SET-171 is a JNK (c-Jun N-terminal kinase) inhibitor that exhibits significant anticancer activity and lipid metabolism regulation by inhibiting liver pyruvate kinase (PKL) expression. In anticancer studies, SET-171 shows IC50 values of 8.82 μM and 2.97 μM against HepG2 and Huh7 cell lines, respectively, indicating high cytotoxicity. Additionally, in non-alcoholic fatty liver disease (NAFLD)-related studies, SET-171 significantly reduces triacylglycerol (TAG) levels and inhibits the expression of steatosis-related proteins. SET-171 holds promise for research on hepatocellular carcinoma (HCC) and NAFLD.

JD118 is a JNK inhibitor. JD118 inhibits JNK1 activity and the expression of cJun (1–135).

(3S)-Tanzisertib (hydrochloride) ((3S)-CC-930 (hydrochloride)) is an orally active JNK inhibitor (IC50 values for JNK1, JNK2, and JNK3 are 61, 7, and 6 nM, respectively). (3S)-Tanzisertib (hydrochloride) selectively inhibits ERK1, p38α, and EGFR (IC50 = 0.48, 3.4, and 0.38 μM, respectively). (3S)-Tanzisertib (hydrochloride) inhibits LPS-induced TNFα production in an acute rat PK-PD model. (3S)-Tanzisertib (hydrochloride) can be used in idiopathic pulmonary fibrosis (IPF) research.

SKLB-D18 is a potent and selective inhibitor of ERK1/2 and ERK5, with IC50s of 38.69, 40.12 and 59.72 nM, respectively. SKLB-D18 is also an autophagy agonist, plays a role in mTOR/p70S6K and NCOA4-mediated ferroptosis, which may mitigate multidrug resistance. SKLB-D18 exhibits significantly superior efficacy in vitro and in vivo against triple-negative breast cancer (TNBC).

ERK2 IN-5 (Compound 5g) is an inhibitor for ERK2, and exhibits good affinity to ERK2 and JNK3 with Ki of 86 and 550 nM.

Boc3Arg is the tert-butyl carbamate-protected arginine. Boc3Arg is an efficient tag to induce degradation through directly localizing the protein to the 20S proteasome.

bpV(bipy) hydrate is the inhibitor for phosphoinositide 3-phosphatase (PTEN) and protein tyrosine phosphatases (PTP-β and PTP-1B) with IC50s of 18, 60.3, and 164 nM, respectively.

Toyaburgine is a unique isoquinoline compound that exhibits anti-tumor activity. It packs a punch by disrupting the PI3K/AKT/mTOR signaling pathway, causing significant morphological changes and cell death in MIA PaCa-2 cells. On top of that, it puts the brakes on cell migration and colony formation. This compound is showing a lot of promise in the realm of pancreatic cancer research.

KIM-161 is a PIK3CA inhibitor. KIM-161 has significant antiproliferative activity with IC50 values of 1.428 and 1.562 µM against PI3KCA mutant breast cancer MCF7 and T47D cells, respectively. KIM-161 induces apoptosis and cell cycle arrest by inhibiting the PI3K/AKT/mTOR signaling pathway and inducing ROS production. KIM-161 can be used to study breast cancer and its PI3KCA mutant subtypes.

JZ19 reduces the LDH and ROS levels, and exhibits antioxidant activity against oxygen-glucose deprivation (OGD)-induced cardiomyocyte injury. JZ19 reverses Isoproterenol-induced cardiomyocyte hypertrophy and apoptosis through PI3K-AKT-GSK3β signaling pathway. JZ19 alleviates Isoproterenol-induced heart failure in mouse models.

Hydroxy celecoxib is a Celecoxib. N-Stearoyltyrosine exhibits neuroprotective efficacy in gerbils ischemia-reperfusion model through protection in the CA1 region of the hippocampus. N-Stearoyltyrosine inhibits the free radicals production and improves antioxidant capacity. N-Stearoyltyrosine inhibits the IR-induced apoptosis.

Erufosine is an inhibitor of PI3K/Akt and Ras/Raf/MAPK signaling pathways. Erufosine inhibits the activity of breast cancer cell lines MCF-7 and MDA-MB 231 (IC50: 40.95/40.8 μM). Erufosine reduces the phosphorylation of PI3K (p85), Akt (PKB), and cRaf. Erufosine can be used in the study of breast cancer and myeloid leukemia.

Dactolisib (BEZ235) hydrochloride is an orally active, dual pan-class I PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR with IC50 of 4 nM/5 nM/7 nM/75 nM and 20.7 nM, respectively. Dactolisib hydrochloride (BEZ235) inhibits mTORC1 and mTORC2.

D-106669 (comppun 150) is a potent inhibitor of PI3Kα, with the IC50 of 0.129 μM. D-106669 plays an important role in cancer research.

AS-605240 (potassium) is an orally active PI3Kγ inhibitor (IC50: 8 nM; Ki: 7.8 nM). AS-605240 (potassium) inhibits MCP-1- and CSF1-induced PKB phosphorylation (IC50 values are 0.181 and 0.550 µM, respectively). AS-605240 (potassium) reduces neutrophil recruitment in RANTES (CCL5)- and thioglycolate-induced peritonitis mouse models (EC50 values are 9.1 and 10 mg/kg, respectively). AS-605240 (potassium) ameliorates αCII-IA-induced arthritis in mice.

(S)-RLY-2608 is an S-enantiomer of of RLY-2608, an RNA-degrading chimera which binds to a four-way RNA helix called SL5 in the 5’ UTR of the SARS-CoV-2 RNA genome and inhibits the virus replication in lung epithelial carcinoma cells. RNA recruiter-linker 1 can be utilized in the synthesis of RIBOTAC.

(2S)-SB02024 (SB02877), the S-enantiomer of SB02024 -induced novel object recognition (NOR) models. VU6024578 is blood brain barrier penetrable.

YB-3−17 is a dual-target compound that effectively and selectively inhibits mTOR with an IC50 of 0.22 nM, while promoting GSPT1 degradation with an IC50 of 5 nM, leading to substantial tumor growth inhibition both in vitro and in vivo. It also exhibits significant antiproliferative activity in glioblastoma models.

PD-M6 is an mTOR PROTAC degrader (DC50: 4.8 μM). PD-M6 promotes the ubiquitination and degradation of mTOR. PD-M6 inhibits the proliferation of HeLa, MCF-7, and HepG2 cancer cell lines (IC50 values of 11.3, 2.58, and 3.23 μM, respectively) and induces autophagy. PD-M6 specifically induces the degradation of LAMTOR1, a key protein in the mTOR signaling pathway.

HYS-072 is an orally active derivative of chrysin.

AV457 is a potent and selective mTOR inhibitor with an IC50 value of 0.54 µM. AV457 inhibits cyst growth in polycystic kidney disease (PKD) organoids. AV457 decreases the protein expression of P-s6, P-p70s6 and don’t decreases the protein expression of P-AKT.

2DII is a potent and selective mTORC2 inhibitor. 2DII selectively binds mSin1 PH domain and decreases the expression of AKT1 phosphorylation.

1-Acetyl-DHA (Compound 7) is a substrate of the phosphotriesterase homology protein (PHP) and can be hydrolyzed by PHP with a kcat/km value of 100 M-1s-1. The level of 1-Acetyl-DHA is regulated by mTORC1 and is negatively correlated with the nuclear acetate level. 1-Acetyl-DHA plays an important role in cellular metabolism and the regulation of histone acetylation.

UCB9386 is the selective and brain penetrant inhibitor for Nuak1 with a pIC50 of 10.1. UCB9386 inhibits Nuak2 and Kak2 with an inhibition rate of ca. 50% at 10 nM.

4-PivO-NMT chloride is an indole-derived AMPK signaling pathway modulator that regulates neurogenesis or neurite outgrowth by modulating AMPK activity. 4-PivO-NMT chloride holds promise for research in the fields of neurological disorders, pain, and inflammation.

ML-B01 is the orally active inhibitor for Akt and PKA with the IC50 of 2 nM and 136 nM. ML-B01 exhibits good ability to penetrate the blood-brain barrier (BBB) in the mouse brain.

Mitapivat (AG-348) hydrochloride is an orally active and selective allosteric pyruvate kinase R (PK-R) activator. Mitapivat hydrochloride accelerates the reaction of PK-R catalyzing the conversion of phosphoenolpyruvate to pyruvate, thereby promoting the glycolytic pathway, increasing the production of adenosine triphosphate (ATP) in red blood cells, and reducing the level of 2,3-diphosphoglycerate (2,3-DPG). Mitapivat hydrochloride is promising for research of pyruvate kinase deficiency and other anemia-related diseases.

Ageladine A dihydrochloride is an inhibitor of matrix metalloproteinase (MMP) isolated from the marine sponge Agelas nakamurai, possessing anti-angiogenic activity. Ageladine A dihydrochloride not only inhibits MMP-2 but also MMP-1, MMP-8, MMP-9, MMP-12, and MMP-13, with IC50 values of 4.65 μM, 2.79 μM, 907.12 nM, 1.83 μM, 767.57 nM, and 1.09 μM, respectively. Additionally, Ageladine A dihydrochloride is a pH-sensitive membrane-permeable dye that emits fluorescence in the blue-green range upon UV excitation, featuring a maximum absorption peak at 370 nm. Furthermore, Ageladine A dihydrochloride serves as a reliable and stable fluorescent pH sensor for detecting changes in intracellular pH values.

CP 524515 is a potent inhbitor of cholesteryl ester transfer protein (CETP) that leads to elevated high-density lipoprotein cholesterol levels.

Z57346765 hydrochloride is an inhibitor of phosphoglycerate kinase 1 (PGK1) that binds to the ADP-binding pocket with a KD value of 2.09 × 10⁻⁵ M, reducing PGK1 metabolic enzyme activity, glucose consumption, and lactate production. It also inhibits DNA replication, impairs DNA damage repair, and induces cell cycle arrest in kidney renal clear cell carcinoma (KIRC) cells.