B-Raf inhibitor 1 dihydrochloride is a potent Raf kinase inhibitor with Kis of 1 nM, 1 nM, and 0.3 nM for B-RafWT, B-RafV600E, and C-Raf, respectively.
MMAF hydrochloride is an antitubulin agent that inhibit cell division; inhibits H3397 cell growth with an IC50 of 105 nM.
BAY 1217389 is a potent, and selective inhibitor of the monopolar spindle 1 (MPS1) kinase with an IC50 value less than 10 nM.
Glyphosate-13C2,15N is the 13C and 15N labled Glyphosate (HY-B0863). Glyphosate is an herbicidal derivative of the amino acid glycine. Glyphosate targets and blocks a plant metabolic pathway not found in animals, the shikimate pathway, required for the synthesis of aromatic amino acids in plants[1].
CCT-251921 is a potent, selective, and orally bioavailable CDK8 inhibitor with an IC50 of 2.3 nM.
Alloimperatorin (Prangenidin), a coumarin compound, is extracted from Angelica dahurica. Alloimperatorin (Prangenidin) has antitumor activity[1][2].
AUT1 is a Kv3 potassium channel modulator, with pEC50s of 5.33 and 5.31 for human recombinant Kv3.1b and Kv3.2a, respectively, exhibits 10-fold lower potency at human recombinant Kv3.3 channel (pEC50, 4.5)[1].
RG2833 is a brain-penetrant HDAC inhibitor with IC50 of 60 nM and 50 nM for HDAC1 and HDAC3, respectively.
EPZ011989 trifluoroacetate is a potent, selective orally bioavailable EZH2 inhibitor with Ki < 3 nM for EZH2 wt and EZH2 Y646; 15-fold selectivity over EZH1 and >3000-fold selectivity over other HMTase.IC50 value: < 3 nM ( Ki for wt EZH2, EZH2 Y646)Target: EZH2 inhibitorIn vitro: EPZ011989 is also a specific EZH2 inhibitor with a >15-fold selectivity over EZH1 and >3000-fold selectivity relative to the Ki of 20 other histone methyltransferases (HMTs) tested. EPZ011989 also exhibits metabolic stability. Furthermore, EPZ011989 reduces cellular H3K27 methylation in the Y641F, mutant-bearing human lymphoma cell line, WSU-DLCL2, with an IC50 below 100 nM. This functional response translates to activity in a long-term proliferation assay where EPZ011989 demonstrates an average lowest cytotoxic concentration (LCC) in WSU-DLCL2 cells of 208 nM. In vivo: The LCC parameter, when corrected for plasma protein-binding, predicts an efficacious plasma level in mouse for EPZ011989 of 158 ng/mL. The pharmacokinetics in SCID mice following oral administration of 125, 250, 500, and 1000 mg/kg indicated that the 1000 mg/kg dose provided coverage over the LCC for 24 h, while the 250 and 500 mg/kg doses provided coverage over this value for approximately 8 h. EPZ011989 demonstrates significant tumor growth inhibition in a mouse xenograft model of human B cell lymphoma.
Me-Tet-PEG4-NHBoc is an ADC Linker containing 4 PEG units. Me-Tet-PEG4-NHBoc can utilize its own Tetrazine group to undergo a specific inverse electron demand Diels-Alder reaction (iEDDA) with compounds with TCO groups.
PROTAC HER3-binding moiety 1 (compound 1b) is a Her3 Ligand for PROTAC[1].
Vialinin A (Terrestrin A) is a p-terphenyl compound with antioxidant properties[1]. Vialinin A is a potent inhibitor of TNF-α, USP4, USP5, and sentrin/SUMO-specific protease 1 (SENP1). Vialinin A (Terrestrin A) can be used for autoimmune diseases and cancer research[2][3].
Afuresertib is a potent and ATP-competitive specific Akt inhibitor.
Propargyl-PEG12-OH is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
SCFSkp2-IN-2 (Compound AAA-237) is a Skp2 inhibitor with a KD of 28.77 μM. AAA-237 induces apoptosis of NSCLC cells and shows antitumor activities[1].
2-(N,N-Dimethylamino)-N6,N6-dimethyladenosine is an adenosine analog. Adenosine analogs mostly act as smooth muscle vasodilators and have also been shown to inhibit cancer progression. Its popular products are adenosine phosphate, Acadesine (HY-13417), Clofarabine (HY-A0005), Fludarabine phosphate (HY-B0028) and Vidarabine (HY-B0277)[1].
N4-Benzoyl-3’-O-methylcytidine is a cytidine analog. Cytidine analogs have a mechanism of inhibiting DNA methyltransferases (such as Zebularine, HY-13420), and have potential anti-metabolic and anti-tumor activities[1].
Succinic anhydride is a cyclic anhydride and an ADC linker extracted from patent WO2009064913A1. It can react with compound 4 of the patent to link the prodrug to an amine or hydroxy 1 group of a targeting polypeptide[1].
5-(Furan-2-yl)-2’-O-methyl-5’-O-DMTr-uridine 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].
SIRT1-IN-3 (compound 3j) is a potent and selective SIRT1 inhibitor, with an IC50 of 4.2 μM[1].
Ezurpimtrostat (compound 2-2) is used for the study of fibrosis, cancer, autophagy and cathepsins B (CTSB), L (CTSL) and D (CTSD) related diseases (extracted from patent WO2020048694 A1)[1].
Fadrozole hydrochloride hemihydrate is an orally active, potent, selective and nonsteroidal aromatase inhibitor, with an IC50 of 6.4 nM. Fadrozole hydrochloride hemihydrate inhibits the production of estrogen and progesterone, with IC50 values of 0.03 and 120 μM. Fadrozole hydrochloride hemihydrate shows prevention of spontaneous tumours. Fadrozole hydrochloride hemihydrate can be used for the research of estrogen-dependent disease and cancer[1][2][3].
MP-Ala-Ala-PAB is a cleavable ADC Linker (ADC Linker). Fmoc-Ala-Ala-PAB can be used in the synthesis of antibody-drug conjugates (ADCs)[1].
PKD-IN-1 dihydrochloride (compound 32), an aminoethylamino-aryl (AEAA) compound, acts as PKD-1 inhibitor. PKD-IN-1 can be used for protein kinase D (PKD)-mediated diseases research[1].
tert-Butyl 11-aminoundecanoate (compound 6b) is a PROTAC linker, which refers to the PEG composition. tert-Butyl 11-aminoundecanoate can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins[1].
Litronesib is a selective Eg5 inhibitor, with antitumor activity.
Mubritinib (TAK-165) is a potent and selective EGFR2/HER2 inhibitor with an IC50 of 6 nM.
m-PEG8-C10-phosphonic acid is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
eCF309 is a potent and highly selective mTOR inhibitor with remarkably low off-target activities (IC50 = 10-15 nM, both in vitro and in cells)[1].
dBET6 is a highly potent, selective and cell-permeable degrader of BET based on PROTAC, with an IC50 of 14 nM, and has antitumor activity.