Amsacrine is an inhibitor of topoisomerase II, and acts as an antineoplastic agent which can intercalates into the DNA of tumor cells.
Forodesine(BCX-1777 freebase; Immucillin-H) is an orally bioavailable PNP inhibitor with picomolar potency; induces apoptosis, mainly in T cells.IC50 value:Target: PNP inhibitorForodesine and ara-G cytotoxicities were higher in T-cell acute lymphoblastic leukemia (T-ALL) samples than in B-cell precursor (BCP)-ALL and acute myeloid leukemia (AML) samples. Resistance to forodesine did not preclude ara-G sensitivity and vice versa, indicating that both drugs rely on different resistance mechanisms [1]. BCX1777 was well tolerated at doses up to 300 mg once daily and showed preliminary evidence of activity in relapsed or refractory peripheral T/natural killer-cell malignancies, warranting further investigation [2]. after 48 hours of treatment with forodesine there was a slight dGTP increase in 5T33MM and RPMI-8226 MM cells associated with partial inhibition of proliferation and a limited induction of apoptosis [3]. In the presence of 10 μM deoxyguanosine, forodesine effectively inhibited the growth of CEM cells but not that of CEM/ara-G cells [4].
SMO-IN-1 (Compound 15) is an orally active Smoothened (SMO) inhibitor with an EC50 of 89 nM against sonic Hh protein (shh)[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].
MAX-40279 is a dual and potent inhibitor of FLT3 kinase and FGFR kinase. MAX-40279 has the potential for the research of acute myelogenous leukemia (AML) (extracted from patent WO2021180032)[1].
DS18561882 is a highly potent, isozyme-selective methylenetetrahydrofolate dehydrogenase 2 (MTHFD2) inhibitor with an IC50 value of 0.0063 μM. DS18561882 also has inhibitory effect on MTHFD1 (IC50=0.57 μM). DS18561882 exhibits a good oral pharmacokinetic profile[1].
Marlumotide is an immunological agent for active immunization, as well as an antineoplastic agent[1].
11-Deoxy Prostaglandin E2 is a selective agonist of EP4 with an EC50 of 0.66 nM. 11-Deoxy Prostaglandin E2 is an analog of prostaglandin E2. 11-Deoxy Prostaglandin E2 can be used in study bone healing, heart failure, and other receptor associated conditions[1][2].
Hoechst stains are part of a family of blue fluorescent dyes used to stain DNA.IC50 Value:Target: These Bis-benzimides were originally developed by Hoechst AG, which numbered all their compounds so that the dye Hoechst 33342 is the 33342nd compound made by the company. There are three related Hoechst stains: Hoechst 33258, Hoechst 33342, and Hoechst 34580. The dyes Hoechst 33258 and Hoechst 33342 are the ones most commonly used and they have similarexcitation/emission spectra. Both dyes are excited by ultraviolet light at around 350 nm, and both emit blue/cyan fluorescent light around anemission maximum at 461 nm. Unbound dye has its maximum fluorescence emission in the 510-540 nm range. Hoechst dyes are soluble in water and in organic solvents such as dimethyl formamide or dimethyl sulfoxide. Concentrations can be achieved of up to 10 mg/mL. Aqueous solutions are stable at 2-6 °C for at least six months when protected from light. For long-term storage the solutions are instead frozen at ≤-20 °C.The dyes bind to the minor groove of double-stranded DNA with a preference for sequences rich in adenine andthymine. Although the dyes can bind to all nucleic acids, AT-rich double-stranded DNA strands enhance fluorescence considerably.Hoechst dyes are cell-permeable and can bind to DNA in live or fixed cells. Therefore, these stains are often called supravital, which means that cells survive a treatment with these compounds. Cells that express specific ATP-binding cassette transporter proteins can also actively transport these stains out of their cytoplasm.
TAS1553 is a potent, orally active protein–protein interaction (PPI) inhibitor with an IC50 values of 0.0396 μM. TAS1553 inhibits DNA replication and reduces intracellular dATP pool. TAS1553 induces apoptosis. TAS1553 can be used for cancer research[1].
Tubulin polymerization-IN-10 is a potent tubulin polymerization inhibitor with an IC50 of 4.25±0.75 μM. Tubulin polymerization-IN-10 has anti-tumor effects[1].
ACTB-1003 is an oral kinase inhibitor with IC50s of 6, 2 and 4 nM for FGFR1, VEGFR2 and Tie-2.
WRG-28 is a selective, extracellularly acting DDR2 allosteric inhibitor with an IC50 of 230 nM. WRG-28 uniquely inhibits receptor-ligand interactions via allosteric modulation of the receptor. WRG-28 inhibits tumor invasion and migration, as well as tumor-supporting roles of the stroma, and inhibits metastatic breast tumor cell colonization in the lungs by targeting DDR2[1].
Propargyl-PEG9-amine is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
Boc-NH-C4-Br is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1].
HAT-IN-1 is an inhibitor of HAT, used in the research of cancer.
7-Isocarapanaubine is an indole that can be isolated from Rauwolfi vomitoria[1].
EZH2-IN-15 (SHR2554) is a EZH2 inhibitor. EZH2-IN-15 has anti-tumor activity, and can be used for research of H3K27me3-dependent tumors[1].
1-Naphthohydroxamic acid (Compound 2) is a potent and selective HDAC8 inhibitor with an IC50 of 14 μM. 1-Naphthohydroxamic acid is more selectively for HDAC8 than class I HDAC1 and class II HDAC6 (IC50 >100 μM). 1-Naphthohydroxamic acid does not increase global histone H4 acetylation and also does not reduce total intracellular HDAC activity[1][2].1-Naphthohydroxamic acid can induce tubulin acetylation[3].
Cimetidine (SKF-92334) hydrochloride is an orally active and inverse histamine H2 receptor antagonist with a Ki of 0.6 μM. Cimetidine hydrochloride is a gastric acid reducer, and can be used for duodenal and gastric ulcers research. Cimetidine hydrochloride has anti-cancer and anti-inflammatory activity[1][2][5].
Zorubicin (Rubidazon) is a derivative of Daunorubicin (HY-13062A). Zorubicin interacts with topoisomerase II and inhibits DNA polymerases. Zorubicin can be used for the research of acute leukemias and sarcomas[1][2][3][4][5].
Protoneogracillin, a furostanol glycoside, shows anti-fungal activity against the plant pathogenic fungus P.oryzae (MMDC=94.0 μM) and cytotoxic activity on K562 cancer cells (IC50=6.6 μM)[1][2].
Sulindac (sodium) (MK-231) is an orally active nonsteroidal anti-inflammatory agent. Sulindac (sodium) is used to reduce pain, swelling, and joint stiffness from arthritis. Sulindac is also used for the research of arthritis of the spine, gouty arthritis. Sulindac (sodium), as an immunomodulatory agent, can downregulate PD-L1 through the blockade of NF-κB signaling and modulates the response of pMMR colorectal cancer (CRC) to anti-PD-L1 immunotherapy, inhibits the development and progression of colorectal cancer CRC. Sulindac (sodium) also inhibits TGF-β1- induced epithelial-mesenchymal transition (EMT) and suppresses lung cancer cell migration and invasion via downregulation of SIRT1[1][2].
Necrostatin 2 is a potent necroptosis inhibitor with EC50 of 50 nM.IC50 Value: 50 nM (EC50) [1]Target: TNF-alphaNecrostatin 2 is a potent in vitro necroptosis inhibitors (exemplified by 1, EC50-0.05 uM) that also were efficacious in an animal model of ischemic stroke. Many Necroptosis inhibitor derivatives are designed for researchers.Necroptosis is a regulated caspase-independent cell death mechanism that results in morphological features resembling necrosis. It can be induced in a FADD-deficient variant of human Jurkat T cells treated with TNF-a. 5-(1H-Indol-3-ylmethyl)-2-thiohydantoins and 5-(1H-indol-3-ylmethyl)hydantoins were found to be potent necroptosis inhibitors (called necrostatins).
Isovitexin 2′′-O-rhamnoside, a phenolic, has antioxidant and antiproliferative activities[1].
19-Hydroxy-10-deacetylbaccatin III (compound 13) is a taxane with potential antitumor activity. 19-Hydroxy-10-deacetylbaccatin III has weak cytotoxicity against A498 and NCI-H226 cell lines. The study found that the inhibition rates of 30 μg/mL 19-Hydroxy-10-deacetylbaccatin III on A498, NCI-H226 and PC-3 were 16.6% and 32% respectively[1].
(Z)-p-cyano-α-Cyanostilbene (compound 11), a phenantrene derivative, has antiproliferative activity. (Z)-p-cyano-α-Cyanostilbene shows significant selectivity against HeLa (IC50=0.21 µM) and HepG2 (IC50=0.230 µM) cells without cytotoxic against normal skin fibroblasts (IC50>100 µM)[1].
Sarsasapogenin is a sapogenin from the Chinese medical herb Anemarrhena asphodeloides Bunge, with antidiabetic, anti-oxidative, anticancer and anti-inflamatory activities.
4'-O-Methylnyasol is an inhibitor of β-hexosaminidase. 4'-O-Methylnyasol inhibits β-hexosaminidase release from rat basophilic leukemia-2H3 cells with an IC50 of 52.67 μM[1].
Schineolignin C is a Lignan that can be isolated from the fruit of schisandra chinensis. schisandra chinensis has antihepatitis, antitumor, and anti-HIV-1 activities[1].