Deforolimus (AP23573; MK-8669) is a potent and selective mTOR inhibitor; inhibits ribosomal protein S6 phosphorylation with an IC50 of 0.2 nM in HT-1080 cells.
GSK4028 is the enantiomeric negative control of GSK4027, which is a PCAF/GCN5 bromodomain chemical probe, the pIC50 of GSK4028 is 4.9 in a time-resolved fluorescence resonance energy transfer (TR-FRET) assay.
L-Serine-d2 ((-)-Serine-d2) is the deuterium labeled L-Serine. L-Serine ((-)-Serine; (S)-Serine), one of the so-called non-essential amino acids, plays a central role in cellular proliferation.
KNK437 is a HSP inhibitor, and inhibits the induction of HSP105, HSP70, and HSP40.
Kazusamycin A (PD-114721) is an antitumor antibiotic. Kazusamycin A can be isolated from fermentation beers of a previously unknown actinomycete[1].
2-(trans-1,4-Dihydroxy-cyclohexyl)-5,7-dihydroxy-chromone is a flavone derivative that can be found in macrothelypteris torresiana. 2-(trans-1,4-Dihydroxy-cyclohexyl)-5,7-dihydroxy-chromone shows cytotoxic[1].
NSC 42834(JAK2 Inhibitor V, Z3), a novel specific inhibitor of Jak2, inhibits Jak2-V617F and Jak2-WT autophosphorylation in a dose-dependent manner but was not cytotoxic to cells at concentrations that inhibited kinase activity. IC50 value:Target: Jak2; Jak2-V617FZ3 selectively inhibited Jak2 kinase function with no effect on Tyk2 or c-Src kinase function. Z3 significantly inhibited proliferation of the Jak2-V617F-expressing, human erythroleukemia cell line, HEL 92.1.7. The Z3-mediated reduction in cell proliferation correlated with reduced Jak2 and STAT3 tyrosine phosphorylation levels as well as marked cell cycle arrest. Finally, Z3 inhibited the growth of hematopoietic progenitor cells isolated from the bone marrow of an essential thrombocythemia patient harboring the Jak2-V617F mutation and a polycythemia vera patient carrying a Jak2-F537I mutation.
IACS-8968 (S-enantiomer) is the S-enantiomer of IACS-8968. IACS-8968 is a dual IDO and TDO inhibitor, with pIC50s of 6.43 for IDO and <5 for TDO, respectively.
Terpendole I, a fungal indoloditerpene, is a ACAT (acyl-CoA: cholesterol acyltransferase) inhibitor (IC50=145 µM)[1].
RIPK3-IN-2 is a RIP3 inhibitor. RIPK3-IN-2 can be used in diseases caused by or associate with activated necrotic pathways research[1].
EZH2-IN-13 is a potent EZH2 inhibitor, for details please refer to compound 73 in patent WO2017139404. EZH2-IN-13 can be used to study cancers or precancerous lesions associated with EZH2 activity[1].
DSHN is a potent small heterodimer partner (SHP) activator. DSHN inhibits Ccl2 expression and secretion by inhibiting p65 activation of Ccl2 promoter activity. DSHN can be used in research of cancer[1].
Lipoamido-PEG4-azide is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
ALV2 is a potent and selective Helios degrader. ALV2 binds CRBN, with an IC50 of 0.57 μM. Helios is the zinc-finger transcription factor that can maintain a stable Treg cell phenotype in the inflammatory tumor microenvironment[1].
Fulvestrant 3-β-D-Glucuronide, a metabolite, is glucuronide and sulfate conjugates of Fulvestrant (HY-13636), a pure anti-estrogenic steroid. Fulvestrant 3-β-D-Glucuronide can be used for the research of breast cancer[1].
Lexatumumab (HGS-ETR 2) is a human agonistic TRAIL receptor 2 (TRAIL-R2, DR5, APO-2) IgG4κ type monoclonal antibody. Lexatumumab induces Apoptosis in malignant mesothelioma. Lexatumumab can be used for malignant pleural mesothelioma (MPM) research[1].
Rebastinib (DCC-2036) is a conformational control Bcr-Abl inhibitor for Abl1WT and Abl1T315I with IC50 of 0.8 nM and 4 nM, also inhibits SRC, KDR, FLT3, and Tie-2, and low activity to seen towards c-Kit.
SiR-COOH could be used to follow the intracellular location of the model therapeutic drug in GFP cells (Abs, 645 nm; Em, 676 nm)[1].
AZD5597 is an inhibitor of CDK with an IC50 of 2 nM. AZD5597 has potent anti-proliferative effects against a range of cancer cell lines[1].
FGFR3-IN-6 is a potent and selective FGFR3 inhibitor with IC50 value less than 350 nM. FGFR3-IN-6 can be used in research of cancer[1].
Demycarosyl-3D-β-D-digitoxosylmithramycin SK is a Mithramycin analog with good anti-tumor activity, which can prevent the proliferation and growth of tumor cells by binding and inhibiting DNA-binding proteins[1].
Sunitinib Malate (SU 11248 Malate) is a potent tyrosine kinase inhibitor targeting VEGFR2 and PDGFRβ with IC50s of 80 nM and 2 nM, respectively.
HX103 is an epidermal growth factor receptor (EGFR)-tyrosine kinase inhibitor (TKI)-based fluorogenic probe. HX103 inhibits EGFR 19 del, EGFR L858R, EGFR wild type and EGFR T790M with IC50s of 1.3, 1.5, 4.0 and 977 nM, respectively. HX103 can be used for quantifying active-EGFR to predict drug sensitivity in NSCLC patients with EGFR-activating mutations[1].
PTG-0861 (JG-265) is a novel potent, selective HDAC6 inhibitor with IC50 of 5.92 nM, >36-fold selectivity over other HDACs.PTG-0861 (JG-265) displays HDAC6 cellular target engagement with EC50 of 0.59 uM (ELISA), has in vitro and cellular selectivity superior to HDAC6-selective inhibitor citarinostat (ACY-241).PTG-0861 (JG-265) demonstrates potency against several blood cancer cell lines (e.g. MV4-11, MM1S), whilst showing limited cytotoxicity against non-malignant cells and CD-1 mice.PTG-0861 (JG-265) exihibits promising in vitro pharmacokinetics achieved with good safety profile in cells and in vivo.
Valproic acid sodium salt is an anticonvulsants used to treat epilepsy, bipolar disorder and migraines. Valproic acid inhibits histone deacetylase 1 (HDAC1) with an IC50 of 0.4 mM.
EGFR-IN-23 is a potent EGFR TKI (tyrosine kinase inhibitor) with an IC50 of 8.05 nM for BaF3/EGFR-DEL19/T790M/C797S cell (WO2021244502A1, compound 8)[1].
Ki8751 is a potent VEGFR2 inhibitor with an IC50 of 0.9 nM.
PF-04979064 is a potent and selective PI3K/mTOR dual kinase inhibitor with Kis of 0.13 nM and 1.42 nM for PI3Kα and mTOR, respectively.
Osemitamab is an IgG1 antibody targeting to human claudin-18.2. Osemitamab consists of human-Mus musculus monoclonal TST001 γ1-chain, disulfide with human-Mus musculus monoclonal TST001 κ-chain, dimer (ACI). Osemitamab in combination with Capecitabine (HY-B0016) and Oxaliplatin (HY-17371), can be used for G/GEJ cancer study[1][2].
Dihydro-5-azacytidine (DHAC), the nucleoside analog, is incorporated into DNA and inhibits DNA methylation. Dihydro-5-azacytidine has an antitumor activity[1][2].