exceptional

JNK3 Inhibitor-4, a potent 2-aryl-1-pyrimidinyl-1H-imidazole-5-yl acetonitrile derivative, demonstrates a strong inhibitory effect on JNK3 with an IC 50 value of 1.0 nM. It exhibits exceptional selectivity against JNK3 when compared to other protein kinases, including isoforms JNK1 (IC 50 = 143.9 nM) and JNK2 (IC 50 = 298.2 nM). Additionally, JNK3 Inhibitor-4 benefits from neuroprotective properties and is predicted to permeate the blood-brain barrier effectively.

Chimmitecan ((S)-9-Allyl-10-hydroxycamptothecin) is a potent topoisomerase I inhibitor with exceptional in vitro and in vivo activity.

GSK-114, a selective inhibitor of TNNI3 Interacting Kinase (TNNI3K) with IC50 of 25 nM, shows significant bias for TNNI3K over B-Raf with IC50 of 1000 nM, exceptional broad spectrum kinase selectivity and adequate oral exposure to enable its use in cellul

Cetaben, a PPARα-independent peroxisome proliferator, is a non-fibrotic lipid-lowering drug that effectively reduces cholesterol and triglyceride concentrations.

DHPS-IN-1, a chemical compound, demonstrates exceptional inhibitory potency against melanoma cells, as evidenced by its IC50 value of 0.014 μM.

MMP13-IN-2 is a highly potent, selective, and orally active inhibitor of MMP-13. It demonstrates exceptional potency against MMP-13, with an IC50 value of 0.036 nM, and exhibits selectivities greater than 1,500-fold over MMP-1, 3, 7, 8, 9, 14, and TACE. Moreover, MMP13-IN-2 possesses the capability to effectively inhibit collagen release from cartilage in vitro. Consequently, MMP13-IN-2 holds great potential for advancing research on collagenase-related diseases.

ATR-IN-9 is a highly effective inhibitor of Ataxia-telangiectasia and RAD-3-related protein kinase (ATR). With an IC50 value as low as 10 nM, ATR-IN-9 demonstrates exceptional potency.

Cucurbit[8]uril is a highly effective and safe supramolecular compound that promotes protein heterodimerization. It selectively induces the heterodimerization of methylviologen and naphthalene functionalized proteins, demonstrating its specificity and versatility. Additionally, Cucurbit[8]uril shows exceptional oral activity and low toxicity, making it a promising candidate for various pharmaceutical and biotechnological applications.

Uzansertib (INCB053914) is a potent ATP-competitive pan-PIM kinase inhibitor. It exhibits exceptional inhibitory activity against PIM1, PIM2, and PIM3 with IC50 values of 0.24 nM, 30 nM, and 0.12 nM, respectively. Furthermore, Uzansertib demonstrates significant anti-proliferative effects against an assorted range of hematologic tumor cell lines.

S-14671 is a 5-HT1A receptor agonist (pKi = 9.3) with high efficacy and exceptional in vivo potency. S-14671 also acts as a 5-HT2A and 5-HT2C receptor antagonist (both are pKi = 7.8).

Acid Ceramidase-IN-1 is a highly effective, orally bioavailable inhibitor of acid ceramidase (AC, ASAH-1) with an IC50 of 0.166 μM and exhibits exceptional brain penetration capabilities in mice.

Cavα2δ-IN-1 demonstrates exceptional specificity for voltage-gated calcium channels Cavα2δ-1 (with a Ki value of 6 nM), in comparison to Cavα2δ-2 (with a Ki value greater than 10,000 nM).

ALK-IN-12 is a highly potent and orally active inhibitor of anaplastic lymphoma kinase (ALK), demonstrating an exceptional IC50 value of 0.18 nM. Additionally, ALK-IN-12 displays inhibitory activity against insulin-like growth factor 1 receptor (IGF1R) and insulin receptor (InsR), with IC50 values of 20.3 nM and 90.6 nM, respectively. Notably, its antitumor effects have been observed, making it a promising compound for targeted cancer therapy.

5'-ODMT cEt m5U Phosphoramidite Amidite, a locked nucleic acid (LNA) analog, demonstrates exceptional safety and antisense activity [1] [2].

Adenosine receptor inhibitor 1 is a highly potent and selective antagonist of adenosine receptor (AR), exhibiting exceptional affinity for A1 AR, A2A AR, A2B AR, and A3 AR, with respective Ki values of >1000, 68.5, >1000, >1000 nM. This compound demonstrates notable antinociceptive, anti-inflammatory, and peripheral analgesic properties, holding great promise for investigating cancer and neurodegenerative diseases [1].

CXCR4 antagonist 3 (compound 12a), an effective antagonist of CXCR4, exhibits an IC50 of 11 nM. It is a congener of TIQ15, showcasing exceptional properties such as CXCR4 antagonism, CYP 2D6 inhibition, metabolic stability, and permeability. With its potential for research on the human immunodeficiency virus, CXCR4 antagonist 3 holds great promise [1].

Compound I16 (ROS inducer 2) is a potent inducer of Reactive Oxygen Species (ROS) with an effective concentration (EC 50) of 3.43 μg/mL demonstrated in vitro. It exhibits exceptional bioactivity in vivo against Xanthomonas axonopodis pv. citri and has potential as a bactericidal agent for investigating intractable plant bacterial diseases [1].

FLT3 ITD-IN-1 (Compound 1) is a highly potent inhibitor of FLT3 internal tandem duplications (FLT3-ITD) with IC50 values of 38.2 nM for FLT3 and 144.1 nM for FLT3-ITD, and shows exceptional antiproliferative activities against several acute myeloid leukemia cell lines [1].

Antimicrobial Agent-5 is a potent antimicrobial agent that exhibits exceptional cell selectivity against both Gram-negative and Gram-positive bacteria. It inhibits the interaction between LPS (lipopolysaccharide) and the CD14/TLR4 (Toll-like receptor 4) receptor, demonstrating anti-inflammatory activity in combating LPS-induced inflammation.

BACE2-IN-1, a potent BACE2 inhibitor characterized by its exceptional selectivity and a Ki value of 1.6 nM, is utilized in the investigation of Type 2 Diabetes.

NS5A-IN-2 (Compound 33) is a potent NS5A inhibitor with remarkable efficacy against HCV genotype 1b, increased activity against genotype 3a (GT 3a), and significant metabolic stability [1].

EGFR-IN-43 (Compound 17c) is a highly effective EGFR inhibitor with single-digit nanomolar activity, uniquely combining tamoxifen or endoxifen with the EGFR inhibitor gefitinib through a covalent bond, maintaining both ER antagonist activity and EGFR inhibition capabilities, demonstrating exceptional anti-cancer efficacy [1].

Trametiglue, a Trametinib derivative, exhibits exceptional potency and selectivity in targeting KSR-MEK and RAF-MEK through distinctive interfacial binding interactions [1].

JH-LPH-28, a sulfonyl piperazine analog, is a potent inhibitor of UDP-2,3-diacylglucosamine pyrophosphate hydrolase LpxH, exhibiting exceptional antibiotic activity with a minimum inhibitory concentration (MIC) of 0.83 μg mL.

PI3Kγ inhibitor 5 is a potent inhibitor of phosphoinositide 3-kinase γ (PI3Kγ), exhibiting an exceptional IC50 value of 34 nM.

Squalene synthase-IN-1 (compound 1) is a potent antihyperlipidemic agent that inhibits Squalene Synthase, demonstrating exceptional antioxidant and anti-inflammatory activities. It significantly reduces glucose and oxidative stress levels without causing toxicity [1].

EEDi-5285, an orally active and highly potent inhibitor targeting embryonic ectoderm development (EED) protein, exhibits anti-cancer activity. It demonstrates exceptional efficacy with an IC50 value of 0.2 nM, indicating robust binding affinity to the EED protein.

4-APC hydrobromide is a potent and specific aldehyde derivatization agent. It contains an aniline moiety that enables rapid and selective reaction with aliphatic aldehydes, as well as a quaternary ammonium group that enhances sensitivity in mass spectrometry (MS) analysis. By utilizing 4-APC hydrobromide, aldehydes can be detected with exceptional sensitivity and selectivity using MS.

SARS-CoV-2-IN-20 (Compound 1a) is a highly effective SARS-CoV-2 inhibitor with an impressive EC50 value of 6.5 μM, demonstrating significant potential for advancing infectious disease research [1].

Vildagliptin dihydrate (LAF237 dihydrate) is a potent and stable dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 of 3.5 nM in human Caco-2 cells, exhibiting exceptional oral bioavailability and significant antihyperglycemic activity [1].

Y18501, an oxysterol-binding protein (OSBPI) inhibitor structurally akin to Oxathiapiprolin, demonstrates potent inhibition against Phytophthora spp. and Pseudoperonospora cubensis with EC50 values between 0.0005 and 0.0046 μg/mL. It exhibits exceptional protective and curative effects on P. cubensis. When used in tandem with Chlorothalonil, Y18501 markedly enhances the suppression of P. cubensis [1].

MLi-2 is a structurally novel, highly potent, and selective LRRK2 kinase inhibitor with central nervous system activity. MLi-2 exhibits exceptional potency in a purified LRRK2 kinase assay in vitro (IC50 = 0.76 nM), a cellular assay monitoring dephosphorylation of LRRK2 pSer935 LRRK2 (IC50 = 1.4 nM), and a radioligand competition binding assay (IC50 = 3.4 nM).

DDR1-IN-4 (Compound 2.45) is a highly potent inhibitor that selectively targets Discoidin Domain Receptor 1 (DDR1) autophosphorylation, demonstrating exceptional efficacy with IC50 values of 29 nM for DDR1 and 1.9 μM for DDR2.

2-Nitrosopyridine is a versatile nitroso compound employed in the synthesis of antibiotics. It serves as a valuable derivatization reagent for Click and Diels-Alder reactions, displaying exceptional dienophile characteristics.

Rac-Finerenone, also known as (Rac)-BAY 94-8862, is the racemate derivative of Finerenone, a selective third-generation nonsteroidal mineralocorticoid receptor antagonist (MR) that is taken orally. With an IC50 value of 18 nM, Finerenone exhibits exceptional selectivity against the glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold).

PROTAC EGFR degrader 2 is a potent compound with an IC50 of 4.0 nM, demonstrating strong antiproliferative activity, and a DC50 of 36.51 nM, indicating robust EGFR degradation activity. It is suitable for synthesizing nitroreductase (NTR)-responsive PROTACs [1].

CK2 inhibitor 3 is a highly potent inhibitor of protein kinase CK2, exhibiting an IC50 value of 280 nM. It effectively inhibits the intracellular activity of CK2 and displays a notable impact on the viability of tumor cells. Moreover, CK2 inhibitor 3 demonstrates exceptional selectivity among a diverse panel of 320 kinases [1].

MSC2360844 hemifumarate is a highly potent and orally active compound that acts as a selective inhibitor of PI3Kδ, with an IC50 value of 145 nM. This compound exhibits exceptional selectivity against a comprehensive panel of 278 additional kinases.

Golgicide A-2 (GCA-2), a derivative of Golgicide A (GCA), is the highly active enantiomer of GCA. It exhibits exceptional selectivity and efficiency in eradicating An. stephensi larvae, making it valuable for dengue virus-related research.

BMS-351 is a potent and selective, nonsteroidal CYP17A1 lyase inhibitor with robust selectivity over steroidogenic CYPs 21A2 and 11B1. BMS-351 emerges as an outstanding preclinical candidate to treat CRPC and is likely to minimize the side effects of current therapies due to its exceptional selectivity. BMS-351 is potentially useful for the Treatment of Prostate Cancer.

Dazucorilant (CORT113176) is a non-steroidal glucocorticoid receptor (GR) modulator characterized by its high affinity and selectivity. With an impressive K i value of ＜1 nM in vitro, Dazucorilant proves to be an exceptional compound for investigating neurological disorders.

Mcl-1 inhibitor 6 is a potent, orally active chemical compound that selectively inhibits the myeloid cell leukemia 1 (Mcl-1) protein, with a high affinity (K d = 0.23 nM) and binding activity (K i = 0.02 μM). This compound exhibits exceptional selectivity over other members of the Bcl-2 family, including Bcl-2, Bcl2A1, Bcl-xL, and Bcl-w (K d >10 μM). Notably, Mcl-1 inhibitor 6 demonstrates strong antitumor activity.

Antimicrobial Agent-10 demonstrates exceptional antibacterial activity and inhibits SARS-CoV-2, positioning it as a potent antimicrobial compound [1].

GSK2332255B is a highly potent and selective TRPC3 and TRPC6 antagonist, exhibiting IC50 values of 5 nM and 4 nM for rat TRPC3 and rat TRPC6, respectively. Furthermore, GSK2332255B demonstrates exceptional selectivity, surpassing a ≥100-fold difference when compared to other calcium-permeable channels.

PGN36 (Compound 18) is a potent and highly selective antagonist of the cannabinoid CB2 receptor (CB2R), exhibiting exceptional affinity with a Ki value of 0.09 μM [1].

KMG-104 is a fluorescent magnesium (Mg2+) probe known for its exceptional selectivity. It has been extensively utilized to investigate the mobilization of Mg2+ in the cytoplasm across different cell types.

ITIC, a non-fullerene acceptor, demonstrates exceptional thermal stability and exhibits a glass-crystal transition at a significantly lower temperature than its high glass transition temperature (Tg) of 180 °C. Furthermore, ITIC, which is an indacenodithienothiophene-based postfullerene electron acceptor, displays a distinct crystallization behavior, differing substantially from that of fullerenes.

Trk-IN-6 exhibits exceptional in vitro potency against a range of TRK mutants (IC50 = 0.2-0.7 nM).

Antifungal agent 14 demonstrates potent broad-spectrum antifungal activity, effectively targeting a variety of fungal strains with exceptional minimum inhibitory concentration values.

SEL24-B489 is a highly effective and orally bioavailable compound that acts as a robust, type I inhibitor of both PIM and FLT3-ITD. It exhibits exceptional binding affinity with K d values of 2 nM for PIM1, 2 nM for PIM2, and 3 nM for PIM3.