Shepherdin (79-87) is amino acids 79 to 87 fragment of Shepherdin. Shepherdin is a peptidomimetic antagonist of the complex between Hsp90 and Survivin. Anticancer activity[1].
Anti-melanoma agent 1 (Compound 5m) is an anti-melanoma agent and induces cell apoptosis[1].
PI3Kα-IN-9 (compound 27) is a selective, long-acting and oral active PI3Kα inhibitor with IC50 values of 4.4, 128, 146 and 153 nM for PI3Kα, PI3Kγ, PI3Kδ and PI3Kβ, respectively. PI3Kα-IN-9 has antiproliferative activity and induces apoptosis. PI3Kα-IN-9 can be used for cancer research[1].
Necrostatin-5 (Nec-5) is a potent necroptosis inhibitor with an EC50 value of 0.24 µM. Necrostatin-5 also is a RIP1 inhibitor. Necrostatin-5 shows cardioprotective effects[1][2][3].
Pim-1 kinase inhibitor 1 is a Pim-1 kinase inhibitor with an IC50 of 0.11 μM for Pim-1 kinase. Pim-1 kinase inhibitor 1 shows anticancer activity to several cancer cell lines by promotes cell apoptosis. Pim-1 kinase inhibitor 1 can be used for the research of cancer[1].
erythro-Austrobailignan-6 is an orally active anti-cancer agent. erythro-Austrobailignan-6 inhibits DNA topoisomerase I and II activity. erythro-Austrobailignan-6 induces cell apoptosis and increases phosphorylation of p38 and JNK[1][2].
Maduramicin (Maduramycin) is isolated from the actinomycete Actinomadura rubra. Maduramicin is an anticoccidial agent for the the treatment of Eimeria spp., E. adenoeides, E. gallopavonis, and E. dispersa infection[1]. Maduramicin induces cell apoptosis in chicken myocardial cells via intrinsic and extrinsic pathways[2].
Tenovin-6 Hydrochloride is a water soluble inhibitor of SIRT1 and SIRT2, slightly inhibits HDAC8, and is also a potent activator of p53, with IC50s of 21 μM, 10 μM, 67 μM for SirT1, SirT2, and SirT3, respectively.
Topoisomerase II inhibitor 9 (Compound 19b) is a Topo II inhibitor with an IC50 of 0.97 μM. Topoisomerase II inhibitor 9 is also a classical DNA-intercalator with an IC50 of 43.51 μM. Topoisomerase II inhibitor 9 arrests the cell cycle at the G2/M phase and induces apoptosis in Hep G‐2 cells[1].
Momelotinib-2,2,6,6-d4 (CYT387-2,2,6,6-d4) is the deuterium labeled Momelotinib (HY-10961). Momelotinib (CYT387) is an orally acitve and ATP-competitive JAK1/JAK2 inhibitor with IC50s of 11 nM and 18 nM, respectively[1][2].
4-(Dodecylamino)phenol (p-DDAP) is an anticancer agent. 4-(Dodecylamino)phenol has anti-tumor activity and can suppress proliferation, arrest the cell cycle and induce apoptotic cell death. 4-(Dodecylamino)phenol can be used for the research of cancer, such as prostate cancer[1][2].
Pectolinarin, isolated from Cirsium chanroenicum, possesses anti-inflammatory activity[1]. Pectolinarin inhibits secretion of IL-6 and IL-8, as well as the production of PGE2 and NO. Pectolinarin suppresses cell proliferation and inflammatory response and induces apoptosis via inactivation of the PI3K/Akt pathway[2].
Topoisomerase II inhibitor 7 (compound 3a) is a potent inhibitor of topoisomerase II alpha subtype, with an IC50 of 3.19 μM. Topoisomerase II inhibitor 7 can induce cell cycle arrest and apoptosis[1].
Apoptolidin is a polyketide isolated from Nocardiopsis bacteria[1]. Apoptolidin is a selective mitochondrial F1FO ATPase inhibitor. Apoptolidin is an apoptosis inducer and induces apoptotic cell death in cells transformed with the adenovirus type 12 oncogenes including ElA (IC50=10-17 ng/ml) but not in normal cells[1][2].
Isoharringtonine is a natural alkaloid that can be purified from Cephalotaxus koreana Nakai. Isoharringtonine can inhibit cancer cell proliferation and migration, and induce cancer cell apoptosis. Isoharringtonine can be used for the research of cancers[1][2].
Asperosaponin VI, A saponin component from Dipsacus asper wall, induces osteoblast differentiation through BMP‐2/p38 and ERK1/2 pathway[1]. Asperosaponin Ⅵ inhibits apoptosis in hypoxia-induced cardiomyocyte by increasing the Bcl-2/Bax ratio and decreasing active caspase-3 expression, as well as enhancing of p-Akt and p-CREB[2].
RO-5963 is a dual p53-MDM2 and p53-MDMX inhibitor with IC50s of ~17 nM and ~24 nM, respectively[1].
Cerivastatin is a synthetic lipid-lowering agent and a highly potent, well-tolerated and orally active HMG-CoA reductase inhibitor, with a Ki of 1.3 nM/L. Cerivastatin reduces low-density lipoprotein cholesterol levels. Cerivastatin also inhibits proliferation and invasiveness of MDA-MB-231 cells, mainly by RhoA inhibition, and has anti-cancer effect[1][2][3].
Ferroptosis-IN-4 (compound 6k) is a ferroptosis inhibitor with EC50 value of 20 μM. Ferroptosis-IN-4 has no obvious cytotoxicity. Ferroptosis-IN-4 has a protective effect in glycerol-induced RM-AKI mice with alleviating kidney dysfunction[1].
ARD-61 is a highly potent, effective and specific PROTAC androgen receptor (AR) degrader. ARD-61 potently and effectively induces AR and progesterone receptors (PR) degradation in AR+ cancer cell lines. ARD-61 induces apoptosis and effectively induces tumor growth inhibition in the MDA-MB-453 xenograft model in mice[1].
MIK665 (S-64315) is a special Mcl-1 inhibitor[1].
RWJ-56110 is a potent, selective, peptide-mimetic inhibitor of PAR-1 activation and internalization (binding IC50=0.44 uM) and shows no effect on PAR-2, PAR-3, or PAR-4. RWJ-56110 inhibits the aggregation of human platelets induced by both SFLLRN-NH2 (IC50=0.16 μM) and thrombin (IC50=0.34 μM), quite selective relative to U46619 (HY-108566). RWJ-56110 blocks angiogenesis and blocks the formation of new vessel in vivo. RWJ-56110 induces cell apoptosis[1][2].
Zharp2-1 is an oral effective RIPK2 inhibitor, highly associated with inflammatory bowel disease (IBD). Zharp2-1 blocker muramyl dipeptide (MDP) induces growth of mononuclear cells and induces inflammatory cell factor infection. Zharp2-1 attenuates MDP-induced small inguinal peritonitis, or ameliorates by DNBS-induced large inguinal conjunctivitis[1].
Flavokawain B (Flavokavain B) is a chalcone isolated from the root extracts of kava-kava plant and a potent apoptosis inducer for inhibiting the growth of various cancer cell lines. Flavokawain B (Flavokavain B) shows strong antiangiogenic activity. Flavokawain B (Flavokavain B) inhibits human brain endothelial cell (HUVEC) migration and tube formation with very low and non-toxic concentrations[1][2].
Rosiglitazone (BRL 49653) potassium is an orally active selective PPARγ agonist (EC50: 60 nM, Kd: 40 nM). Rosiglitazone potassium is a TRPC5 activator (EC50: 30 μM) and TRPM3 inhibitor. Rosiglitazone potassium can be used in the research of obesity and diabetes, senescence, ovarian cancer[1][2][4][7].
CAM833 (CAM-833) is a potent, specific chemical inhibitor of the RAD51-BRCA2 interaction and RAD51 oligomerization with Kd of 366 nM;CAM833 inhibited RAD51 foci formation 6 h after exposure to 3 Gy IR, in a concentration-dependent manner with an IC50 of 6 uM, causeed a concentration-dependent decrease in RAD51 foci accompanied by increased DNA damage in A549 cells.CAM833 inhibted RAD51 molecular clustering at DNA damage sites visualized by SMLM, suppressed homologous recombination and potentiated cell-cycle arrest.CAM833 potentiated the growth suppressive effect of PARP1 inhibition in BRCA2 wild-type cells, as well as dose-dependent growth inhibition when combined with ionizing radiation.
Momelotinib-d2 (CYT387-d2) is the deuterium labeled Momelotinib (HY-10961). Momelotinib (CYT387) is an orally active and ATP-competitive inhibitor of JAK1/JAK2 with IC50a of 11 nM and 18 nM,respectively, shows much less activity against JAK3[1][2].
GPNA hydrochloride is a well known substrate of the enzyme γ-glutamyltransferase (GGT). GPNA hydrochloride is a specific glutamine (Gln) transporter ASCT2 inhibitor. GPNA hydrochloride also inhibit Na+-dependent carriers, such as SNAT family (SNAT1/2/4/5), and the Na+-independent leucine transporters LAT1/2. GPNA reversibly induces apoptosis in A549 cells[1].
L-Cystine-3,3'-13C2 is the 13C labeled L-Cystine[1]. L-Cystine is an amino acid and intracellular thiol, which plays a critical role in the regulation of cellular processes[2].
α-Lipoic Acid is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. α-Lipoic Acid inhibits NF-κB-dependent HIV-1 LTR activation.