Bleomycin B4 (Phleomycin F) is an Antibiotic. Bleomycin B4 has antitumor activity. Bleomycin B4 can be used for the research of cancer[1][2][3].
SU056 is a YB-1 inhibitor. SU056 induces cell-cycle arrest, apoptosis, and inhibits cell migration in ovarian cancer cells. SU056 interacts with YB-1 and inhibits and its associated downstream proteins and pathways. SU056 can enhance the cytotoxic effects of Paclitaxel (HY-B0015)[1].
DT-2 is a potent and selective inhibitor of the cGMP-dependent protein kinase (PKG). DT-2 inhibits PKG catalyzed phosphorylation (Ki: 12.5 nM)[1].
1,4-Anhydro-2,3-di-O-isopropylidene-4-thio-D-ribitol is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
5-Azidomethyl-2’,3’,5’-tri-O-benzoyl uridine is a thymidine analog. Analogs of this series have insertional activity towards replicated DNA. They can be used to label cells and track DNA synthesis[1].
FLT3-IN-1 Succinate is a potent FLT3 inhibitor extracted from patent WO2015056683A1, compound example A.
3-tert-Butyl-4-methoxyphenol is a PROTAC linker, belongs to alkyl/ether class, with insecticidal activity. 3-tert-Butyl-4-methoxyphenol also induced increased activities of glutathione (GSH) S-transferase and epoxide hydrolase in the liver and forestomach tissues of A/HeJ mice, regulating the carcinogen metabolism system[1][2].
α-Cembrenediol is a potent inhibitor of EBV.α-Cembrenediol inhibits the early antigen of the Epstein-Bar virus. α-Cembrenediol also has anti-tumour activity[1].
MTP is a PKM2 inhibitor. MTP induces cancer cell apoptosis by modulating caspase-3 activation. MTP induces autophagy and increases ROS generation. MTP also inhibits JAK2 signaling. MTP can be used for research of oral squamous cell carcinoma[1].
Ezutromid is a novel Small utrophin's translation modulator with EC50 of 0.4 uM .In vitro: 1) SMT C1100 induces increased levels of utrophin RNA in human muscle cells.2) Treatment of human DMD cells with SMT C1100 lead to a 2-fold increase in utrophin protein levels at an optimal concentration of 0.3 uM after 3 days of treatment. 3) SMT C1100 wassafe and well tolerated with plasma concentrations achieved suf?cient to cause a 50% increase in concentrations of utrophin in cells. 4) SMT C1100 led to a 30% increase in Utrn mRNA level and resulted in a 2.0-fold increase in UTRN protein level .In vivo: 1)The reference for administration is 50 mg/kg. 2) it was considered that no toxicity was determined for SMT C1100 administered by oral gavage to the mouse up to dose levels of 2000 mg/kg/day for 28 days.Note: You can dissolve the products in phosphate buffered saline (PBS), 0.1% Tween-20, 5% DMSO)
Piperlactam S is an active compound. Piperlactam S can be isolated from Piper kadsura. Piperlactam S can be used for the research of chronic inflammation[1].
Fmoc-Gly-Gly-Phe-Gly-CH2-O-CH2-Cbz is a PROTAC linker and a maleimide-GGFG peptide linker. Fmoc-Gly-Gly-Phe-Gly-CH2-O-CH2-Cbz can be used in the synthesis of the Deruxtecan[1].
MG-115 is a potent and reversible proteasome inhibitor, with Kis of 21 nM and 35 nM for 20S and 26S proteasome, respectively. MG-115 specifically inhibit the chymotrypsin-like activity of the proteasome, induces p53-dependent apoptosis[1][2][3].
2,4-PDCA (2,4 pyridine dicarboxylic acid) is a broad-spectrum inhibitor of 2OG oxygenase, including JmjC domain-containing family of histone demethylases (JHDMs). 2,4-PDCA is a target chemical in the field of bio-based plastics[1][2][3].
Apoptotic agent-1 (Compound 8a) is an apoptotic agent with high antiproliferative activity against cancer cells and low cytotoxic effect. Apoptotic agent-1 induces over-expression of Fas receptor and Cyto C genes[1].
N6-Furfuryl-2’-C-methyladenosine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
Echinomycin (Quinomycin A) is potent small-molecule and cell-permeable inhibitor of hypoxia-inducible factor-1 (HIF-1) DNA-binding activity. Echinomycin selectively inhibits the cancer stem cells (CSCs) with an IC50 of 29.4 pM[1][2].
Skimmianine is a furoquinoline alkaloid present mainly in the Rutaceae family, with analgesic, antispastic, anti-inflammatory activities and antiplatelet aggregation effect. Skimmianine exhibits cytotoxicity against a variety of cancer cell lines and genotoxicity[1].
Fluorescein (Uranine) sodium is widely used as a fluorescent tracer in medicinal and biological applications and tumor infected tissues tracer. Fluorescein (Uranine) sodium is a representative green fluorophore that has been widely used as a scaffold of practically useful green fluorescent probes[1][2].
2-Amino-2-(p-tolyl)acetic acid is used for optimizing azide skeleton, and is the intermediate in the synthesis of 1,3, 4-thiadiazole compounds. 1,3,4-thiadiazole compounds exhibit potential anti-cancer activity, and inhibit glutaminase (GLSI)[1][2].
9-(2’-O-Acetyl-5’-O-benzoyl-3’-O-methyl-beta-D-ribofuranosyl)-2,6-dichloropurine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
Alofanib (RPT835) is a potent and selective allosteric inhibitor of fibroblast growth factor receptor 2 (FGFR2). Anticancer activities[1]. Antiangiogenic Activity[2].
Tos-PEG7-OH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Arachidic acid-13C is the 13C labeled Arachidic acid. Arachidonic acid (Icosanoic acid), a long-chain fatty acid, is present in all mammalian cells, typically esterified to membrane phospholipids, and is one of the most abundant polyunsaturated fatty acids present in human tissue[1][2][3].
BI 7446 is a cyclic dinucleotide (CDN)-based potent and selective stimulator of interferon genes (STING) agonist. BI 7446 can activate all five STING variants in cells and induce tumor-specific immune-mediated tumor rejection. BI 7446 can be used for immuno-oncology research[1].
SIRT5 inhibitor 2 (compound 49) is a potent SIRT5 inhibitor with an IC50 value of 2.3 μM. SIRT5 inhibitor 2 has inhibitory activity against the SIRT5-dependent desuccinylation. SIRT5 inhibitor 2 can be used for researching cancer and neurodegenerative diseases[1].
Dihydroguaiaretic acid, is isolated from the fruits of Schisandra chinensis with an anti-cancer activty[1].
CK2-IN-9 is a potent and selective inhibitor of CK2 kinase with an IC50 of 3 nM. CK2-IN-9 reduces Wnt reporter activity with an IC50 of 75 nM. CK2-IN-9 has low exposure (AUC=0.36 μM/h) and high clearance (CL=65 mL/min/kg) properties in rat[1].
Costunolide, a sesquiterpene lactone, exhibits anti-inflammatory and anti-oxidant properties and mediates apoptosis.IC50 Value: 6.2 - 9.8 ug/mL(sarcoma cells viability)[3]Target: Apoptosis inducerin vitro: Costunolide significantly inhibited RANKL-induced BMM differentiation into osteoclasts in a dose-dependent manner without affecting cytotoxicity. Costunolide did not regulate the early signaling pathways of RANKL, including the mitogen-activated protein kinase and NF-κB pathways. However, costunolide suppressed nuclear factor of activated T-cells, cytoplasmic 1 (NFATc1) expression via inhibition of c-Fos transcriptional activity without affecting RANKL-induced c-Fos expression. The inhibitory effects ofcostunolide were rescued by overexpression of constitutively active (CA)-NFATc1 [1]. Exposure of T24 cells to costunolide was also associated with increased expression of Bax, down-regulation of Bcl-2, survivin and significant activation of caspase-3, and its downstream target PARP [2]. Both costunolide and dehydrocostus lactone inhibited cell viability dose- and time-dependently. IC50 values ranged from 6.2 ug/mL to 9.8 ug/mL. Cells treated with costunolide showed no changes in cell cycle, little in caspase 3/7 activity, and low levels of cleaved caspase-3 after 24 and 48 h [3].in vivo: Neither costunolide nor alpha-MGBL affected the blood-ethanol elevation in pylorus-ligated rats or that induced by intraperitoneal and intraduodenal ethanol administration [4]. Costunolide and alpha-MGBL suppressed gastric emptying in rats given 20% ethanol and 1% sodium carboxymethyl cellulose.Clinical trial:
Thalidomide-NH-C5-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology[1].