024/9/14)
簡(jiǎn)介：qr-6401, a selective macrocyclic cdk2 inhibitor, is orally active with ic50 values of 0.37 nm for cdk2/e1, 10 nm for cdk9/t1, 22 nm for cdk1/a2, 34 nm for cdk6/d3, and 45 nm for cdk4/d1. it exhibits potent antitumor activity in the ovcar3 ovarian cancer xenograft model, indicating its potential for use in cancer research [1].
SLMP53-2；化合物 SLMP53-2SLMP53-2 (2024/9/14)
簡(jiǎn)介：slmp53-2 is a mutant p53 reactivator that restores the wild-type-like conformation and dna-binding ability of mutp53-y220c through enhanced interaction with hsp70, thereby reinstating p53´s transcriptional activity. this compound induces cell cycle arrest, apoptosis, and endoplasmic reticulum (er) stress, displaying antitumor activity [1] [2].
MDM2/XIAP-IN-2；化合物 MDM2/XIAP-IN-2MDM2/XIAP-IN-2 (2024/9/14)
簡(jiǎn)介：mdm2/xiap-in-2 is a dual inhibitor targeting murine double minute 2 (mdm2) and x-linked inhibitor of apoptosis protein (xiap). it promotes the degradation of mdm2 and impedes translation of xiap mrna, effectively inhibiting cancer cell proliferation. notably, it exhibits potent activity against the acute lymphoblastic leukemia cell line eu-1, with an ic50 of 0.3 μm [1].
TrkB-IN-1；化合物 TrkB-IN-1TrkB-IN-1 (2024/9/14)
簡(jiǎn)介：trkb-in-1 is a potent, orally active agonist of the trkb receptor, with favorable pharmacokinetic (pk) properties. it has been shown to reverse cognitive deficits in an alzheimer´s disease (ad) mouse model, thus serving as a valuable tool for alzheimer’s disease research [1].
Lp-PLA2-IN-12；化合物 Lp-PLA2-IN-12Lp-PLA2-IN-12 (2024/9/14)
簡(jiǎn)介：lp-pla2-in-12 (compound 19), an lp-pla2 inhibitor, is utilized in researching neurodegenerative diseases including alzheimer´s disease (ad), glaucoma, age-related macular degeneration (amd), and cardiovascular conditions such as atherosclerosis [1].
Emodepside；化合物EmodepsideBay 44-4400；Bay 44-4400 (2024/9/14)
簡(jiǎn)介：emodepside (bay 44-4400) is an anthelmintic drug that is effective against a number of gastrointestinal nematodes,with broad-spectrum anthelmintic activity.
VEGFR2-IN-3；化合物 VEGFR2-IN-3VEGFR2-IN-3 (2024/9/14)
簡(jiǎn)介：vegfr2-in-3 (compound 385) is a potent inhibitor of vegfr2 [1].
Ys-II；化合物 Ys-IIYs-II (2024/9/14)
簡(jiǎn)介：compound 1 (ys-ii) is a spirostanol glycoside extracted from the stem of yucca elephantipes, exhibiting antifungal properties by inhibiting candida albicans and cryptococcus neoformans growth with ic50 values of 5 and 6 μg/ml, respectively [1].
CARM1-IN-3；化合物 CARM1-IN-3CARM1-IN-3 (2024/9/14)
簡(jiǎn)介：carm1-in-3 (compound 17b) is a potent, selective inhibitor of co-activator associated arginine methyltransferase (carm1), exhibiting ic50 values of 0.07 μm for carm1 and greater than 25 μm for carm3 [1].
Pyrene phosphoramidite dU；化合物 Pyrene phosphoramidite dUPyrene phosphoramidite dU (2024/9/14)
簡(jiǎn)介：pyrene phosphoramidite du, a click chemistry reagent featuring pyrene moieties, can be incorporated into dna, resulting in pronounced blue fluorescence.
6-Hydroxyluteolin；化合物 6-Hydroxyluteolin6-Hydroxyluteolin (2024/9/14)
簡(jiǎn)介：6-hydroxyluteolin (compound 17), a flavonoid, exhibits inhibition of aldose reductase (ar) [1].
ATP synthase inhibitor 2 TFA；化合物 ATP synthase inhibitor 2 TFAATP synthase inhibitor 2 TFA (2024/9/14)
簡(jiǎn)介：atp synthase inhibitor 2 (compound 22) tfa is a potent inhibitor of pseudomonas aeruginosa atp synthase with an ic50 value of 10 μg/ml. it effectively halts atp synthesis in pseudomonas aeruginosa at a concentration of 128 μg/ml [1].
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