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.

ACLY Inhibitor 7 is a highly potent and selective small molecule inhibitor that exhibits exceptional inhibitory activity against human ATP citrate lyase (hACLY). ACLY Inhibitor 7 demonstrates an IC50 value of less than 1 nM as measured by the ADP-Glo assay, indicating its potential for metabolic disease and oncology research.

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.

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.

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

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).

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.

Isopyrazam, a plant protection product, exhibits potent antifungal activity. When applied to crops, it effectively inhibits the growth of various plant pathogenic fungi, significantly enhancing both the yield and quality of the crops. This compound demonstrates exceptional disease resistance capabilities in agricultural applications.

RR-49 is an innovative difluorinated analogue. This compound demonstrates exceptional pH sensitivity, showing the same efficacy for DAMGO in MOR cAMP assays at pH 6.5 as it does at pH 7.4, but with a 19-fold increase in potency (IC50). It holds significant promise as an analgesic for treating inflammatory pain with a lower potential for abuse.

LB 11058 is a novel injectable cephalosporin featuring a C-3 pyridyl-substituted vinyl sulfide and a C-7 2-amino-5-chloro-1,3-thiazole group. This compound exhibits exceptional activity against Streptococcus pneumoniae and demonstrates similar efficacy against β-hemolytic streptococci. The inhibition pattern for LB 11058 with S. aureus is consistent, as all isolates are inhibited under this pattern.

UNC8969 is a macrocyclic dual MERTK AXL inhibitor (IC50 MERTK = 1.1 nM; IC50 AXL = 5.3 nM). The compound exhibits low nanomolar activity against MERTK and AXL while demonstrating good selectivity over TYRO3 and FLT3. Target binding and selectivity have been confirmed through NanoBRET and cell-based MERTK and AXL phosphorylation assays. UNC8969 possesses excellent pharmacokinetic properties (large AUC and long half-life) and shows exceptional anti-tumor activity against lung cancer cell lines, indicating its potential as a therapeutic compound.

PSMA-D5 exhibits a binding affinity for PSMA with a Ki of 0.21 nM and becomes useful for PSMA tracing following radiolabeling. When marked with [68Ga], PSMA-D5 contains a DOTA chelator, facilitating the convenient labeling with therapeutic radionuclides such as 177Lu and 225Ac. Additionally, [68Ga]-labeled PSMA-D5 demonstrates exceptional pharmacokinetic properties and significant tumor uptake in 22Rv1 tumors. This compound can be employed in the synthesis and research of radiolabeled conjugates (RDC).

4A3-SCC-PH is a degradable ionic lipid (LDIL) characterized by a unique cone-shaped structure responsive to GSH. This configuration enables exceptional endosomal escape and rapid mRNA release.

HPK1-IN-55 (compound 19) is a selective and orally active inhibitor of hematopoietic progenitor kinase 1 (HPK1) with an IC50 of less than 0.51 nM. It exhibits exceptional kinase selectivity, being over 637 times more selective for HPK1 compared to GCK kinase and over 1022 times compared to LCK. HPK1-IN-55 possesses anti-cancer properties.

LYG-409 is an orally active GSPT1 degrader. It demonstrates exceptional in vivo anti-tumor activity against acute myeloid leukemia and prostate cancer, with tumor growth inhibition rates (TGI) of 94.34% and 104.49%, respectively. LYG-409 inhibits KG-1 cells by degrading GSPT1, with an IC50 of 9.50 nM and a DC50 of 7.87 nM in vitro.

SDH-IN-23 (Compound B21) is an SDH inhibitor with exceptional nematicidal activity. It can suppress nematode feeding, reproduction, and embryonic development while also inducing lethal effects through mechanisms such as oxidative stress, intestinal damage, and SDH inhibition.

RP-1664 is a selective and orally active PLK4 inhibitor with an IC50 of 3 nM. This compound demonstrates exceptional selectivity over related kinases, disrupts centriole biogenesis in cancer cells leading to PLK4 and p21 protein accumulation, shows enhanced sensitivity in TRIM37-high-expressing cells, and exhibits antitumor activity in breast cancer and neuroblastoma research.

(Rac)-Epoxiconazole is a chiral triazole fungicide released into the environment as a racemic mixture, known for its broad-spectrum, long-lasting, and exceptional fungicidal efficacy. It exhibits high persistence in soil, with a reported half-life exceeding 300 days.

FG-2101 is a selective, orally active non-hydroxamate LpxC inhibitor with an IC50 of approximately 1 nM. It demonstrates exceptional selectivity over other bacterial and human metalloproteases. FG-2101 is useful for studying infections caused by Gram-negative bacteria, including resistant strains.

N14G-Fe, the Fe3+ chelated form of N14G, can identify Mycobacterium tuberculosis in sputum samples from tuberculosis patients, exhibiting exceptional fluorescence properties. Additionally, N14G-Fe effectively traverses the cell wall and the inner membrane region where IrtAB is located.

Antifungalagent 131 (compound A20) is an antifungal agent with a minimum inhibitory concentration (MIC) of 64 μg/mL. When used in combination with Fluconazole, it demonstrates exceptional antifungal potential.

MK-3207 is a highly potent and orally bioavailable small molecule antagonist of the calcitonin gene-related peptide (CGRP) receptor, demonstrating an in vitro IC50 of 0.12 nM and a Ki of 0.024 nM for the human receptor with exceptional selectivity over the related human AM1, AM2, CTR, and AMY3 receptors, though it exhibits lower affinity for CGRP receptors from other species such as canine and rodent; in vitro studies confirm its potent antagonism of human and rhesus monkey CGRP receptors (K(i) = 0.024 nM), and in vivo models show it produces a concentration-dependent inhibition of dermal vasodilation, requiring plasma concentrations of 0.8 nM and 7 nM to block 50% and 90% of the blood flow increase, respectively.

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

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).