EGFR-IN-71 is a potent narrow spectrum epidermal growth factor receptor (EGFR) inhibitor with IC50 values of 3.7 μM. EGFR-IN-71 can be used for researching chordoma[1].
(S,R,S)-AHPC-C7-amine (VH032-C7-amine) hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used for estrogen-related receptor α (ERRα) PROTAC degrader[1].
BX517 is a potent and selective inhibitor of PDK1 with IC50 of 6 nM.
Angiotensin II 5-valine is an agonist of angiotensin receptor.
Indirubin-5-sulfonate is a cyclin-dependent kinase (CDK) inhibitor, with IC50 values of 55 nM, 35 nM, 150 nM, 300 nM and 65 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E, CDK4/cyclin D1, and CDK5/p35, respectively[1]. Indirubin-5-sulfonate also shows inhibitory activity against GSK-3β[2].
MRTX849 ethoxypropanoic acid incorporates a ligand for KRAS G12C, and a PROTAC linker. MRTX849 ethoxypropanoic acid can be used in the synthesis of PROTAC LC-2 (HY-137516). LC-2 is a potent and first-in-class PROTAC capable of degrading endogenous KRAS G12C (DC50s between 0.25 and 0.76 μM)[1][2].
Vitamin K5 (Synkamin) is a photosensitizer and a antimicrobial agent. Vitamin K5 is a specific PKM2 inhibitor with IC50 values of 28, 191 and 120 μM for PKM2, PKM1 and PKL. Vitamin K5 induces apoptosis of colon 26 cells. Vitamin K5 can be used for the research of infection and cancer, and it also can be used as a preservative for pharmaceuticals, foods, and beverages[1][2][3].
TCO-PEG8-NHS ester is a PEG-based PROTAC linker can be used in the synthesis of PROTACs[1].
Berkeleylactone F is an antibiotic macrolide compound. Berkeleylactone F showed modest inhibition of CCRF-CEM leukemia cells[1].
Pz-1 is a potent RET and VEGFR2 inhibitor with IC50s of less than 1 nM for both wild type kinases.
Sotetsuflavone is a potent inhibitor of DENV-NS5 RdRp (Dengue virus NS5 RNA-dependent RNA polymerase) with an IC50 of 0.16 uM, is the most active compound of this series .
(1S,3R)-GNE-502 (compound 179) is a potent ERα degrader with an EC50 value of 13 nM against ERα in MCF7 HCS. (1S,3R)-GNE-502 can be used to research cancer related with estrogen receptor[1].
ZC0101 is a potent, orally active IDO1 and TrxR dual inhibitor with IC50 values of 0.084 μM and 7.98 μM, respectively. ZC0101 effectively induces apoptosis and ROS accumulation in cancer cells[1].
Ferroptosis inducer-1 (compound BX-3a) is a Ferroptosis inducer with antitumor potential[1].
DCLX069 is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 value of 17.9 µM. DCLX069 shows less active against PRMT4 and PRMT6. DCLX069 has anticancer effects[1].
Werner syndrome RecQ helicase-IN-3 is a potent and orally active werner syndrome recQ helicase (WRN) inhibitor with an IC50 value of 0.06 µM. Werner syndrome RecQ helicase-IN-3 shows antiproliferative activity. Werner syndrome RecQ helicase-IN-3 shows anticancer activity[1].
SCO-PEG3-NHS is a PEG linker with a terminal imine(NH) group. SCO-PEG3-NHS is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
GNE-371 is a potent and selective chemical probe for the second bromodomains of human transcription-initiation-factor TFIID subunit 1 and transcription-initiation-factor TFIID subunit 1-like, with an IC50 of 10 nM for TAF1(2).
Ciliobrevin A is a hedgehog (Hh) signaling pathway inhibitor with median inhibitory concentration (IC50) less than 10 μM.
2-(3-Hydroxypicolinamido)acetic acid is a 2OG oxygenase inhibitor with an IC50 value of 3.4 μM. 2-(3-Hydroxypicolinamido)acetic acid can be used as a functional probe for potential therapeutic research[1].
DBeQ is a selective, potent, reversible, and ATP-competitive p97 inhibitor, with an IC50 value of 1.5 μM and 1.6 μM for p97(wt) and p97(C522A), respectively; DBeQ also inhibits Vps4 with an IC50 of 11.5 μM.
Y08284 is a potent, selective, oral active CBP bromodomain inhibitor with an IC50 of 4.21 nM. Y08284 suppresses the proliferation of prostate cancer cell lines LNCaP, C4-2B, and 22Rv1. Antitumor activity[1].
Vorsetuzumab mafodotin (SGN-75) is an Auristatin-based anti-CD70 antibody-drug conjugate (ADC). Vorsetuzumab mafodotin consists of a humanized monoclonal antibody, Vorsetuzumab and an ADC cytotoxin MMAF. Vorsetuzumab mafodotin has antineoplastic activity[1].
Brefeldin A is a specific inhibitor of protein trafficking which blocks the protein transport from the endoplasmic reticulum to the Golgi complex.
NH2-PEG5-C6-Cl (K-7) is a PROTAC linker, which refers to the PEG composition. NH2-PEG5-C6-Cl can be used in the synthesis of a series of PROTACs, and it induces degradation of intracellular molecules by autophagy[1].
Lificiguat binds to the β subunit of soluble guanylyl cyclase(sGC) with Kd of 0.6-1.1 μM in the presence of CO.
Biotinylated-JQ1 (Biotin-JQ1) is a biotinylated derivative of JQ1 with high affinity for the bromodomain of BRD4. Biotinylated-JQ1 inhibits MM1.S multiple myeloma cells proliferation with the EC50 of 0.4 μM[1].
Monomethyl auristatin E intermediate-11 is an intermediate reactant in the synthesis of Monomethyl auristatin E (HY-15162). Monomethyl auristatin E (MMAE) is a microtubule/tubulin inhibitor with anticancer activity. MMAE is widely used as the cytotoxic component (ADC Cytotoxin) of antibody-drug conjugates (ADCs)[1].
U-104 is a potent carbonic anhydrase (CA) inhibitor for CA IX and CA XII with Ki of 45.1 nM and 4.5 nM; low inhibition for CA I and CA II.IC50 value: 45.1 nM/4.5 nM(Ki, CA IX/CA XII) [1]Target: Carbonic anhydrase inhibitorin vitro: U-104 (50 μM) blocks the mesenchymal phenotype in the cancer stem cells population in hypoxia condition of 4T1 cells. U-104 (<50 μM) significantly reduces migration in a dose-dependent manner in metastatic MDA-MB-231 LM2-4Luc+ cells , with cells growing as compact colonies similar to parental MDA-MB-231 cells [2]. in vivo: U-104 (38 mg/kg) inhibits primary tumor growth in the mice implanted orthotopically with MDA-MB-231 LM2-4Luc+ cells. U-104 (19 mg/kg) inhibits metastases formation in the 4T1 experimental metastasis mice model [1]. U-104 (38 mg/kg) significantly delay primary tumor growth and reduces cancer stem cell population in NOD/SCID mice orthotopically implanted with MDA-MB-231 LM2-4Luc+ cells. U-104 (5 mg/mL, oral gavage) shows a significant delay in tumor growth in Balb/c mice orthotopically implanted with 4T1 cells [2].
KP1019 (FFC14A) is a Ru(III)-based anti-metastatic and cytotoxic anti-cancer agent. KP1019 induces DNA damage and apoptosis in cancer cells[1][2].