BRD4 Inhibitor-15 (compound 13) is a potent BRD4 inhibitor, with an IC50 of 18 nM. BRD4 Inhibitor-15 induces apoptosis of 22RV1 cells by regulating Bcl-2/Bax proteins and activating caspase-3 signaling pathway. BRD4 Inhibitor-15 down-regulates the c-Myc level in 22RV1 cells. BRD4 Inhibitor-15 can be used for prostate cancer research[1].
Degarelix acetate hydrate is a competitive and reversible gonadotropin-releasing hormone receptor (GnRHR/LHRHR) antagonist. Degarelix acetate hydrate can be used for prostate cancer research[1].
3-O-Methylgallic acid (3,4-Dihydroxy-5-methoxybenzoic acid) is an anthocyanin metabolite and has potent antioxidant capacity. 3-O-methylgallic acid inhibits Caco-2 cell proliferation with an IC50 value of 24.1 μM. 3-O-methylgallic acid also induces cell apoptosis and has anti-cancer effects[1][2].
JDB175 is a highly selective BTK inhibitor with oral activity and excellent blood-brain barrier penetration. JDB175 shows good activity in the mouse model of central nervous system lymphoma without obvious signs of toxicity, effectively inhibits the proliferation of BTK signaling pathway of human lymphoma cells, induces cell cycle arrest, and promotes cell apoptosis [1].
alpha-Mangostin-d3 (α-Mangostin-d3) is the deuterium labeled alpha-Mangostin. alpha-Mangostin (α-Mangostin) is a dietary xanthone with broad biological activities, such as antioxidant, anti-allergic, antiviral, antibacterial, anti-inflammatory and anticancer effects. It is an inhibitor of mutant IDH1 (IDH1-R132H) with a Ki of 2.85 μM[1][2][3].
(R)-MIK665 is the less active enantiomer of MIK665. MIK665 is a special Mcl-1 inhibitor with an IC50 of 1.81 nM.
Ciwujianoside B is isolated from Eleutherococcus senticosus leaf, is able to penetrate and work in the brain after the oral administration. Ciwujianoside B significantly enhances object recognition memory[1].Ciwujianoside B shows radioprotective effects on the hematopoietic system in mice, which is associated with changes in the cell cycle, reduces DNA damage and down-regulates the ratio of Bax/Bcl-2 in bone marrow cells exposed to radiation[2].
(R)-OY-101 is an orally active and specific inhibitor of P-gp. (R)-OY-101 increases tumor sensitivity to anticancer agents. (R)-OY-101 has good activity in reversing tumor resistance and promoting apoptosis and can be used in cancer related research[1].
β-Ionone, isolated from plant oils, is effective in the induction of apoptosis in gastric adenocarcinoma SGC7901 cells. Anti-cancer activity[1].
P53R3 is a novel p53 reactivator that restores sequence-specific DNA binding of the endogenously expressed p53(R175H) and p53(R273H) mutants in gel-shift assays; induces p53-dependent antiproliferative effects with much higher specificity and over a wider range of concentrations than PRIMA-1; strongly enhances the mRNA, total protein and cell surface expression of DR5.
EPI-001 is a selective inhibitor of Androgen Receptor (AR), and it can inhibit transactivation of the AR amino-terminal domain (NTD), with an IC50 of 6 μM. EPI-001 is also a selective modulator of PPARγ. EPI-001 exhibits anti-tumor activity in vitro and in vivo[1][2].
Physalin F is a secosteroid with potent anti-inflammatory and immunomodulatory activities. Physalin F induces apoptosis of PBMC, decreasing the spontaneous proliferation and cytokine production caused by Human T-lymphotropic virus type 1 (HTLV-1) infection[1].
Metronidazole-d3 is deuterium labeled Metronidazole.
Imipramine is an orally active tertiary amine tricyclic antidepressant. Imipramine is a Fascin1 inhibitor with antitumor activities. Imipramine stimulates U-87MG glioma cells autophagy and induces HL-60 cell apoptosis. Imipramine shows neuroprotective and immunomodulatory effects[1][2][3][4].
Bid BH3 (80-99) is a biological active peptide. (BID is a pro-apoptotic member of the 'BH3-only' (BOPS) subset of the BCL-2 family of proteins that constitute a critical control point in apoptosis. Bid is the first of the BOPs reported to bind and activate Bcl-2, Bax, and Bak. Bid serves as a death-inducing ligand that moves from the cytosol to the mitochondrial membrane to inactivate Bcl-2 or to activate Bax.Pyroglutamyl (pGlu) peptides may spontaneously form when either Glutamine (Q) or Glutamic acid (E) is located at the sequence N-terminus. The conversion of Q or E to pGlu is a natural occurrence and in general it is believed that the hydrophobic γ-lactam ring of pGlu may play a role in peptide stability against gastrointestinal proteases. Pyroglutamyl peptides are therefore considered a normal subset of such peptides and are included as part of the peptide purity during HPLC analysis.)
Nimustine is a nitrosourea alkylating agent. Nimustine induces cell apoptosis, and activates DNA damage response and MAPK signaling. Nimustine shows anti-cancer effects, it can be used for the research of cancer[1][2].
PI3K/Akt/mTOR-IN-3 (compound 3d) is a potent PI3K/AKT/mTOR inhibitor. PI3K/Akt/mTOR-IN-3 displays the inhibitory activity in MCF-7, HeLa and HepG2 cells, with IC50 values of 0.77, 1.23, and 4.57μM, respectively. PI3K/Akt/mTOR-IN-3 inhibits the migration of MCF-7 and HeLa cells at the concentration of 4 μM. PI3K/Akt/mTOR-IN-3 induces cell apoptosis and S phase arrest[1].
Hematoporphyrin monomethyl ether, second generation of porphyrin-related photosensitizer, is characterized by its single form, high yield of singlet oxygen, high selectivity, and low toxicity, which has been widely used in the diagnosis and treatment of various tumors, including lung cancer, bladder cancer, and nevus flammeus and brain glioma[1].
SS28, a SRT501 analog with oral bioavailability, inhibits tubulin polymerization to cause cell cycle arrest at G2/M phase. SS28 results in apoptosis rather than necrosis tubulin[1].
PETCM is an activator of caspase-3. PETCM can induces cell apoptosis and stimulate apoptosome formation in HeLa cell cytosols[1].
Lidocaine, an amide local anesthetic, has anti-inflammatory properties in vitro and in vivo, possibly due to an attenuation of pro-inflammatory cytokines, intracellular adhesion molecule-1 (ICAM-1), and reduction of neutrophils influx.Target: Lidocaine is a common local anesthetic and antiarrhythmic drug. Lidocaine is used topically to relieve itching, burning and pain from skin inflammations, injected as a dental anesthetic or as a local anesthetic for minor surgery. Lidocaine, the first amino amide–type local anesthetic, was first synthesized under the name xylocaine by Swedish chemist Nils Lofgren in 1943. His colleague Bengt Lundqvist performed the first injection anesthesia experiments on himself.Lidocaine is approximately 95% metabolized (dealkylated) in the liver by CYP3A4 to the pharmacologically-active metabolites monoethylglycinexylidide (MEGX) and then subsequently to the inactive glycine xylidide. MEGX has a longer half life than lidocaine but also is a less potent sodium channel blocker. The elimination half-life of lidocaine is approximately 90–120 minutes in most patients. This may be prolonged in patients with hepatic impairment (average 343 minutes) or congestive heart failure (average 136 minutes).
BCL6-IN-9 (compound 1) is a potent B-cell lymphoma 6 protein (BCL6) inhibitor, with an IC50 of 3.9 nM. BCL6-IN-9 can be used for the research of cancer[1].
HKPao (Hunter-killer peptide ao) is a biologically active peptide. HKPao (Hunter-killer peptide ao) has anti-obesity and anti-tumor pro-apoptotic activity to cause release of cytochrome c from vesicles[1].
Pioglitazone D4 (U 72107 D4) is a deuterium labeled Pioglitazone. Pioglitazone (U 72107) is a potent and selective PPARγ agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 and 0.99 μM for human and mouse PPARγ, respectively[1].
Levomenol is a monocyclic sesquiterpene alcohol found in various plants and mainly in Matricaria chamomilla, which exerts antioxidant, anti-inflammatory, and anti-apoptotic activities. Levomenol has neuroprotective effects, can attenuate nociceptive behaviour and central sensitisation in a rodent model of trigeminal neuropathic pain[1][2].
STAT3-IN-13 (compound 6f) is a potent STAT3 inhibitor. STAT3-IN-13 has anti-proliferative effects and binds to the STAT3 SH2 domain with a KD of 0.46 μM. STAT3-IN-13 inhibits the phosphorylation of STAT3 Y705 and downstream target gene expression. STAT3-IN-13 induces apoptosis in vitro and suppresses the growth and metastasis of tumor in vivo. STAT3-IN-13 can be used for cancer research[1].
SCH529074 is a potent and orally active p53 activator. SCH529074 binds specifically and conformation-dependently to p53 DBD ( DNA binding domain) with a Ki of 1-2 μM in a saturable manner. SCH529074 restores mutant p53 function and interrupts HDM2-mediated ubiquitination of wild Type p53. SCH529074 can be used for the study of non-small-cell lung carcinoma (NSCLC)[1][2].
Sclareol is isolated from Salvia sclarea with anticarcinogenic activity. Sclareol shows strong cytotoxic activity against mouse leukemia (P-388), human epidermal carcinoma (KB) cells and human leukemia cell lines. Sclareol induces cell apoptosis[1].
HIOC is a potent and selective activator of TrkB (tropomyosin related kinase B) receptor. HIOC can pass the blood-brain and blood-retinal barriers.HIOC activates TrkB/ERK pathway and decreases neuronal cell apoptosis. HIOC attenuates early brain injury after SAH (subarachnoid hemorrhage). HIOC shows protective activity in an animal model for light-induced retinal degeneration[1][2][3].
HLI373 dihydrochloride is an efficacious Hdm2 inhibitor. HLI373 dihydrochloride inhibits the ubiquitin ligase activity of Hdm2. HLI373 dihydrochloride is effective in inducing apoptosis of several tumor cells that are sensitive to DNA-damaging agents[1]. Antimalarial activity[2].