Apoptosis Inducer

Apoptosis inducer 45 is an apoptosis inducer. Apoptosis inducer 45 is cytotoxically active against the MCF-7 cell line. Apoptosis inducer 45 elicits MCF-7 cell apoptosis via the mitochondrial pathway (increases the Bax/Bcl-2 ratio) by activating cleavage of caspase-9, thereby inducing the fragmentation of DNA repair protein PARP. Apoptosis inducer 45 also can induce caspase-8 cleavage, subsequently initiating cleavage of caspase-3 and its downstream protein PARP to culminate in the extrinsic apoptosis. Apoptosis inducer 45 can be used in the research of breast cancer.

Viridiflorol is an active natural molecule with anti-cancer effect. Viridiflorol induces anti-neoplastic effects on breast (MCF-7, IC₅₀ = 10 µM), lung (A549, IC₅₀ = 30 µM), and brain (Daoy, IC₅₀ = 0.1 µM) cancer cells through apoptosis. Viridiflorol can be used for breast, lung, and brain cancer research.

[Ru(dpp)(bpy)(mtmp)](PF6)2 (Compound 5) is a trisheteroleptic ruthenium complex. [Ru(dpp)(bpy)(mtmp)](PF6)2 has a light-activated anticancer activity. [Ru(dpp)(bpy)(mtmp)](PF6)2 can selectively cleave off upon green light irradiation, thereby releasing a phototoxic ruthenium-based photoproduct that binds to nuclear DNA, induces DNA damage and apoptosis in cancer cells. [Ru(dpp)(bpy)(mtmp)](PF6)2 can be used for phototherapy of cancers like conjunctival melanoma research.

CDK2-IN-50 is a CDK2 inhibitor (IC₅₀ = 0.77 nM). CDK2-IN-50 can induce G1 phase arrest, indicating that it has an effective CDK2/cyclin E targeting mechanism. CDK2-IN-50 also has a significant pro-apoptotic effect. CDK2-IN-50 can be used for the study of breast cancer.

Scr-IN-1 (Compound 4e) is a Tyrosine kinase inhibitor. Scr-IN-1 inhibits HCT-116 cells and MIA-PaCa-2 cells with IC₅₀s of 0.16 μM and 1.16 μM, respectively. Scr-IN-1 displays selectivity profile on HCT-116 cells and MIA-PaCa-2 cells with SI > 625 and SI > 86, respectively. Scr-IN-1 induces Apoptosis in HCT-116 colon cancer cell and does not cause any change in the rate of necrotic cells. Scr-IN-1 is a novel SRC kinase inhibitor candidate for HCT-116 cells. Scr-IN-1 is potential for cancer research.

Dynorphin A TFA is an endogenous opioid peptide involved in inhibitory neurotransmission in the central nervous system (CNS). Dynorphin A TFA is a highy potent kappa opioid receptor (KOR) agonist, and is also an agonist for other opioid receptors, such as mu (MOR) and delta (DOR). Dynorphin A TFA can induce neuronal death, and can be used in the research of neurological disease.

SKLB0565 is a potent tubulin inhibitor. SKLB0565 shows significant anti-proliferative activity against CRC (colorectal carcinoma) cell lines, with IC₅₀ values ranging from 0.012 μM to 0.081 μM. SKLB0565 causes G2/M phase arrest and mitochondria-mediated intrinsic apoptosis. SKLB0565 inhibits cell migration and disrupted the tube formation of HUVECs.

Topoisomerase I-IN-20 is a Topoisomerase I inhibitor. Topoisomerase I-IN-20 disrupts DNA synthesis and transcription, thereby inhibiting the proliferation and migration of cancer cells. Topoisomerase I-IN-20 induces S-phase cell cycle arrest and mitochondria-mediated Apoptosis in cancer cells, which is characterized by upregulated expression of p53, Bax, caspase-3 and caspase-9, along with downregulated expression of Bcl-2. Topoisomerase I-IN-20 increases intracellular ROS levels. Topoisomerase I-IN-20 is applicable to lung cancer-related research.

NIK-12192 is an orally active inhibitor of vacuolar H⁺-ATPase. NIK-12192 reduces intracellular pH, decreases lysosomal volume and acidity, and alters the intracellular localization of V-ATPase by inhibiting proton pumps. NIK-12192 induces αvβ5 integrin polarization, cytoskeletal disruption, cell detachment, anoikis-mediated delayed apoptosis and necrosis, a delayed reduction in mitochondrial membrane potential, and lysosomal/phagosomal accumulation. NIK-12192 inhibits tumor cell migration, invasion, and three-dimensional spheroid growth, and enhances the activity of Topotecan (HY-13768). NIK-12192 suppresses spontaneous lung metastasis in vivo. NIK-12192 is used in research related to colon cancer, ovarian cancer, lung cancer, breast cancer, renal cancer, prostate cancer, acute myeloid leukemia, and melanoma.

CDK9/CycT1 degrader-1 is an autophagy-anchored bifunctional degrader that mediates the degradation of the CDK9/cyclin T1 protein complex. CDK9/CycT1 degrader-1 binds both CDK9 and LC3B simultaneously to form a ternary complex, achieving target protein degradation via the autophagy-lysosome pathway. CDK9/CycT1 degrader-1 downregulates the protein levels of Mcl‑1 and c‑Myc and induces apoptosis. PROTAC CDK9/CycT1 Degrader-2 is applicable to cancer-related research.

SHP2 inhibitor LY6 (LY6) is a selective SHP2 inhibitor with an IC₅₀ of 9.8 μM, showing 7-fold selectivity over SHP1. SHP2 inhibitor LY6 inhibits SHP2-mediated cell signaling pathways and suppresses cell proliferation. SHP2 inhibitor LY6 elicits induces apoptosis and G2/M cell cycle arrest in lung cancer cells. SHP2 inhibitor LY6 can be used for the research of B cell acute lymphoblastic leukemia, acute myeloid leukemia, and lung cancer.

KF-20444 is an orally active ALK inhibitor with blood-brain barrier penetration. KF-20444 exhibits strong inhibitory activity against ALK fusion proteins (EML4-ALK) and ALK resistance mutations (including L1196M, G1202R, and F1174L). KF-20444 effectively suppresses the phosphorylation of ALK in ALK-driven cancer cell lines, thereby inhibiting cancer cell proliferation and inducing apoptosis. KF-20444 demonstrates anti-tumor efficacy in mouse models bearing ALK-positive non-small cell lung cancer (NSCLC) or neuroblastoma. KF-20444 can be used for the study of ALK-driven malignancies.

Apoptosis inducer 5 (compound 1b) is a lignan enantiomer that can be found in Crataegus pinnatifida. Apoptosis inducer 5 exhibits cytotoxic effect via apoptosis and autophagy in Hep3B cells.

Vernodalin is an orally active, cytotoxic sesquiterpene lactone with a K_d value of 9.55 μM for p38 MAPK. Vernodalin downregulates the expression of phosphorylated ERK, JNK, AKT, PI3K, mTOR, p38MAPK, FAK, MMP-2, MMP-9, and uPA, while upregulates the expression of TIMP-1 and TIMP-2. Vernodalin increases ROS production, upregulates the expression of Bax and caspase 3, downregulates the expression of Bcl-2, and induces apoptosis (apoptosis), oxidative stress response and cell cycle arrest. Vernodalin inhibits the proliferation, adhesion and metastasis of cancer cells. Vernodalin enhances the activity of VEGF-B, AMPK and eNOS signaling pathways. Vernodalin alleviates myocardial injury and restores hemodynamic parameters. Vernodalin inhibits the growth of Trypanosoma brucei rhodesiense. Vernodalin can be used in research related to various cancers including gastric cancer, colorectal cancer and lung cancer, as well as African human trypanosomiasis and myocardial infarction.

Apoptosis inducer 23 (compound 6e) is an apoptosis inducer with antitumor activity. Apoptosis inducer 23 plays an important role in lung cancer research by inducing apoptosis through mitochondrial damage.

HYS-072 is an orally active derivative of chrysin (HY-14589) with antitumor activity. HYS-072 induces apoptosis and autophagy by inhibiting the PI3K/AKT/mTOR signaling pathway and suppresses tumor growth in vivo in xenograft models by modulating autophagy-related pathways. HYS-072 can be used in the research of triple-negative breast cancer.

Cernuumolide J (TMJ-105) is an JAK2/STAT3 inhibitor. Cernuumolide J induces G2/M phase arrest and apoptosis in HEL leukemia cells by downregulating the phosphorylation of JAK2, STAT3, and Erk, and activating the phosphorylation of JNK and p38 MAPK. Cernuumolide J inhibits HEL leukemia cell growth in a time- and concentration-dependent manner, with an IC₅₀ value of 1.79 μM. Cernuumolide J can be used for research in the field of anti-cancer therapy.

Cefatrizine (BL-S-640) is an orally active and broad-spectrum cephalosporin antibiotic. Cefatrizine is also a eEF2K inhibitor, with anti-proliferative activity in human breast cancer cells, which could induce ER stress, leading to cell death. Cefatrizine can be used in studies of cancer and bacterial infection.

AKN-028 TFA, a novel tyrosine kinase (TK) inhibitor, is a potent, orally active FMS-like receptor tyrosine kinase 3 (FLT3) inhibitor with an IC₅₀ value of 6 nM. AKN-028 TFA inhibits FLT3 autophosphorylation. AKN-028 TFA induces dose-dependent cytotoxic response (mean IC₅₀=1 μM). AKN-028 TFA induces apoptosisby activation of caspase 3. AKN-028 TFA can be used in research of acute myeloid leukemia (AML).

PF-3758309 (PF-03758309) dihydrochloride is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (K_d= 2.7 nM; K_i=18.7 nM). PF-3758309 dihydrochloride has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation.