Bexarotene-d3 (LGD1069-d3) is the deuterium labeled Bexarotene. Bexarotene (LGD1069) is a high-affinity and selective retinoid X receptors (RXR) agonist with EC50s of 33, 24, 25 nM for RXRα, RXRβ, and RXRγ, respectively. Bexarotene shows limited affinity for RAR receptors (EC50 >10000 nM). Bexarotene can be used for the research of cutaneous T-cell lymphoma[1][2][3][4].
2,6-Dithiopurine (2,6-Dimercaptopurine) is a nucleophilic scavenger for electrophilic carcinogens. 2,6-Dithiopurine abolishes both DNA adduct formation and the initiation of carcinogenesis[1].
Monomethyl auristatin E intermediate-4 is an intermediate reagent 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].
Tucotuzumab (Anti-EPCAM Recombinant Antibody) is a protein composed of an IgG1 monoclonal antibody specific for the human Epithelial Cell Adhesion Molecule (EpCAM) antigen, linked to two molecules of IL-2. Tucotuzumab is an immunosuppressant and antineoplastic agent[1].
Allyl methyl sulfide is a bioactive organosulfur compound found in garlic. Allyl methyl sulfide exhibits antibacterial, antioxidant and anticancer properties[1].
Neamine tetrahydrochloride, a degradation product of Neomycin, is a broad-spectrum aminoglycoside antibiotic. Neamine tetrahydrochloride is an anti-angiogenesis agent targeting angiogenin. Neamine tetrahydrochloride has potent antibacterial, antitumor and neuroprotective activities[1][2].
Ganetespib is a heat shock protein 90 (HSP90) inhibitor which exhibits potent cytotoxicity in a wide variety of hematological and solid tumor cell lines.
TAM558 intermediate-54 is an intermediate in the synthesis of TAM558 (HY-148127).TAM558 is the payload molecule used in the synthesis of OMTX705.OMTX705 is a humanized anti-fibroblast activation protein (FAP) antibody that binds to the cytolysin TAM470 (HY-148128) and has anti-tumor activity[1].
Rigosertib (sodium) is a non-ATP-competitive inhibitor of PLK1 with an IC50 of 9 nM, and shows 30-fold selectivity over PLK2.
Clivatuzumab is a humanized anti-mucin monoclonal antibody targeting an epitope in the MUC1 antigen expressed in most pancreatic cancers[1].
AFP464, is an active HIF-1α inhibitor with an IC50 of 0.25 μM, also is a potent aryl hydrocarbon receptor (AhR) activator.
E3 Ligase Ligand-Linker Conjugates 24 (TFA) incorporates an E3 ligase ligand and a linker, can be an immunomodulater for the treatment of cancer.
GSK2194069 is a potent and specific inhibitor of the β-ketoacyl reductase (KR) activity of hFAS with an IC50 of 7.7 ± 4.1 nM in an assay detecting released CoA.IC50 value: Target: hFAS inhibitor
Trofosfamide-d4 is the deuterium labeled Trofosfamide. Trofosfamide is an orally bioavailable oxazaphosphorine derivative with antineoplastic activity[1][2].
(S)-ErSO is the dextrorotatory enantiomer of ErSO. (S)-ErSO is inactive in MCF-7 cells (from patent WO2020009958A1, compound (s)-105)[1].
Atrasentan is an endothelin receptor antagonist with IC50 of 0.0551 nM for ETA.
EcoRI Methyltransferase is a bacterial sequence-specific S-adenosyl-L-methionine-dependent DNA methyltransferase. EcoRI Methyltransferase relies on a complex conformational mechanism to achieve its remarkable specificity, including DNA bending, base flipping and intercalation into the DNA[1].
Oligomycin A, created by Streptomyces, acts as a mitochondrial F0F1-ATPase inhibitor, with a Ki of 1 μM; Oligomycin A shows anti-fungal activity.
RTS-V5 is a dual HDAC/proteasome inhibitor with IC50s of 6.9, 18, 15, 0.27, 0.53 μM for HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, respectively.
H-8 (dihydrochloride) is a cell-permeable, reversible and ATP-competitive PKA inhibitor[1].
VEGFR-2-IN-23 (compound 11b) is a potent and selective VEGFR-2 inhibitor with an IC50 value of 0.34 nM. VEGFR-2-IN-23 shows antitumor activity. VEGFR-2-IN-23 induces apoptosis and cell cycle arrest at G1 phase[1].
anti-TNBC agent-1 is a potent anti-triple-negative breast cancer (TNBC) agent. anti-TNBC agent-1 exhibits potent activity against different breast cancer cells with IC50 values ranging from 0.20 μM to 0.27 μM. anti-TNBC agent-1 induces apoptosis of SUM-159 cells through mitochondria pathway and causes G1 phase arrest of SUM-159 cells[1].
SBE13 Hydrochloride is a potent and selective Plk1 inhibitor, with an IC50 of 200 pM; SBE13 Hydrochloride poorly inhibits Plk2 (IC50>66 μM) or Plk3 (IC50=875 nM).
CGK733 is a potent ATM/ATR inhibitor, used for the research of cancer.
SMYD2-IN-1 is a SMYD2 inhibitor extracted from patent WO2016166186A1, compound example 1.1, has an IC50 of 4.45 nM[1].
Pomalidomide-C3-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a linker used in PROTAC technology[1].
AXL-IN-13 is a potent and orally active AXL inhibitor (IC50: 1.6 nM, Kd: 0.26 nM). AXL-IN-13 reverses TGF-β1-induced epithelial-mesenchymal transition (EMT), and inhibits cancer cell migration and invasion[1].
CDK-IN-2 is a potent and specific CDK9 inhibitor with IC50 of <8 nM, extracted from reference 1, example 4.IC50 Value: <8 nM [1]Target: CDK9In vitro:In vivo:
Euphornin is a anticaner agent, that can be isolated from E. helioscopia. Euphornin induces apoptosis via caspase-mediated pathways. Euphornin induces cell cycle arrest by increasing the level of the phospho-CDK1 (Tyr15) protein[1].
Rociletinib (CO-1686) is an orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M, and the Ki values for EGFRL858R/T790M and EGFRWT are 21.5 nM and 303.3 nM, respectively.