NVP-CGM097 is a potent and selective MDM2 inhibitor with IC50 of 1.7±0.1 nM for hMDM2.
Isatuximab is a monoclonal antibody targeting the transmembrane receptor and ectoenzyme CD38, a protein highly expressed on hematological malignant cells, including those in multiple myeloma (MM). Isatuximab has antitumor activity via multiple biological mechanisms, including antibody-dependent cellular-mediated cytotoxicity, complement-dependent cytotoxicity, antibody-dependent cellular phagocytosis, and direct induction of apoptosis without crosslinking. Isatuximab also directly inhibits CD38 ectoenzyme activity, which is implicated in many cellular functions[1][2].
ζ-Stat trisodium (NSC37044 trisodium) is a specific and atypical PKC-ζ inhibitor, with an IC50 of 5 μM. ζ-Stat trisodium can reduce melanoma cell lines proliferation and induce apoptosis, and has antitumor activity in vitro[1][2].
Mcl1-IN-8 (Comp8) is a Mcl-1-PUMA interface inhibitor, with a Ki of 0.3 μM. Mcl1-IN-8 (Comp8) exhibits dual activity on reduce PUMA-dependent apoptosis while deactivating Mcl-1-mediated anti-apoptosis in cancer cells[1].
Sirt1/2-IN-3 (compound PS9) is a dual inhibitor of SIRT1/2 with IC50s of 1.4 μM (SIRT1) and 2.0 μM (SIRT2), respsectivley. Sirt1/2-IN-3 completely blocks p53 deacetylation, and increase of p53 and α-tubulin acetylation. Sirt1/2-IN-3 induces apoptosis and shows anti-proliferation activity against human leukemia cell lines[1].
Dutasteride-13C6 is the 13C labeled Dutasteride[1]. Dutasteride (GG745) is a potent inhibitor of both 5α-reductase isozymes. Dutasteride may possess off-target effects on the androgen receptor (AR) due to its structural similarity to DHT[2].
ASTX660 is an orally bioavailable dual antagonist of cellular inhibitor of apoptosis protein (cIAP) and X-linked inhibitor of apoptosis protein (XIAP).
Sirt1/2-IN-2 (compound hsa55) is a dual inhibitor of SIRT1/2 with IC50s of 1.8 μM (SIRT1) and 2.4 μM (SIRT2), respsectivley. Sirt1/2-IN-2 completely blocks p53 deacetylation, and increase of p53 and α-tubulin acetylation. Sirt1/2-IN-2 induces apoptosis and shows anti-proliferation activity against human leukemia cell lines[1].
PROTAC RIPK degrader-6 (example 1) is a PROTAC targeting RIP Kinase degradation wherein the RIP2 kinase inhibitor is linked via a linker to a cereblon binder[1].
Fidaxomicin-D7 (OPT-80-D7) is the deuterium labeled Fidaxomicin. Fidaxomicin (OPT-80), a macrocyclic RNA polymerase inhibitor, has a narrow spectrum of activity. Fidaxomicin selectively eradicates pathogenic Clostridium difficile with minimal disruption to the multiple species of bacteria that make up the normal, healthy intestinal flora[1][2].
Dimethyl malonate is a competitive inhibitor of succinate dehydrogenase (SDH). Dimethyl malonate is able to cross the blood-brain barrier and hydrolyse to malonate. Dimethyl malonate reduces neuronal apoptosis[1].
Medicarpin is a flavonoid isolated from Medicago sativa. Medicarpin induces apoptosis and overcome multidrug resistance in leukemia P388 cells by modulating P-gp-mediated efflux of drugs[1].
Gemcitabine monophosphate (Gemcitabine 5′-phosphate) is one of the active intermediates of Gemcitabine (HY-17026). Gemcitabine monophosphate shows synergistic anti-cancer effects[1][2].
Dacarbazine citrate is a cell cycle nonspecific antineoplastic alkylating agent. Dacarbazine citrate inhibits T and B lymphoblastic response, with IC50 values of 50 and 10 μg/mL, respectively. Dacarbazine Citrate can be used for the research of apoptosis and various cancers such as metastatic malignant melanoma[1][2].
Tubulin polymerization-IN-41 is a potent tubulin polymerization inhibitor with the IC50 of 2.61 μM. Tubulin polymerization-IN-41 targets the Colchicine-binding site of tubulin. Tubulin polymerization-IN-41 has anticancer effects[1].
Tubulysin G is a highly cytotoxic peptide isolated from the myxobacterial species Archangium geophyra and Angiococcus disciformis. Tubulysin displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the lower nanomolar range[1]. Tubulysin G is a cytotoxic activity tubulysin which inhibits tubulin polymerization and leads to cell cycle arrest and apoptosis[2].
Glaucocalyxin A, an ent-kauranoid diterpene from Rabdosia japonica var., induces apoptosis in osteosarcoma by inhibiting nuclear translocation of Five-zinc finger Glis 1 (GLI1) via regulating PI3K/Akt signaling pathway. Glaucocalyxin A has antitumor effect[1].
Adenosine-d2 is the deuterium labeled Adenosine. Adenosine (Adenine riboside), a ubiquitous endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular physio
CCT241161 is an orally active pan-RAF inhibitor with IC50s of 3, 6, 10, 15 and 30 nM for LCK, CRAF, SRC, V600E-BRAF and BRAF, respectively. CCT241161 shows good activity to in BRAF and NRAS mutant melanomas. CCT241161 also exhibits anticancer cell proliferative activity[1].
Phenformin (1-phenethylbiguanide) is an orally active antidiabetic and anticancer agent. Phenformin has an incidence of associated lactic acidosis. Phenformin acts through acting AMPK activation and blocking mTOR pathway. Phenformin is also a substrate of P-glycoprotein (P-gp), and an OXPHOS inhibitor. Phenformin induces cancer cell apoptosis[1][2].
MBM-17 (compound 42c) is a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 3 nM. It effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-55 shows antitumor activities, and no obvious toxicity to mice[1].
Hirsutine, an indole alkaloid of Uncaria rhynchophylla, exhibits anti-cancer activity. Hirsutine induces apoptosis and is a potent Dengue virus inhibitor exhibiting low cytotoxicity[1][2][3].
Erastin2 is a ferroptosis inducer and a potent, selective inhibitor of the system xc(-) cystine/glutamate transporter[1][2].
Rohinitib is a potent and specific inhibitor of eIF4A1, inhibits growth and survival of AML cells especially cells with FLT3-ITD.
Angiogenesis inhibitor 3 (compound 8) is a potent angiogenesis inhibitor. Angiogenesis inhibitor 3 inhibits the proliferation of HUVEC and HCT-15 cells, with IC50 values of 1.00 and 0.71 μM. Angiogenesis inhibitor 3 induces the apoptosis of HUVEC and HCT-15 cells. Angiogenesis inhibitor 3 shows anticancer activity, and suppresses the invasion of cancer cells. Angiogenesis inhibitor 3 inhibits the angiogenesis in zebrafish embryos[1].
5-Fluorouracil-13C,15N2 is the 13C and 15N labeled 5-Fluorouracil[1]. 5-Fluorouracil (5-FU) is an analogue of uracil and a potent antitumor agent. 5-Fluorouracil affects pyrimidine synthesis by inhibiting thymidylate synthetase thus depleting intracellular dTTP pools. 5-Fluorouracil induces apoptosis and can be used as a chemical sensitizer[2][3]. 5-Fluorouracil also inhibits HIV[4].
Zeylenone, isolated from ethanol extract of the leaves of Uvaria grandiflora Roxb. Zeylenone, a naturally occurring cyclohexene oxide, inhibits proliferation and induces apoptosis in cervical carcinoma cells via PI3K/AKT/mTOR and MAPK/ERK pathways[1].
UCM-1336 is a potent ICMT inhibitor, with an IC50 of 2 μM. UCM-1336 induces mislocalization of endogenous Ras, decreases Ras activation and induces cell death by autophagy and apoptosis[1].
Brazilein is an important immunosuppressive component isolated from Caesalpinia sappan L. Brazilein induces apoptosis in mice spleen lymphocytes[1].
SM-433, a Smac mimetic, function as inhibitor of inhibitor of apoptosis proteins (IAPs). SM-433 exhibits strong binding affinity XIAP BIR3 protein with an IC50<1 μM. (patent WO2008128171A2)[1].