Apoptose

Malformin A, from A. niger, is a plant growth regulator and has anti-TMV and cancer cell cytotoxic properties. Intraperitoneal LD50 in mice is 3.1 mg/kg.

NecroIr1, an iridium(III) complex, induces necroptosis in Cisplatin-resistant lung cells, targeting mitochondria and disrupting MMP.

PARP-1/2-IN-2-IN-1 (Compound 12e) effectively inhibits PARP1/2 and CDK12 with IC 50 values of 34 nM, 30 nM, and 285 nM respectively, impairing DNA damage repair

Ganoderic acid Mf: antitumor triterpenoid, arrests G1 cell cycle, selective for cancer cells, triggers apoptosis via mitochondria.

PD-L1degrader-2 (Compound B3) is an orally effective AUTAC degrader that degrades PD-L1 via the autophagy-lysosome pathway with a DC50 of 0.5 μM. It inhibits the interaction between PD-1 and PD-L1, with an IC50 of 22.8 nM. PD-L1degrader-2 upregulates the expression of Atg9b, Lamp1, and Mitf, activating the autophagy-lysosome system. It exhibits antitumor activity in the CT26 mouse model.

Rat form of the beta-Amyloid (1-40) peptide

Emavusertib Tosylate (also known as CA-4948) is a potent inhibitor of IRAK4/FLT3 with demonstrated antitumor activity. In cell lines such as ABC DLBCL and AML, CA-4948 exhibits strong cellular efficacy. Among 329 evaluated kinases, it shows medium to high selectivity. The compound has excellent oral bioavailability and favorable pharmacokinetic properties in ADME and PK profiles. In preclinical models involving mice, rats, and dogs, CA-4948 demonstrated good oral bioavailability and displayed over 90% tumor growth inhibition in relevant tumor models, correlating well with in vivo pharmacodynamic regulation.

Disitertide (P144) is a TGF-β1 receptor blocker, PI3K inhibitor, and apoptosis inducer.

Prodigiosin hydrochloride is a bioactive red pigment from bacteria with antibacterial, antifungal, anticancer properties, and inhibits Wnt/β-catenin.

Nauclefine, a plant alkaloid, triggers cancer cell death through PDE3A-SLFN12, binding but not inhibiting PDE3A.

USP1-IN-11 (compound 38-P2) is a selective, reversible, and non-competitive inhibitor of USP1 (Ubiquitin-specific protease 1). It activates the DDR (DNA damage repair) pathway, leading to cell cycle arrest and apoptosis, thereby inhibiting cell survival. USP1-IN-11 increases sensitivity to Olaparib in drug-resistant cells and works synergistically with Andrographolide in cancer cells with functional BRCA. In the MDA-MB-436 xenograft model, USP1-IN-11 demonstrates significant dose-dependent antitumor activity.

RA-XII is a useful organic compound for research related to life sciences. The catalog number is T125868 and the CAS number is 143343-98-0.

Arisostatin A is a secondary metabolite produced by microorganisms, recognized as an antibiotic (antibiotic) with activity against Gram-positive bacteria. This compound also exhibits potent antitumor properties. It induces apoptosis (apoptosis) by activating caspase-3 and generating reactive oxygen species (ROS) in AMC-HN-4 cells.

YB-0158 ammonium (Wnt pathway inhibitor 2 ammonium) is a reverse-rotation peptidomimetic with translation-enhancing potential and anticancer activity.

HSP90-IN-18 inhibits Hsp90 with 0.39 μM IC50, useful for viral, neurodegenerative, and inflammatory research.

Thymidine 3',5'-diphosphate tetrasodium inhibits staphylococcal nuclease, SND1 & tyrosyl nuclease; has anti-tumor properties & catalyzes biochemical reactions.

NS3694 is an inhibitor of apoptosis and inhibits apoptosome formation and caspase activation.

YL5084 is a selective JNK2/3 inhibitor with IC50s: JNK2 (70 nM), JNK3 (84 nM), and antiproliferative, apoptosis-inducing effects.

Thalidomide-5-propoxyethanamine acts as a cereblon (CRBN) ligand derived from Thalidomide, and it serves the purpose of recruiting the CRBN protein.

KRASG12C IN-16 (Compound SK-17) is a selective, covalent, and orally active KRASG12C inhibitor. It can induce apoptosis and effectively prevent the activation of the MAPK and PI3K/mTOR signaling pathways. Additionally, KRASG12C IN-16 exhibits antitumor activity against pancreatic cancer.

VTP50469 fumarate is a highly selective and orally active inhibitor of Menin-MLL interaction (Ki: 104 pM), and has potently anti-leukemia activity.

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.

IPH10 is an anticancer agent with strong antitumor effects in vivo and exhibits no liver or kidney toxicity. It significantly increases the reactive oxygen species (ROS) levels in tumor cells, decreases mitochondrial membrane potential, and induces apoptosis (apoptosis) in these cells.

Conjugated 18-C ω-6 fatty acid from Jacaranda seeds, induces cancer cell apoptosis via oxidative stress; metabolizes to cytotoxic CLA.

Apoptosis Inducer 11 (compound 3u) promotes apoptosis via the mitochondrial pathway and elicits a G2/M block alongside a marked reduction in the S phase within

5-LOX-in-2: a 5-lipoxygenase inhibitor with IC50 of 0.33 μM, reduces kidney cancer cell activity, induces apoptosis.

Anticancer Agent 146 (Compound 1.19) acts as a necroptosis inducer and demonstrates anti-tumor efficacy in the MDA-MB-231 mouse xenograft model [1].

Compound 9a, a withanolide, induces apoptosis and has anti-cancer properties.

Flaccidoside II, an active triterpenoid saponin from Anemone flaccida rhizome, both inhibits proliferation and induces apoptosis in Malignant Peripheral Nerve

Multi-kinase-IN-4 (compound 5d) is a multi-targeted kinase inhibitor active against VEGFR2, EGFR, HER2, and CDK2, with respective IC50 values of 0.33, 0.22, 0.

TAT-NEP1-40, a blood-brain barrier (BBB) permeable peptide, confers protection to PC12 cells against oxygen and glucose deprivation (OGD) while promoting

TAT-NEP1-40 TFA, a blood-brain barrier-permeable peptide, safeguards PC12 cells against oxygen and glucose deprivation (OGD) and fosters neurite outgrowth.

TG101209 analog 1 (Compound 8h) serves as an inhibitor of BUB1B, exhibiting an IC50 of 10.36 μM. It also possesses cytotoxic properties, demonstrated by an IC50 of 1.347 μM against Caki-1 cells, and can induce necrosis and apoptosis.

AXL/Angiokinase-IN-1 (compound 11b) is an inhibitor of AXL/triple angiokinase, with an IC50 of 3.75 nM for AXL expression. This compound suppresses epithelial-mesenchymal transition (EMT) in Bxpc-3 cells and prevents metastasis in lung cancer cells. Additionally, AXL/Angiokinase-IN-1 impairs the functions of vascular and fibroblast cells and induces apoptosis in both cancer and fibroblast cells. It is characterized by low toxicity and favorable metabolic stability.

CYP51/PD-L1-IN-1 (compound L11), a quinazoline with antifungal properties, simultaneously inhibits CYP51 (IC50: 0.884 μM) and PD-L1 (IC50: 0.083 μM).

RIPK2-IN-2, a RIP2 kinase PROTAC inhibitor, blocks proinflammatory signaling in autoinflammatory diseases.

CAY10726, an arylurea fatty acid, cuts ATP by 28% and promotes apoptosis in breast cancer cells by depleting mitochondrial lipids.

XM-U-14 is a selective PROTAC USP7 degrader that induces the degradation of USP7 in the RS4;11 cell line with a DC50 of 0.74 nM. This compound elevates the levels of p53 and p21, and significantly inhibits the growth of acute lymphoblastic leukemia (ALL) cells, with IC50 values of 0.5 nM in RS4;11 cells and 8.3 nM in Reh cells. Moreover, XM-U-14 induces apoptosis and cell cycle arrest, and effectively inhibits tumor growth.

Zapalog: photocleavable dimerizer controlling instant protein interactions.

eIF4E-IN-1 inhibits eIF4E and boosts immunity by targeting PD-1, PD-L1, LAG3, TIM3, IDO, aiding cancer and infection treatment.

Thalidomide-NH-PEG3-COOH is a cereblon-based E3 ligase ligand-linker for PROTAC synthesis.

Anticancer agent 52 exhibits potent cytotoxicity, induces apoptosis, and has potential in bladder cancer research.

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.

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.

p38α inhibitor6 (compound 19) is a p38α inhibitor with an IC50 value of 0.68 μM. It induces apoptosis, arrests the cell cycle in the G0 and G2/M phases, reduces TNF-α concentration, upregulates the expression of the tumor suppressor gene p53, increases the Bax/BCL-2 ratio, and activates caspase3/7.

PI3K/HDAC-IN-4 (Compound 31f) is a dual inhibitor targeting PI3K and HDAC, with an IC50 of 0.2μM. It demonstrates high selectivity for HDAC1-3, with IC50 values of 75.5 nM, 70.9 nM, and 1.9 nM, respectively. As a potent pan-PI3K inhibitor, PI3K/HDAC-IN-4 has IC50 values of 2.5 nM, 80.5 nM, 10.0 nM, and 57.2 nM for PI3Kα, β, δ, and γ, respectively. This compound effectively induces apoptosis in tumor cells by concurrently inhibiting the PI3K/AKT/mTOR signaling pathway and HDAC1-3. It shows significant antiproliferative activity across various tumor cell lines, such as MV4-11, Jeko-1, HL60, and MCF-7, with IC50 values of 0.2, 0.9, 0.8, and 1.5 μM, respectively. PI3K/HDAC-IN-4 is applicable in the study of lymphoma and leukemia.

Mcl1-IN-26 is an effective and selective myeloid cell leukemia 1 inhibitor.

HC Toxin: cyclic tetrapeptide, reversible HDAC inhibitor (IC50=30 nM), upregulates 15-lipoxygenase-1, induces fetal hemoglobin, from C. carbonum.

Ganoderic acid T1, a derivative of Ganoderic acid T, triggers cancer cell apoptosis by boosting ROS and activating caspases.

Sodium valproate is an anti-epileptic, boosting brain GABA levels and possibly affecting potassium channels for membrane stability.

Ilicicolin A is a useful organic compound for research related to life sciences. The catalog number is T125289 and the CAS number is 22581-06-2.

TrxR-IN-7 (14f) is a potent inhibitor of thioredoxin reductase (TrxR), with an IC50 value of 3.5 µM. It exhibits antiproliferative activity and can induce apoptosis and the production of reactive oxygen species (ROS).

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.

TS-IN-5 (Compound 15) is an inhibitor of thymidylate synthase (TS). It induces apoptosis by modulating the proteins Bax, BCL-2, PI3K, and STAT1. TS-IN-5 exhibits antitumor activity against liver cancer, breast cancer, and colon 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.

NSC243928 mesylate binds to human lymphocyte antigen 6 (LY6), a cell growth inhibitor with anticancer activity.

HEMTAC CDK4/6 degrader 1, a PROTAC targeting HSP90/CDK4/6, Kd of 35.7 μM, disrupts B16F10 melanoma cell cycle, and induces apoptosis.

AZD1152 is a pro-drug of Barasertib (AZD1152)-hQPA. Which is a highly selective Aurora B inhibitor with IC50 of 0.37 nM in a cell-free assay.

2,5-Dimethylcyclohexa-2,5-diene-1,4-dione inhibits the viability of HL60 and K562 cells and exhibits antibacterial and anticancer properties.

Delmitide, a TNF-alpha production inhibitor, is used potentially for the treatment of Crohn's disease and ulcerative colitis.

EGFR-IN-143 (Compound 5f) is a potent EGFR inhibitor with an IC50 value of 0.15 μM. It induces apoptosis by arresting the cell cycle at the G2/M phase and exhibits antitumor activity.

NSC90616 is a mutant p53 rescue compound [1] .

Monactin is a Marcrotetrolide antibiotic produced by cycloheximide producing species of Streptomyces. It is a homolog of nonactin from the same species.

Akt/NF-κB/MAPK-IN-1 (compound 2m) serves as a potent, orally active inhibitor targeting NO with an IC50 of 7.70 μM and demonstrates low toxicity.

Nargenicin: a macrolide antibiotic effective against S. aureus, MRSA, M. luteus; inhibits bacterial DnaE and reduces inflammation and leukemia cell growth.

Galloflavin Potassium is an inhibitor of lactate dehydrogenase.

YCH3124 (compound Z33) is an inhibitor of USP7, exhibiting anti-tumor activity with an IC50 value of 41.9 nM. This compound demonstrates substantial in vitro anti-proliferative effects on various tumor cells, including LNCaP (IC50= 3.6 nM) and CHP-212 (IC50=9.9 nM). Moreover, YCH3124 induces apoptosis in CHP-212 cells by disrupting the cell cycle process during the G1 phase.

TD1092, a pan-IAP degrader, activates caspase 3/7, induces apoptosis in cancer cells, inhibits NF-κB, and is used in cancer research.

TNF-α-IN-9 is an NDM-1 inhibitor-3 analog and is a TNF-α inhibitor.TNF-α-IN-9 shows low inhibitory activity.

Photosensitizer-5, a photodynamic agent, exhibits cytotoxicity towards HeLa and HepG2 cells, with IC50 values of 10.4 nM and 6.9 nM, respectively. It induces cell death through lipid peroxidation via an iron-independent ferroptosis pathway. Additionally, Photosensitizer-5 displays antitumor activity in HeLa-tumor-bearing mice.

RO7567132 is a bispecific antibody that binds and agonizes LTBR bivalently while binds and antagonizes FAP monovalently, inducing the formation of local TLS.

C8 D-threo Ceramide, a potent bioactive sphingolipid, is cytotoxic with IC50=17µM, enhances DNA fragmentation and pore formation, and activates CAPK.

XIAP BIR2/BIR2-3 inhibitor-1 (compound 3) serves as a potent dual inhibitor targeting BIR2 and BIR2-3 domains, with IC50 values of 1.9 nM and 0.8 nM, respectively. This compound is utilized in cancer research studies [1].

TD52 dihydrochloride, an Erlotinib derivative, inhibits protein phosphatase 2A and induces apoptosis in TNBC by disrupting CIP2A/PP2A/p-Akt signaling.

RET-IN-4: Oral RET inhibitor, IC50 ~1 nM for variants. Selective over JAK2/FLT3. Potent anticancer use.

L 683519 is one of the Tacrolimus impurities with immunosuppressant and could restrain the activity of FK-506 binding protein.

Enpp/Carbonic anhydrase-IN-2 is a potent dual inhibitor of Enpp and carbonic anhydrase, inhibiting NPP1, NPP2, NPP3, CA-IX, CA-XII, with IC50 values of 1.13, 1.

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

Mcl-1 antagonist 1 is a Mcl-1 protein antagonist.

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.

Thalidomide-O-amido-PEG4-propargyl is a polyethylene glycol (PEG)-based linker employed for the synthesis of proteolysis targeting chimeras (PROTACs)[1].

MDM2ligand 4 is a ligand of MDM2 and can be used in the synthesis of the PROTAC degrader [KT-253].

PARP1-IN-27 (Compound 9B) serves as an inhibitor of both PARP1 and PARP2, exhibiting IC 50 values of 2.53 nM and 6.45 nM, respectively, in SUM149PT cells. This compound effectively suppresses the proliferation of BRCA-mutated cancer cell lines such as SUM149PT, HCC1937, and Capan-1, with respective IC 50 values of 0.62, 1.91, and 4.26 μM. Additionally, PARP1-IN-27 exacerbates DNA double-strand breaks, enhances ROS production, causes G2/M phase cell cycle arrest, and triggers apoptosis in SUM149PT cells.

CPTH2 is an inhibitor of the HAT activity of Gcn5.

FHD-286 is an inhibitor of BRM/BRG1 ATPase and can be used for studies on the treatment of BAF-related disorders such as acute myeloid leukemia.

A unique collection of 420 compounds targeting PI3K/Akt/mTOR signaling for research in PI3K/Akt/mTOR signaling, and drug discovery in diseases involved with

ERK-IN-6, a potent agent, inhibits ESCC growth and induces apoptosis through the ERK pathway.

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

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.

NEP162 is a BRD4 PROTAC degrader with DC50 values of 1.2 μM in SW480 cells and 1.6 μM in U2OS cells. NEP162 exhibits antiproliferative activity, effectively inhibiting tumor growth and inducing apoptosis. It is applicable in research on cancers such as osteosarcoma, colorectal cancer, and non-small cell lung cancer.

Compound 7, also known as RAR/RXR agonist-1, is a chlorinated isomer of retinoic acid and acts as a selective RARα agonist and a partial RXRα agonist. It is capable of activating RXRα, thereby inducing G2/M arrest and apoptosis in cancer cells.

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.

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

7-Methoxy-1-tetralone may have insecticidal activity.

W 7 is a biochemical.

FLT3/IRAK4-IN-1 is a selective inhibitor of FLT3 and IRAK4, exhibiting significant activity against FLT3-WT (IC50= 1.95 nM), FLT3-D835Y (IC50= 3.22 nM), and IRAK4 (IC50= 53.72 nM). It demonstrates low cytotoxicity towards normal bone marrow cells, effectively promotes apoptosis, and has potential to overcome resistance. FLT3/IRAK4-IN-1 can be utilized in studies of acute myeloid leukemia (AML).

Curzerene, a sesquiterpene compound derived from the rhizome of Curculigo orchioides Gaertn, possesses potent anti-cancer properties.