Flezurafenib is an oral inhibitor of pan-RAF with potential antineoplastic activity.

Methylcarbamyl PAF C-8 is resistant to the degradation function of platelet-activating factor acetylhydrolase (PAF-AH). It has a half-life of more than 100 minutes in platelet-poor plasma and possesses the activity of inducing platelet aggregation. In NRK-49 cells overexpressing the PAF receptor, Methylcarbamyl PAF C-8 can induce the expression of c-myc and c-fos, and activate mitogen-activated protein kinase (MAPK). Additionally, Methylcarbamyl PAF C-8 can induce cell cycle arrest in the G1 phase. Methylcarbamyl PAF C-8 holds promise for research in the fields of cardiovascular diseases and anti-cancer therapy.

JX10 is a senomorphic agent. JX10 suppresses the expression of p38 MAPK and NF-κB. JX10 exhibits competent antiaging effects in C. elegans, senescent cells, and aged mice.

JD123 inhibits JNK1 activity and the expression of cJun (1-135). JD123 is a ATP-competitive p38-γ MAPK inhibitor, but not effect to ERK1, ERK2, or p38-α, p38-β or p38-δ..

DB-10 is a pro-agent of 3-nbutylphthalide (NBP). DB-10 has significantly high uptake ability via pyrilamine cationic transporters in the temperature and energy dependent manner in cells. DB-10 improves the survival rate of cells. DB-10 could rapidly convert into active original agent and increase the accumulation in the brain in vivo. DB-10 can be used for ischemic stroke study.

NUCC-0200808 (Compound 12g) is an inhibitor of MNK1 with an IC50 of 42 nM. NUCC-0200808 reduces eIF4E phosphorylation and cell viability in AML cells, and induces apoptosis. NUCC-0200808 holds promise for research in the field of leukemia.

HSND80 (Compound 1) is an orally active inhibitor of MNK/p70S6K, with Kd values of 44 nM against MNK1 and 4 nM against MNK2. HSND80 has a longer target residence time of 45 mins and 58 mins against MNK1 and MNK2 respectively. HSND80 can suppress non-small cell lung cancer (NSCLC) both in vitro and in vivo, and suppress Triple-Negative Breast Cancer (TNBC) in vitro.

Famlasertib is a potent, brain-penetrant MAP4K inhibitor with IC50s value of 0.3 nM, 23.7 nM, and 44.7 nM for HGK (MAP4K4), MLK3, and MLK1, respectively. Famlasertib shows motor neuron protection and anti-inflammatory properties. Famlasertib can be used for the study of amyotrophic lateral sclerosis (ALS).

AZ3246 is an orally active and selective inhibitor of HPK1 with an IC50 < 3 nM. AZ3246 induces IL-2 secretion in T cells with an EC50 of 90 nM. AZ3246 is a low-clearance antitumor compound.

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.