Apoptosis

DPP-4-IN-8 (compound 27) is a potent and selective inhibitor of dipeptidyl peptidase 4 (DPP4), with an inhibition constant (Ki) of 0.96 μM.

Euphjatrophane M (Compound 6) is a FOXO1 inhibitor that reduces NF-κBp65 phosphorylation and exhibits anti-inflammatory properties. It can inhibit the production of nitric oxide and also suppress the mRNA expression of IL-6, IL-1β, and TNFα in LPS-induced RAW 264.7 macrophages.

Thalidomide-O-C5-acid, a synthesized E3 ligase linker, merges cereblon and PROTAC tech.

Narasin inhibits dengue virus, treats coccidiosis without harm to cells, and induces cancer cell apoptosis.

Compound PDK0379, with CAS No. 86-73-7, is a fragment molecule that serves as an important scaffold for molecular linking, expansion, and modification. Compound PDK0379 provides a structural basis and research tool for the design and screening of novel drug candidates, and is commonly used in drug discovery, drug synthesis, and related research.

22-SLF is a PROTAC degrader that operates by FBXO22-dependent degradation of FK506 Binding Protein 12 (FKBP12) with a DC50 of 0.5 µM. Additionally, 22-SLF can degrade other endogenous proteins, such as BRD4 and the EML4-ALK fusion protein (EML4-ALK fusion protein).

EGFR-IN-83 (Compound 9), an EGFR inhibitor with an IC50 of 2.53 nM, exhibits antiproliferative effects on MCF-7 and MDA-MB-231 cell lines, with respective IC50

Thyrotropin (TSH), a thyroid-stimulating hormone, is synthesized by thyrotrope cells in the anterior pituitary gland and modulates the endocrine activity of the

Trehalose-6,6'-dibehenate, a bioactive glycolipid, is applicable for the preparation of vaccine adjuvant [1].

cis,trans-Germacrone is an antitumor, antioxidant isomer that inhibits lung cancer and affects Akt/MDM2/p53.

Triphenyl phosphate is an flame retardant and endocrine disruptor that activates MAO-A/ROS/NF-κB pathways, disrupting placental tryptophan metabolism.

NSC 15830 (S-(1,2-Dichlorovinyl)-L-cysteine) hydrochloride is a nephrotoxic compound that serves as a metabolite of trichloroethylene. This compound is capable of inhibiting TNF-α stimulated by pathogens.

MPP hydrochloride is a selective estrogen receptor (ERR) modulator.

Anticanceragent 205 (compound 9) is an effective anticancer agent that binds to the G4-mtDNA target, inhibiting the replication, transcription, and translation of mtDNA (mitochondrial genome). It induces mitochondrial dysfunction, increases ROS production, and triggers DNA damage and cellular senescence. Anticanceragent 205 also promotes apoptosis and causes cell cycle arrest at the G0/G1 phase, showing potential for research in colorectal cancer.

Emavusertib Phosphate (also known as CA-4948) is a potent inhibitor of IRAK4 and FLT3, exhibiting antitumor activity. In ABC DLBCL and AML cell lines, it demonstrates significant cellular efficacy. Furthermore, CA-4948 shows moderate to high selectivity across a panel of 329 kinases and possesses favorable ADME and PK profiles, including good oral bioavailability in mice, rats, and dogs. It achieves over 90% tumor growth inhibition in relevant tumor models and correlates excellently with in vivo PD modulation.

2,2-Dimethyl-2,3-dihydrobenzofuran-7-ol inhibits the proliferation of the THP-1 cell line and anti-infective Leishmania and Toxoplasma gondii RH.

PROTAC EGFR degrader 6 effectively degrades EGFR Del19 in HCC827 cells (DC50=45.2 nM) and induces apoptosis and G1 arrest.

CYP51/PD-L1-IN-2 (compound L20), a quinazoline with antifungal properties, is a potent dual inhibitor targeting both CYP51 (IC50: 0.263 μM) and PD-L1 (IC50: 0.

EGFR-IN-144 (Compound 4B) inhibits EGFR (IC50=0.639 µg/mL) and tubulin polymerization (IC50=7.339 µg/mL). It exhibits cytotoxicity in various cancer cells with a GI50 at the nanomolar level. EGFR-IN-144 reduces the expression of mTOR, TNF-α, and IL-6, causes G1/S phase cell cycle arrest, and induces apoptosis.

CXCR4-IN-2 (compound A1), a potent bifunctional fluorinated small molecule, inhibits CXCR4 and exhibits anticancer properties by exerting cytotoxicity (IC 50:

LWY713 is a PROTAC-based FLT3 degrader (DC50=0.64 nM) that selectively induces FLT3 degradation through a cereblon and proteasome-dependent mechanism. It inhibits cell proliferation and causes G0/G1 phase arrest and apoptosis (apoptosis) in MV4-11 cells. In MV4-11 xenograft models, LWY713 demonstrates significant in vivo antitumor activity. The E3 ligase ligand and linker consist of Lenalidomide-Glycolic acid, while the target protein ligand's active control is NaproxenGilteritinib.

NLRP3-IN-62 (Compound 1) is an inhibitor of NLRP3. It effectively inhibits pyroptosis in THP-1 cells with an IC50 of 0.7 nM and suppresses IL-β release with an IC50 of 108.5 nM.

CSN5-IN-2 (Compound 31) is a CSN5 inhibitor with an IC50 of 0.36 μM. It increases Cullin 1 neddylation levels in cancer cells and downregulates the expression of RAD51 and PD-L1. CSN5-IN-2 exhibits antitumor activity, which is enhanced when used in combination with Talazoparib.

YB-0158 inhibits Wnt, targets colorectal CSCs, disrupts Sam68/Src, induces apoptosis, and has anti-cancer properties.

Anti-TNBC agent-8 (Compound TP2) is a photodynamic therapeutic compound that targets mitochondrial DNA G-quadruplexes (mtG4). Under white light exposure, it exhibits an IC50 of 0.42 μM against 4T1 cells. Anti-TNBC agent-8 tightly binds to mtG4, leading to the production of substantial reactive oxygen species (ROS) under illumination. This results in the loss of mitochondrial membrane potential (MMP), reduced ATP production, elevated ROS levels, and significant apoptosis in triple-negative breast cancer (TNBC) cells, thus demonstrating its tumor growth inhibitory activity. Anti-TNBC agent-8 is applicable for research in TNBC.

EM 163是一种 TIR-TIR 相互作用抑制剂，它是MyD88蛋白的TIR（Toll/白细胞介素-1受体）结构域拟态。EM 163针对IL-1受体中的TIR 结构域，阻断与MyD88的相互作用。EM 163抑制葡萄球菌肠毒素B（SEB）引起的体内炎症细胞因子的产生。EM 163能保护小鼠免受SEB 冲击引起的死亡。在体外的大鼠海马神经元中，EM 163阻断p38的激活和IL-1β对化学诱导的长期电位（LTP）引发的蛋白质合成的抑制作用。

5-HT1AR Agonist 2 (Compound 4f) is a potent agonist of the 5-HT1A receptor with a Ki value of 10.0 nM. It also binds to SERT, D2, and 5-HT6 receptors with Ki values of 2.8 nM, 23 nM, and 192 nM, respectively. Furthermore, this compound demonstrates stability in microsomes and induces hypothermia in mice.

Citreoviridin from Penicillium citreoviride blocks brain Na+/K+-ATPase; boosts Na+/K+- and Mg2+-ATPase in microsomes dose-dependently.

Amiloride hydrochloride dihydrate (Amiloride HCl dihydrate) is a pyrazine compound inhibiting SODIUM reabsorption through SODIUM CHANNELS in renal EPITHELIAL CELLS. This inhibition creates a negative potential in the luminal membranes of principal cells, located in the distal convoluted tubule and collecting duct. Negative potential reduces secretion of potassium and hydrogen ions. Amiloride hydrochloride dihydrate is used in conjunction with DIURETICS to spare POTASSIUM loss.

FLT3-IN-28 (Compound 12y) is an orally active FLT3 inhibitor with antitumor properties. It selectively targets cancer cells with FLT3 internal tandem duplication (ITD) mutations, demonstrating IC50 values of 85, 290, 130, 65, and 220 nM against BaF3-FLT3-ITD, BaF3-TEL-VEGFR2, MV4-11, MOLM-13, and MOLM-14 cell lines, respectively. These lines include acute myeloid leukemia (AML) cells harboring FLT3-ITD mutations such as MV4-11 and MOLM-13/14. The compound also reduces phosphorylation levels of FLT3 and STAT5 in MOLM-13 cells, leading to cell cycle arrest and apoptosis. With an oral bioavailability of 19.2% in SD rats, FLT3-IN-28 extends survival in a dose-dependent manner in MOLM-13 xenografted NSG mouse models. It holds promise for research in FLT3-ITD-related cancer studies.

FF2049 is a selective HDAC PROTAC degrader with a DC50 of 257 nM for HDAC1. It facilitates the ubiquitination and degradation of HDAC and promotes apoptosis (Apoptosis). FF2049 is applicable in research involving hematological and solid tumors.

Mitochondria modulator-2 (Compound Ir1) induces depolarization of the mitochondrial membrane potential, generates reactive oxygen species (ROS), inhibits the migration of A549 cells, causes cell cycle arrest at the G2/M phase, and triggers apoptosis in A549 cells.

Antioxidant agent-20 (Compound 3d) exhibits potent anti-inflammatory and antioxidant activities. It reduces reactive oxygen species (ROS) and apoptosis in a dose-dependent manner. Antioxidant agent-20 demonstrates photoprotective effects on UVB-exposed human skin keratinocytes (HaCaT) (IC50=5.13 µM) by activating Nrf2/HO-1 signaling and inhibiting the NF-κB pathway.

Taxamairin B is a potent anti-inflammatory compound that inhibits the expression of proinflammatory cytokines (TNF-α, IL-1β, and IL-6) and reduces the

SH-5, an AKT inhibitor potentiates apoptosis and inhibits invasion through the suppression of anti-apoptotic, proliferative and metastatic gene products

Bfl-1-IN-6 (Compound 20) is an orally active inhibitor of Bcl-2-related protein A1 (BFL1) with an IC50 of 19 nM. This compound can stabilize BFL1 protein, activate cleaved caspase 3, and demonstrates antitumor activity in mouse models.

BGC4 is a gold(III) complex based on biphenyl. It inhibits human recombinant thioredoxin reductase (TrxR) with an IC50 of 10.7 μM, exhibits cytotoxicity with an IC50 of 5.4 μM in MDA-MB-231 cells, and induces apoptosis. Additionally, BGC4 demonstrates antitumor activity in mouse models.

HPCR exhibits antiproliferative activity against various cancer cells and is involved in apoptosis (apoptosis).

LD4172 is a PROTAC degrader capable of degrading RIP kinase (RIPK1) with a DC50 in the nanomolar range. When used in combination with TNF-α, LD4172 can induce apoptosis in B16F10 cells. In mouse models, it demonstrates antitumor activity. (Pink: ligand for target protein; Black: linker; Blue: ligand for E3 ligase VHL)

FKBP12 ligand-1 is the target protein ligand for MC-25B, which is a PROTAC targeting FKBP12.

DD0-2363 (Compound 32d) is a dual-target inhibitor of WDR5-MLL1/HDAC. It can suppress the proliferation of acute myeloid leukemia cells and induce apoptosis. With its antitumor properties, DD0-2363 is applicable for research on acute myeloid leukemia.

FAK-IN-24 (Compound 9f) is a potent FAK inhibitor with an IC50 of 0.815 nM. It induces DNA damage and apoptosis, and exhibits activity against glioblastoma. FAK-IN-24 effectively inhibits proliferation of glioblastoma cell lines U87-MG (IC50= 15 nM) and U251 (IC50= 20 nM), and suppresses tumor growth in U87-MG xenograft models.

TCF4/β-catenin-IN-1 (Compound 8b) is an inhibitor of TCF4/β-catenin that induces apoptosis. This compound enhances the expression of p53, caspase-3, caspase-8, caspase-9, and Bax proteins, while reducing Bcl-2 protein levels. TCF4/β-catenin-IN-1 also inhibits CYP3A4, CYP1A2, and CYP2C19, demonstrating significant cytotoxic activity in cancer cells.

GD3 Ganglioside sodium is a crucial ganglioside in human melanoma and functions as an inducer of mitochondrial permeability. It targets mitochondria directly in a manner controlled by bcl-2. Following the aggregation of death-inducing receptors, ceramide accumulates rapidly, synthesizes GD3 ganglioside, and triggers apoptosis.

HYS-072 is an orally active derivative of chrysin with antitumor properties. It induces apoptosis (Apoptosis) and autophagy (Autophagy) by inhibiting the PI3K/AKT/mTOR signaling pathway, and suppresses tumor growth in xenograft models in vivo by modulating autophagy-related pathways. HYS-072 is applicable for research in treating triple-negative breast cancer.

Tubulin-IN-53 is a potent inhibitor of microtubulin (Tubulin) with an IC50 of 6.06 μM. By targeting the colchicine binding site on tubulin, Tubulin-IN-53 hinders tubulin polymerization, disrupting the microtubule network. It induces cell cycle arrest at the G2/M phase and apoptosis (apoptosis) in MCF-7 cells, while inhibiting cell migration. This compound also leads to a reduction in mitochondrial membrane potential and an increase in reactive oxygen species (ROS) accumulation. Additionally, Tubulin-IN-53 disrupts angiogenesis in human umbilical vein endothelial cells and is applicable in research on cancers such as breast and lung cancer.

FKBP12 Ligand-Linker Conjugate 1 is a complex comprising a target protein ligand for FKBP12 and a linker, which is utilized in the synthesis of the PROTAC degrader MC-25B.