FR900359 is a depsipeptide selective inhibitor of Gαq/11/14 in mammalia, can inhibits ERK pathway. FR900359 suppresses the proliferation of melanoma cells and decreases of blood pressure. FR900359 also protected against airway hyperreactivity in murine models of allergen sensitization in Ovalbumins(HY-W250978)–induced sensitization model of asthma. FR900359 can be used for cancer and cardiovascular disease research[1][2][3][4].
Aromatase-IN-2 is a potent Aromatase inhibitor with an IC50 value of 1.5 µM[1].
Multi-kinase-IN-3 (compound 2) is a potent angiokinase inhibitor. Multi-kinase-IN-3 shows inhibition activity against VEGFR-2 and PDGFRβ, with IC50 values of 58.3 and 55 nM, respectively[1].
PAD-IN-2 is a potent pad4 inhibitor (IC50: <1 μM). PAD-IN-2 can be used in the research of auto-immune diseases and cancers, such as rheumatoid arthritis, vasculitis, systemic lupus erythematosis, cutaneous lupus erythematosis, ulcerative colitis, cystic fibrosis, asthma, multiple sclerosis and psoriasis[1].
1-Boc-azetidine-3-yl-methanol is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). 1-Boc-azetidine-3-yl-methanol is also a alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1]
TRK-IN-13 is a potent inhibitor of TRK. Protein kinases play a critical role in the control of cell growth and differentiation and are responsible for the control of a wide variety of cellular signal transduction processes. TRK-IN-13 has the potential for the research of TRK-related diseases (extracted from patent WO2012034091A1, compound X-24)[1].
Volociximab (M200) is a chimeric human/murine IgG4 antibody IIA1 targeting integrin α5β1 (EC50=0.2 nM). Integrin α5β1 is a major fibronectin receptor involved in angiogenesis. Volociximab has antiangiogenic and antitumor activities and inhibits the proliferation of human umbilical vein vascular endothelial cells (HUVECs)[1][2].
RET-IN-5 is a potent RET (rearranged during transfection) inhibitor with an IC50s of 0.4 nM and 135.1 nM for RET and VEGFR2, respectively (WO2021213476A1, compound 18)[1].
RKI-1313 is a ROCK inhibitor with IC50s of 34, 8 µM for ROCK 1 and ROCK 2, respectively. RKI-1313 shows little effect on the phosphorylation levels of ROCK substrates, migration, invasion or anchorage-independent growth[1].
Genkwadaphnin is a daphnane diterpenoid, targeting of importin-β1 to reduce the nuclear accumulation of key CRPC drivers, and shut down their downstream oncogenic signaling. Genkwadaphnin shows potent anti-tumor activity and inhibits castration-resistant prostate cancer (CRPC) in vivo in mice[1].
ALK-IN-6 (compound 11) is an orally bioavailable inhibitor of anaplastic lymphoma kinase (ALK), with IC50 values of 71 nM, 18.72 nM and 36.81 nM for ALK wild, ALK F1196M and ALK F1174L, respectively[1].
Escin IA is a triterpene saponin isolated from horse chestnut, which inhibits HIV-1 protease with IC50 values of 35 μM. Escin IA has anti-TNBC metastasis activity, and its action mechanisms involved inhibition of epithelial-mesenchymal transition process by down-regulating LOXL2 expression[1][2].
BRD4-BD1/2-IN-1 is a potent BRD4 inhibitor with IC50s of <100 nM for BRD4 BD-1 and BRD4 BD-2, respectively (US20150148375A1, compound 5)[1].
Mal-PEG2-NHS ester is a nonclaevable ADC linker containing a Maleimide group, 2-unit PEG and an NHS ester.
Dolastatin 10 is a potent antimitotic peptide, isolated from the marine mollusk Dolabela auricularia, that inhibits tubulin polymerization.
Ac-AAVALLPAVLLALLAP-LEHD-CHO is an inhibitor of caspases 4, 5 and 9. Ac-AAVALLPAVLLALLAP-LEHD-CHO shows protective effects upon Neocarzinostatin (HY-111183)-treated MCF-7 cells[1].
SPDMV-sulfo is a glutathione cleavable ADC linker used for the antibody-drug conjugate (ADCs)[1].
Ardisiacrispin B displays cytotoxic effects in multi-factorial drug resistant cancer cells via ferroptotic and apoptotic cell death[1].
Deltazinone 1 (Deltazinone1) is a novel highly selective PDEδ inhibitor that inhibits PDEδ/Ras interaction with Kd of 8±4 nM; displays excellent selectivity against a broad panel of pharmacologically relevant proteins; inhibits the PDEδ-Ras interaction in in-cell measurement with Kd of 58±17 nM, exhibits less unspecific cytotoxicity than Deltarasin in a set of human pancreatic cancer cell lines, including KRas mutation and oncogenic KRas-dependence, decreases Ras-mediated signalling in pancreatic cancer cells.
3’,5’-Di-O-acetyl-2’-deoxy-N3-methyl 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].
(3S,5S,6R)-Navtemadlin is the inactive isomer of Navtemadlin (HY-12296), and can be used as an experimental control. Navtemadlin (AMG 232) is a potent, selective and orally available inhibitor of p53-MDM2 interaction, with an IC50 of 0.6 nM. Navtemadlin binds to MDM2 with a Kd of 0.045 nM[1][2].
Anthraflavic acid, a flavonoid, is a potent IQ mutagenicity inhibitor by virtue of its ability to inhibit both its microsomal and cytosolic activation pathways. Anthraflavic acid is a potent and specific cytochrome P-448 inhibitor activity an enzyme system closely associated with the activation of many chemical carcinogens[1].
Sildenafil-d3-1 (UK-92480-d3-1) is deuterium labeled Sildenafil-d3. Sildenafil (UK-92480) is a potent phosphodiesterase type 5 (PDE5) inhibitor with an IC50 of 5.22 nM.
Pracinostat is a potent histone deacetylase (HDAC) inhibitor, with IC50s of 40-140 nM, used for cancer research.
3'-Deoxyinosine 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].
Lenalidomide-5-aminomethyl is the Lenalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Lenalidomide-5-aminomethyl can be connected to the ligand for protein by a linker to form PROTAC[1].
BPR1R024 mesylate is an orally active and selective colony-stimulating factor-1 receptor (CSF1R) inhibitor.BPR1R024 mesylate is the equivalent of BPR1R024 (HY-132935). BPR1R024 has potent CSF1R inhibition activity with an IC50 value of 0.53 nM. BPR1R024 can be used for the research of immuno-oncology[1].
Furanodiene is a natural terpenoid isolated from Rhizoma Curcumae. Furanodiene plays anti-cancer effects through anti-angiogenesis and inducing ROS production, DNA strand breaks and apoptosis. Furanodiene suppresseed efflux transporter Pgp (P-glycoprotein) function and reduced Pgp protein level[1].
CD437 is a selective Retinoic Acid Receptor γ (RARγ) agonist.
5-(Furan-2-yl)-2’-O-methyl-5’-O-DMTr-cytidine 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].