MI-773 is a new small molecule inhibitor of the MDM2-p53 interaction, binds to MDM2 with high affinity (Ki=0.88 nM) and blocks the p53-MDM2 interaction.
Bz 423 is a pro-apoptotic 1,4-benzodiazepine with therapeutic properties in murine models of lupus demonstrating selectivity for autoreactive lymphocytes, and activates Bax and Bak.
WEHI-539 is a selective inhibitor of Bcl-XL with IC50 of 1.1 nM.
Astin B is a orally active and potent cyclic pentapeptide, that can be isolated from Aster tataricus. Astin B has hepatotoxic effects in vitro and in vivo and that hepatic injury was primarily mediated by apoptosis in a mitochondria/caspase-dependent manner. Astin B induces autophagy in L-02 cells, increases LC3-II and decreases p62 expression[1].
Neocarzinostatin, a potent DNA-damaging, anti-tumor antibiotic, recognizes double-stranded DNA bulge and induces DNA double strand breaks (DSBs). Neocarzinostatin induces apoptosis. Neocarzinostatin has potential for EpCAM-positive cancers treatment [1][2].
Butylated hydroxytoluene-d24 is the deuterium labeled Butylated hydroxytoluene[1]. Butylated hydroxytoluene is an antioxidant widely used in foods and in food-related products[2]. Butylated hydroxytoluene is a Ferroptosis inhibitor[3].
Prion Protein 106-126 (human) is a peptide fragment of prion, it can induct neuronal apoptosis, antiproteinase K digestion, fiber formation, and mediate the conversion of normal cellular prion protein (PrPc) into pathogenic isoform (PrPSc). Prion Protein 106-126 (human) is generally used as the model to investigate neural degeneration of prion disease[1][2].
Patritumab (Human Anti-ERBB3 Recombinant Antibody) is a neutralizing monoclonal antibody to ERBB3. Patritumab shows a synergy with Cetuximab (HY-P9905), potently inhibits the phosphorylation of EGFR, HER2, HER3, ERK, and Akt. Patritumab also induces cell apoptosis and suppresses the growth of pancreatic, non-small cell lung cancer, and colorectal cancer xenograft tumors[1].
Griseofulvin-13C,d3 is the 13C- and deuterium labeled.
6,8-Diprenylorobol, a prenylated isoflavone, is a nature product that could be isolated from the leaves of Cudrania tricuspidata. 6,8-Diprenylorobol antiproliferative effect and induces apoptosis through activation of p53 and generation of ROS[1][2].
T-1101 tosylate (TAI-95 tosylate) is a Hec1/Nek2 (Highly expressed in cancer 1 / NIMA-related kinase 2) inhibitor with antitumor activity. T-1101 tosylate is inactive toward normal cells, kinases and hERG[1]
Bax inhibitor peptide, negative control is a inhibitor of Bax. Bax inhibitor peptide, negative control inhibits Bax translocation to mitochondria and Bax-mediated apoptosis in vitro[1].
Afatinib (BIBW 2992) oxalate is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively. Afatinib oxalate can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer[1][2][3][4].
Humanin, an anti-apoptotic peptide of 24 amino acids, is a Bax inhibitor. Humanin prevents the translocation of Bax from cytosol to mitochondria, blocks Bax from the inactive to active conformation. Humanin is a mitochondria-associated peptide with a neuroprotective effect against AD-related neurotoxicity. Humanin also improves overall insulin sensitivity in animal. Humanin are related to aging[1][2]. Humanin analogue, in which the serine at position 14 is replaced by glycine, names HNG[2].
Ginsenoside Rh1 is isolated from the root of Panax Ginseng. Ginsenoside Rh1 inhibits the expression of PPAR-γ, TNF-α, IL-6, and IL-1β.
MC2590 is a potent pyridine-containing histone deacetylase (HDAC) inhibitor. MC2590 is a inhibitor of HDAC1-3, −6, −8, and −10 (class I/IIb-selective inhibitor) with ic50 of 0.098 μM, 0.156 μM, 0.039 μM, 0.015 μM, 0.047 μM, 0.071 μM, respectively. MC2590 also inhibits HDAC isoforms HDAC4 (IC50=2.73 μM), HDAC5 (IC50=1.35 μM), HDAC7 (IC50=2.06 μM), HDAC9 (IC50=2.79 μM), HDAC11 (IC50=3.98 μM). MC2625 induces G2/M cell cycle arrest and modulates pro- and anti-apoptotic microRNAs towards apoptosis induction[1].
Didocosahexaenoin, an omega-3 derivative, is a diglyceride of DHA and can be synthesised from DHA triglycerides. Didocosahexaenoin causes significant loss of mitochondrial membrane potential and induces ROS production. Didocosahexaenoin induces stronger cytotoxicity than DHA in human prostate carcinoma cells[1].
CUR61414 is a novel, potent and cell permeable Hedgehog signaling pathway inhibitor (IC50 =100-200 nM). CUR61414 is a small-molecule aminoproline class compound and selectively binds to smoothened (Smo) with a Ki value of 44 nM. CUR-61414 can induce apoptosis in cancer cells without affecting neighboring non-tumor cells[1][2].
Neoechinulin A is an isoprenyl indole alkaloid that exhibits scavenging, neurotrophic factor-like, and anti-apoptotic activities. Neoechinulin A induces memory improvements and antidepressant-like effects in mice[1][2].
Chrysotoxine is a dual inhibitor of Src/Akt. Chrysotoxine suppresses cancer stem cells (CSCs) phenotypes by down-regulating Src/Akt signaling. Chrysotoxine reduces cell viability and increases apoptosis level in H460 and H23 cells instead of non-tumor cell lines. Chrysotoxine shows rapid excretion and low bioavailability in rats. Chrysotoxine is used in cancer research[1][2].
Heptelidic acid (Koningic acid) is a sesquiterpene antibiotic[1]. Heptelidic acid inhibits Etoposide-induced apoptosis via downregulation of caspases[2]. Koningic acid (KA) is a specific GAPDH inhibitor with an IC50of 90 μM[3].
Meisoindigo(Natura-α; N-Methylisoindigotin; Dian III), a derivative of Indigo naturalis, might induce apoptosis and myeloid differentiation of acute myeloid leukemia (AML).IC50 value:Target: apoptosis inducerin vitro: Meisoindigo inhibited the growth of leukemic cells by inducing marked apoptosis and moderate cell-cycle arrest at the G(0)/G(1) phase. It down-regulated anti-apoptotic Bcl-2, and up-regulated pro-apoptotic Bak and Bax and cell-cycle related proteins, p21and p27. Furthermore, it induced myeloid differentiation, as demonstrated by morphologic changes, up-regulation of CD11b, and increased nitroblue tetrazolium reduction activity in all cell lines tested. In addition, meisoindigo down-regulated the expression of human telomerase reverse transcriptase and enhanced the cytotoxicity of conventional chemotherapeutic agents, cytarabine and idarubicin. As with the results from cell lines, meisoindigo also induced apoptosis, up-regulated p21 and p27, and down-regulated Bcl-2 in primary AML cells [1]. meisoindigo effectively inhibits HT-29 cell proliferation (IC(50) 4.3 mmol/L), arrests HT-29 cells in G2/ M phase and induces HT-29 cell apoptosis. The downstream genes and proteins of GSK-3beta(ser(9)) expression level decrease [2].in vivo: The in vivo anti-leukemic activity of meisoindigo was also demonstrated by decreased spleen size in a dose-dependent manner [1]. Meisoindigo significantly inhibits the HT-29 xenograft tumors growth at the dose of 100 mg/kg. The mechanism of meisoindigo activity against HT-29 cells may be related to its inhibition of glycogen synthase kinase-3beta, GSK-3beta(ser(9)) phosphorylation in Wnt signaling pathway [2].
(rel)-Oxaliplatin is a DNA synthesis inhibitor. (rel)-Oxaliplatin causes DNA crosslinking damage, prevents DNA replication and transcription and induces apoptosis. (rel)-Oxaliplatin can be used for cancer research[1][2][3].
CX-5011 is a CK2 inhibitor. CX-5011 also induces Rac1 activation. CX-5011 induces apoptosis and induces cancer cell death[1][2].
OT-82 is a potent, selective and orally active inhibitor of NAMPT. OT-82 is selectively toxic to cells of hematopoietic origin and induces cell death in a NAD+ dependent manner. OT-82 is a promising antineoplastic agent for the study of hematological malignancies[1].
DL-alpha-Tocopherol-d9 is the deuterium labeled DL-alpha-Tocopherol[1]. DL-alpha-Tocopherol is a synthetic vitamin E, with antioxidation effect. DL-alpha-Tocopherol protects human skin fibroblasts against the cytotoxic effect of UVB[2].
ROS-generating agent 1 (Compound 2c) covalently modifies the Sec-498 residue of TrxR to generate ROS. ROS-generating agent 1 reduces intracellular TrxR protein level. ROS-generating agent 1 results in ROS-dependent apoptosis and ferroptosis of NCI-H460 cells. ROS-generating agent 1 has anti-cancer activities[1].
EP12 is a c-Myc inhibitor. EP12 is a c-Myc G4 stabilizer. EP12 induces apoptosis and DNA damage in multiple myeloma cells. EP12 disrupts the nuclear translocation of P65/P50 by interfering with the NF-κB signaling pathway. EP12 inhibits multiple myeloma growth[1].
E64FC26 is a highly potent pan-style inhibitor of Protein Disulfide Isomerase (PDI) with IC50 of 1.9 uM (PDIA1), also inhibits all other members of the PDI family, including PDIA3, PDIA4, TXNDC5, and PDIA6; induces robust ER stress response in MM cells, with expression of ER stress markers ATF4 and CHOP; induces an oxidative stress response in a panel of heterogeneous PI sensitive and resistant cell lines that was characterized by the induction of Nrf2, synergistically enhances the anti-MM cytotoxic effects of PIs; improves survival and enhanced the activity of bortezomib without any adverse effects.
Nitidine chloride, a potential anti-malarial lead compound derived from Zanthoxylum nitidum (Roxb) DC, exerts potent anticancer activity through diverse pathways, including inducing apoptosis, inhibiting STAT3 signaling cascade, DNA topoisomerase 1 and 2A, ERK and c-Src/FAK associated signaling pathway. Nitidine chloride inhibits LPS-induced inflammatory cytokines production via MAPK and NF-kB pathway[1][2][3][4][5][6].