Apoptosis

Autophagy-IN-1 blocks autophagy in cancer cells, hinders tumor growth in mice, and aids in studying colorectal cancer.

DHU-Se1: potent anti-inflammatory, releases reactive selenium from macrophages, inhibits iNOS/TNF-α, blocks M0 to M1 polarization.

RET-IN-7 exhibits strong inhibitory effects against RET kinase in vitro and shows significant efficacy in treating RET-driven tumor xenografts in mice through

CK156 inhibits DAPK with high selectivity; IC50: 182 nM (DRAK1), 34 μM (CK2a1), 39 μM (CK2a2); key in autoimmune/inflammation research.

Z-3578 is a small molecule antagonist targeting the MrgX2 (Mas-related G protein-coupled receptor X2) with notable anti-pseudoallergic properties, exhibiting a KD value of 729 nM. It effectively inhibits mast cell degranulation induced by substance P (SP) and C48/80, with IC50 values of 4.90 µM and 6.18 µM, respectively, suppresses the release of β-hexosaminidase, and significantly reduces the release of histamine and TNF-α, as well as intracellular calcium flux. Additionally, in a mouse pseudoallergy model, Z-3578 significantly alleviates foot swelling, dye leakage, and reduces serum histamine levels, indicating a strong in vivo anti-allergic effect. Z-3578 presents as a promising lead compound in the field of anti-allergic treatments, particularly for pseudoallergic reactions.

FLT3/TrKA-IN-1: Potent dual kinase inhibitor for FLT3 & TrKA, promising for AML research.

Anticancer agent 64 (5m) induces apoptosis, has IC50 2.4μM in CCRF-CEM, activates caspases, cleaves PARP, affects mitochondria.

D18: Dual agonist for TLR7/8, boosts PD-L1, aids tumor sensitivity to PD-1/PD-L1 inhibitors, and is a cytotoxin for ADC HE-S2.

HDAC-IN-37 inhibits HDACs 1, 3, 8, & 6, induces histone acetylation, halts G1 to S phase, and triggers early apoptosis.

Potent dual c-Met/HDAC inhibitor, IC50: HDAC1 5.4 nM, c-Met 18.49 nM; anti-cancer, induces apoptosis, G2/M arrest in HCT-116.

Sinulatumolin E, a terpenoid, inhibits TNF-α (IC 50: 3.6 μM); has anti-inflammatory properties.

ASK1-IN-8 (Compound 35) is an orally active inhibitor of apoptosis signal-regulating kinase 1 (ASK1) with an IC50 value of 1.8 nM. In a mouse liver injury model induced by Acetaminophen, ASK1-IN-8 significantly reduces plasma alanine aminotransferase (ALT) levels, offering liver protection. This compound is useful for research in liver disease-related fields.

XPO1-IN-1: an oral MM.1S cell inhibitor (IC50: 24 nM), induces apoptosis, stable metabolism, good pharmacokinetics.

EGFR-IN-62: IC50 of 10-242 nM for various EGFR mutations, blocks A549/H1975 cell cycle, induces apoptosis, and inhibits cell motility and proliferation.

Tubulin inhibitor 13 (E27), IC50 16.1 μM, blocks tubulin polymerization, cancer cell migration, and invasion, induces apoptosis.

PARP10/15-IN-2 (Compound 8h) blocks PARP10/15, has IC50s: 0.15μM/0.37μM, cell-permeable, prevents apoptosis.

CDK4/6-IN-10: Oral CDK4 (IC50: 22 nM) & CDK6 (IC50: 10 nM) inhibitor with anti-cancer potential for MM research.

BCL6-IN-9 (compound 1) is a potent inhibitor of B-cell lymphoma 6 protein (BCL6) (IC50: 3.9 nM) and can be used to study cancer.

Anticancer agent 65: Effective on A549 cells, IC50 1.07 μM, halts S phase, triggers apoptosis, elevates p53/p21, causes ROS and MMP collapse.

GL0388, a Bax activator, induces apoptosis, hinders breast cancer growth, and has IC50 of 0.299-1.57 μM.