PHT-247 is an inhibitor of the pleckstrin homology (PH) domain of Akt, and it is also an inhibitor of PDPK1 with Kis of 2.7 µM and 5.2 µM and for Akt and PDPK1, respectively.
CC-92480 is a cereblon E3 ubiquitin ligase modulating drug (CELMoD). CC-92480 shows high affinity to cereblon, resulting in potent antimyeloma activity[1].
Tos-PEG9-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Ru(bpy)2(mcbpy-O-Su-ester)(PF6)2 is a potent ruthenium-based dye. Ru(bpy)2(mcbpy-O-Su-ester)(PF6)2 can bu used as an effective quencher of quantum dots (QDs) fluorescence and the capture probe of virus antigen EV71. Ru(bpy)2(mcbpy-O-Su-ester)(PF6)2 can be used sensitive electrogenerated chemiluminescence (ECL) labels for detection of matrix metalloproteinases (MMPs)[1][2][3].
AZM475271 is a potent and selective Src kinase inhibitor with IC50 of 5 nM; no inhibitory activity on Flt3, KDR, Tie-2.IC50 value: 5 nM [1]Target: Src inhibitorin vitro: AZM475271 demonstrated strong dose-dependent inhibition of Src tyrosine kinase activity in the L3.6pl human pancreatic carcinoma cell line. Maximum reduction of Src kinase activity was observed after incubation for 4 hours with ≥5 μmol/L. The IC50 concentration of AZM475271 to inhibit the phosphorylation of c-src, lck, and c-yes was 0.01, 0.03, and 0.08 μmol/L, respectively, in comparison with an IC50 of 0.7 μmol/L AZM475271 to inhibit KDR [2].in vivo: Tumors appeared to be palpable at day 14 after tumor cell injection in all animals except mice treated with both AZM475271 and gemcitabine, in which the earliest possible palpation of the tumors was at day 17 after tumor cell injection. Treatment with gemcitabine or AZM475271 alone did not significantly change animal weight [2].
KRAS G12C inhibitor 54 (Compound 1) is a KRAS G12C inhibitor[1].
IMAB027 (ASP1650) is a specific anti-CLDN6 mAb, while CLDN6 (Claudin 6) is a tight junction membrane protein, aberrantly expressed in various human cancer types, ovarian cancers particularly. IMAB 027 shows anti-tumor activity, and induces apoptosis in CLDN6+ ovarian and testicular cancer cell lines[1].
MEK/PI3K-IN-2 (compound 6s) is a potent MEK/PI3K inhibitor, with IC50 values of 352 nM (MEK1), 107 nM (PI3Kα), and 137 nM (PI3Kδ), respectively. MEK/PI3K-IN-2 suppresses pAKT and pERK1/2 levels. MEK/PI3K-IN-2 shows anti-proliferative activity against tumor cell lines[1].
2’,3’,5’-Tri-O-acetyl-5,N3-dimethyluridine 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].
TM5007 is a poent and orally active inhibitor of plasminogen activator inhibitor-1 (PAI-1) with an IC50 of 29 μM. TM5007 enhance fibrinolysis activity and inhibits coagulation. TM5007 also prevents the fibrotic process initiated by bleomycin in mouse lung[1].
Patent Blue V (Acid blue 1) is a novel biological dye that can be used as an intraocular dye for retinectomy. Retinectomy refers to the removal of the translucent inner limiting membrane (ILM). The application of appropriate dyes in vitreoretinal surgery can achieve the purpose of complete removal. Patent Blue V can be used to stain retinal premembranous structures. Spectral analysis shows that Patent Blue V has strong absorption below 450 nm and above 600 nm, showing a blue-green color. Patent Blue V is also used as a marker in lymphangiography for resection of neoplastic lymph nodes[1][2].
DRF-1042 is an orally active camptothecin analog, which acts to inhibit DNA topoisomerase I. DRF-1042 shows good anticancer activity against a panel of human cancer cell lines[1][2].
XMD8-87 is a potent TNK2 inhibitor with IC50 values of 38 and 113 nM for the D163E and R806Q mutations, respectively.
4-Quinolone (Kynurine) is a quinoline derivative. Kynurine pathway modulates tryptophan metabolism and involves in neuroprotective effect. Kynurine promotes tumor cell survival and motility by suppressing antitumor immune[1][2].
ML385 is a specific nuclear factor erythroid 2-related factor 2 (NRF2) inhibitor with an IC50 of 1.9 μM.
Crocin is a nutraceutical and the main constituent isolated from the stigmas of Crocus sativus with immense pharmacological properties as anti-inflammatory, anticancer, antidepressant and anticonvulsant[1].
N-ε-propargyloxycarbonyl-L-lysine (H-L-Lys(Poc)-OH) is a lysine-based unnatural amino acid (UAA). N-ε-propargyloxycarbonyl-L-lysine is widely used for bio-conjugation of fluorescent probes in diverse organisms from E. coli to mammalian cells even in animals[1][2].
Mal-amido-PEG3-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
YM-08 (Compounds 7a) is a brain-penetrant inhibitors of SIRT2,with the IC50 of 19.9 μM. YM-08 also is inhibitor of Hsp70[1].
2’,3’,5’-Tri-O-benzoyl-5-hydroxymethyl-2’-β-C-methyluridine 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].
CYM-5482 is a potent and selective agonist Sphingosine 1-phosphate receptor 2 (S1PR2) with an IC50 and EC50 of 1.0 and 1.03 μM. CYM-5482 has the potential for the research of cancer diseases[1].
TH34, an HDAC6/8/10 inhibitor with IC50s of 4.6 μM, 1.9 μM, and 7.7 μM respectively, shows high selectivity over HDAC1/2/3[1].
BDP9066 is a potent and selective myotonic dystrophy-related Cdc42-binding kinases MRCK inhibitor with an IC50 of 64 nM for MRCKβ in SCC12 cells, Ki values of 0.0136 nM and 0.0233 nM for MRCKα/β in house determinations, respectively. BDP9066 has therapeutic effect on skin cancer by reducing substrate phosphorylation.
Pomiferin, a flavonoid from the fruits of Maclura pomifera, acts as an potential inhibitor of HDAC, with an IC50 of 1.05 μM, and also potently inhibits mTOR (IC50, 6.2 µM).
(R,R)-VVD-118313 is the isomer of VVD-118313 (HY-151385). VVD-118313 is a selective JAK1 inhibitor and blocks JAK1-dependent trans-phosphorylation and cytokine signaling. VVD-118313 can be used for research of cancer[1].
TP-3654 is a second-generation Pim kinase inhibitor with Ki values of 5 and 42 nM for Pim-1 and Pim-3, respectively.
FMK-MEA is a potent and selective p90 Ribosomal S6 Kinase (RSK) inhibitor.
VH032-C3-Boc is a Boc-modified VH032 (HY-120217) that serves as a ligand for VHL and recruits von Hippel-Lindau (VHL) proteins. VH032-C3-Boc will remove the protective group under acidic conditions and be directly used for PROTAC molecular synthesis. VH032-C3-Boc is a key intermediate for the synthesis of PROTACs based on VHL ligands.
Anamorelin Fumarate is a novel ghrelin receptor agonist with EC50 value of 0.74 nM in the FLIPR assay.
Guaiol is a sesquiterpene alcohol that has been found in several traditional Chinese medicinal plants and has antiproliferative, pro-autophagic, insect repellent, and insecticidal biological activities[1][2][3].