Tos-PEG2-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
CYPMPO is a spin-trapping reagent. CYPMPO, a cyclic DEPMPO-type nitrone, is evaluated for spin-trapping capabilities toward hydroxyl and superoxide radicals. anti-oxidant and anti-tumor activity[1].
PI-103 is a potent PI3K and mTOR inhibitor with IC50s of 8 nM, 88 nM, 48 nM, 150 nM, 20 nM, and 83 nM for p110α, p110β, p110δ, p110γ, mTORC1, and mTORC2. PI-103 also inhibits DNA-PK with an IC50 of 2 nM.
Tos-PEG6-C2-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Dihydroisotanshinone I is a bioactive compound present in a widely used traditional Chinese medicine named danshen.
7-MAD-MDCPT, a Camptothecin analog, is a toxin payload in antibody drug conjugates (ADCs)[1].
Tariquidar is a potent and specific inhibitor of P-glycoprotein (P-gp) with the high affinity (Kd=5.1±0.9 nM).
Sulfisoxazole (Sulfafurazole) diethanolamine is an endothelin receptor antagonist with IC50 values of 0.60 μM and 22 μM against endothelin receptor A and endothelin receptor B, respectively. Sulfisoxazole diethanolamine is a sulfonamide antibacterial with an oxazole substituent. Sulfisoxazole diethanolamine inhibits breast cancer exosome release by targeting endothelin receptor A[1][2].
Epibrassinolide is a natural brassinosteroid (BR) derivative, is a plant regulator with a similar structure to mammalian steroids. Epibrassinolide is a potential apoptotic inducer in various cancer cells without affecting the non-tumor cell growth.
Aliskiren fumarate is an orally active, highly potent and selective renin inhibitor, with IC50 of 1.5 nM. Aliskiren fumarate can be used for the research of hypertension, cardiovascular diseases and cancer cachexia[1][2][3].
Btk inhibitor 1 is a pyrazolo[3,4-d]pyrimidine derivative as a Btk kinase inhibitor.IC50 value:Target: BtkFrom PCT Int. Appl. (2012), WO 2012158843 A2 20121122.
Cathepsin inhibitor 1 (compound 25) is a potent and selective inhibitor of Cathepsin, with pIC50s of 7.9, 6.7, 6.0, 5.5 and 5.2 for CatL, CatL2, CatS, CatK, and CatB, respectively[1].
Cyclocreatine phosphate is an anti-tumor agent. Cyclocreatine phosphate is the proposed active form of cyclocreatine (CCr), a substrate analogue of creatine kinase. Cyclocreatine phosphate has anti-tumour activity and can be used for the research of cancer[1].
Swertiamarin, a secoiridoid glycoside found in genera of Enicostemma Species, confers anti-hyperglycemic and anti-hyperlipidemic effects[1].
Masitinib is an orally available Kit inhibitor with an IC50 of 200 nM. It also inhibits PDGFRα/β with an IC50 of 540 nM/800 nM nM.
Neorauflavane is a potent tyrosinase inhibitor derived from Campylotropis hirtella, with an IC50 value of 30 nM for tyrosinase monophenolase activity and an IC50 value of 500 nM for diphenolase activity. Neorauflavane can effectively reduce the melanin content of B16 melanoma cells[1].
CDK1-IN-2 is a CDK1 inhibitor (IC50: 5.8 μM)[1].
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].
OSU-T315 is an inhibitor of integrin-linked kinase (ILK) with an IC50 of 600 nM.
HIF-2α-IN-8 is a potent and orally active HIF2α inhibitor with IC50 values of 9, 37, 246 nM for HIF2α SPA, HIF2α iScript, HIF2α HRE RGA, respectively. HIF-2α-IN-8 shows antitumor activity[1].
Picfeltarraenin IA, a triterpenoid obtained from Picriafel-terrae Lour (P.fel-terrae), is an acetylcholinesterase (AChE) inhibitor. Picfeltarraenin IA can be used for the treatment of herpes infections, cancer and inflammation[1].
PARP10-IN-2 is a potent mono‐ADP‐ribosyltransferase PARP10 inhibitor with an IC50 of 3.64 μM for human PARP10. PARP10-IN-2 reveals potent inhibition on PARP2 and PARP15 with IC50s of 27 μM and 11 μM for human PARP2 and human PARP15, respectively[1].
Periplocymarin, a cardiac glycoside isolated from Periploca sepium and Periploca graeca, is a potential anti-cancer compound[1][2].
2′-Azido-2′-deoxy-5-methyluridine 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].
Auristatin E is a cytotoxic tubulin modifier with potent and selective antitumor activity; MMAE analog and cytotoxin in Antibody-drug conjugates.
Selpercatinib is a RET kinase inhibitor extracted from patent WO2018071447A1, Compound Example 163, has an IC50 of 14.0 nM, 24.1 nM, and 530.7 nM for RET (WT), RET (V804M) , and RET (G810R), respectively[1]. Antineoplastic activity[2].
Werner syndrome RecQ helicase-IN-4 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-4 shows antiproliferative activity. Werner syndrome RecQ helicase-IN-4 shows anticancer activity[1].
RC-3095 is a bombesin/gastrin releasing peptide receptor antagonist[1].
N-Boc-cis-4-hydroxy-L-proline is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). N-Boc-cis-4-hydroxy-L-proline is also a alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1][2
20(S)-hydroxyCholesterol (20α-Hydroxycholesterol) is an allosteric activator of the oncoprotein smoothened (Smo) that activates the hedgehog (Hh) signaling pathway with an EC50 of 3 μM in a gene transcription reporter assay using NIH3T3 cells[1][2].