Apoptosis

Bafilomycin A1 belongs to the macrolide class of antibiotics and is a V-ATPase inhibitor (IC50=0.44 nM) that is specific and reversible. Bafilomycin A1 is an inhibitor of the late phase of autophagy, blocking the fusion of autophagosomes with lysosomes. Bafilomycin A1 also induces apoptosis.

Y-27632 dihydrochloride (Y-27632 2HCl) is an orally potent, ATP-competitive inhibitor of ROCK-I and ROCK-II. Y-27632 dihydrochloride also inhibits isolation-induced apoptosis in mouse prostate stem or progenitor cells.

Inavolisib (GDC-0077) is an orally available selective PI3Kα inhibitor with an IC50 value of 0.038 nM.It exerts its activity by binding to the ATP-binding site of PI3K, thereby inhibiting the phosphorylation of PIP2 to PIP3.

Verteporfin (BPD-MA) is a YAP inhibitor that inhibits YAP-TEAD interactions. Verteporfin is also a photosensitizer used in photodynamic therapy. Verteporfin also induces apoptosis and inhibits autophagy.

MG-132 (Z-Leu-Leu-Leu-al) is a 26S proteasome inhibitor (IC50=100 nM) that is cell-permeable and reversible. MG-132 acts as an autophagy activator and also induces apoptosis.

Atezolizumab is an antibody inhibitor, a humanized monoclonal antibody, IgG1, which targets PD-L1 and blocks the interaction of PD-L1 with PD-1. Atezolizumab has antitumor activity and promotes T-cells to attack tumor cells.

Nimbolide suppresses CDK4 CDK6 kinase activity. Nimbolide inhibits the NF-κB, Wnt, PI3K-Akt, MAPK, and JAK-STAT signaling pathways. Nimbolide causes apoptosis through the inactivation of NF-κB. Nimbolide is a triterpene derived from the leaves and flowers

Maytansinol (Ansamitocin P-0) inhibits microtubule assembly and causes microtubule disassembly in vitro.

Y-27632 is an orally potent, ATP-competitive inhibitor of ROCK-I and ROCK-II. Y-27632 also inhibits isolation-induced apoptosis in mouse prostate stem or progenitor cells.

Ruxolitinib (INCB018424) is a JAK1/2 inhibitor (IC50=3.3/2.8 nM) that is potent and selective. Rixolitinib exhibits antitumor activity and induces autophagy and apoptosis.

STM2457 is an inhibitor of the RNA methyltransferase METTL3 (IC50=16.9 nM) with selective and oral activity.STM2457 can be used in acute myeloid leukemia (AML) studies.

AOH1996 is an orally active ligand for the replicasome component PCNA (proliferating cell nuclear antigen), targeting the transcription-replication conflict (TRC). It interferes with the interaction of PCNA with its binding proteins, leading to DNA replication stress and apoptosis. AOH1996 causes proteasome-dependent rpb1 degradation and lethal DNA damage by stabilizing the interaction between PCNA and RNA polymerase II, and acts synergistically with DNA damaging agents to inhibit tumor cell growth.

Doxorubicin hydrochloride is an anthracycline antibiotic with cytotoxic and antitumor activity. It is an effective inhibitor of human DNA topoisomerase I and II, with IC50 values of 0.8 μM and 2.67 μM, respectively. In addition to inhibiting DNA topoisomerases, it can reduce the phosphorylation of AMPK and its downstream target, acetyl-CoA carboxylase. Doxorubicin hydrochloride also induces apoptosis and autophagy. In animal studies, it is commonly used to induce models of acute renal failure, chronic kidney injury, and heart failure.

Paclitaxel (Taxol) is a natural product and a microtubule polymer stabilizer. Paclitaxel has anti-tumor activity and causes cell death by inducing mitotic arrest, apoptosis, and cell autophagy.

MPTP hydrochloride is a dopamine neurotoxin and the precursor of MPP⁺. It can induce apoptosis and has the ability to cross the blood-brain barrier. MPTP hydrochloride is toxic to dopaminergic neurons and is commonly used for the construction of Parkinson's disease animal models.

Zotatifin (eFT226) is a selective eIF4A inhibitor with antiviral and anticancer activities, blocking tumor growth driven by receptor tyrosine kinases and inhibiting Sox4 translation, inducing apoptosis.

Deferoxamine (Desferrioxamine B) is an iron chelator. Deferoxamine can be used to reduce the accumulation and deposition of iron in tissues. Deferoxamine can improve neurological dysfunction by inhibiting ferroptosis and neuroinflammation after traumatic brain injury. It has antioxidant, anti-proliferation and anti-tumor activities, and can induce the production of HIF-1α, apoptosis and autophagy in cancer cells. It can be used to treat acute iron toxicity and COVID-19 related diseases.

Staurosporine (AM-2282) is a protein kinase inhibitor with ATP-competitive and non-selective inhibitory activity (IC50=6/15/2/3/3000 nM) against PKC, PKA, c-Fgr, phosphorylase kinase and TAOK2. Staurosporine also induces apoptosis.

Tamoxifen is an orally active selective estrogen receptor modulator (SERM) that acts as an estrogen antagonist in breast cells and an agonist in bone, liver, and uterine cells. It can be used to induce gene knockout and liver injury models in mice, and also exhibits multiple biological activities, including activation of Hsp90, induction of autophagy and apoptosis, and inhibition of EBOV and MARV viral infections.

DAPT (LY-374973) is a γ-secretase inhibitor that inhibits total Aβ and Aβ42 (IC50=115 200 nM) and is orally active. DAPT is also a Notch inhibitor. DAPT induces cell differentiation, autophagy and apoptosis.

LY294002 (SF 1101) is a broad-spectrum inhibitor of PI3K, inhibiting PI3Kα, PI3Kδ, and PI3Kβ (IC50=0.5/0.57/0.97 μM). LY294002 is also an inhibitor of DNA-PK (IC50=1.4 μM) and an inhibitor of CK2 (IC50=98 nM). LY294002 activates apoptosis and autophagy.

Prexasertib (LY2606368) is a selective checkpoint kinase 1 (CHK1) inhibitor (Ki 0.9 nM, IC50<1 nM). Prexasertib causes double-stranded DNA breaks and replication mutations, leading to apoptosis. Prexasertib has antitumor activity.

Mdivi-1 (Mitochondrial division inhibitor 1) is a mitochondrial division inhibitor that inhibits DRP1 and Dynamin I (IC50=1-10 μM). Mdivi-1 inhibits mitochondrial autophagy.

Romidepsin (FR 901228) is an HDAC inhibitor that inhibits HDAC1 2 4 6 (IC50=36 47 510 1400 nM). Romidepsin has antitumor activity and can be used for the treatment of peripheral T-cell lymphoma and cutaneous T-cell lymphoma.