Cancer Stem Cells

Oxymatrine-d₃ is the deuterium labeled Oxymatrine (HY-N0158). Oxymatrine, an alkaloid from Sophora flavescens Alt. with anti-inflammatory, antifibrosis, and antitumor effects, inhibits the iNOS expression and TGF-β/Smad pathway. Oxymatrine inhibits bocavirus minute virus of canines (MVC) replication, reduces viral gene expression and decreases apoptosis induced by viral infection.

Trilinolein (Standard) is the analytical standard of Trilinolein (HY-128393). This product is intended for research and analytical applications. Trilinolein is an orally active triglyceride that inhibits the PI3K/Akt, Ras/MEK/ERK signaling pathways, and MMP-2. Trilinolein can reduce oxidative stress, induce apoptosis, and inhibit cell migration. Trilinolein can be used in the research fields of cardiovascular disease, cerebrovascular disease (such as cerebral ischemia), and non-small cell lung cancer.

WHN-88 is a Porcupine (PORCN) inhibitor. WHN-88 can eliminate the palmitoylation of Wnt ligands, preventing their secretion and subsequent Wnt/β-catenin signaling. WHN-88 can inhibit cancer cell stemness and suppress the occurrence and development of breast tumors in MMTV-Wnt1 transgenic mice.

D-2-Phosphoglyceric acid is an intermediate product of glycolysis and gluconeogenesis, and its level changes are associated with the glycolysis pathway regulated by MCT4. The intracellular level of D-2-Phosphoglyceric acid decreases in hypoxic glioblastoma stem cells after MCT4 knockdown. D-2-Phosphoglyceric acid can be used in the research of glioblastoma.

3',4'-Dimethoxyflavone is a lipophilic flavone, can be isolated from the leaves of Primula veris. 3',4'-Dimethoxyflavone can reduce the synthesis and accumulation of PARP and protect cortical neurones against cell death induced by Parthanatos. 3',4'-Dimethoxyflavone is also an aryl hydrocarbon receptor antagonist in human breast cancer cells. 3',4'-Dimethoxyflavone can promote the proliferation of human hematopoietic stem cells. 3',4'-Dimethoxyflavone has various biological activities, including antioxidant, anti-cancer, anti-inflammatory, anti-atherogenic, hypolipidaemic, and neuroprotective or neurotrophic effects.

Erlotinib-d₈ (CP-358774-d₈) is the deuterated-labeled Erlotinib (HY-50896). Erlotinib (CP-358774) is a selective, orally active EGFR tyrosine kinase inhibitor. Erlotinib also acts as a substrate and inhibitor of OATP2B1, with an IC₅₀ of approximately 0.079 μM for inhibiting OATP2B1-mediated uptake of estrone 3-sulfate. Erlotinib blocks EGFR phosphorylation, downstream signal transduction, as well as the growth and proliferation of cancer cells. Erlotinib inhibits MMP-10-mediated renal injury, fibrotic lesions, the ERK1/2, GSK-3β and β-catenin signaling pathways, as well as the deposition of fibronectin, α-SMA, collagen and renal injury markers. Erlotinib is metabolized via CYP3A to produce the active metabolite OSI-420. Erlotinib can be used in research related to non-small cell lung cancer, gastric cancer, papillary renal cell carcinoma, EGFR inhibitor resistance and renal fibrosis.

Tropisetron-d₅ (SDZ-ICS-930-d₅ (free base)) is deuterium labeled Tropisetron. Tropisetron (SDZ-ICS-930 free base) is an orally active anti-inflammatory and antiemetic agent. Tropisetron is 5-HT₃R antagonists with a K_i of 5.3 nM. Tropisetron is also a partial agonist of α7 nicotinic receptor (α7 nAChR) with an EC₅₀ of 1.3 μM. In addition, Tropisetron has antitumor and neuroprotective effects.

mCMY020 is a covalent inhibitor of TEAD. mCMY020 effectively reduces YAP (Yes-associated protein)-driven transcription and selectively slows the proliferation of Hippo-deficient cancer cells. mCMY020 can be used in cancer research.

LDN193189 (DM-3189) Tetrahydrochloride (Standard) is the analytical standard of LDN193189 Tetrahydrochloride (HY-12071A). This product is intended for research and analytical applications. LDN193189 (DM-3189) Tetrahydrochloride is a potent selective BMP type I receptor (BMP I) inhibitor. LDN193189 efficiently inhibits transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC₅₀ values of 5 nM and 30 nM, respectively. LDN193189 can be used for the research of bone morphogenetic protein signalling, such as fibrodysplasia ossificans progressiva.

WAY 316606 (Standard) is the analytical standard of WAY 316606 (HY-10858). This product is intended for research and analytical applications. WAY 316606 is an inhibitor of the secreted protein sFRP-1, an endogenous antagonist of the secreted glycoprotein Wnt. The affinity of WAY-316606 for sFRP-1 is determined using the FP binding assay with IC₅₀ of 0.5 μM.

CDK8-IN-16 (Compound 51) is an orally active dual inhibitor for CDK8 and CDK19 wih IC₅₀ of 5.1 nM and 5.6 nM. CDK8-IN-16 inhibits the phospho-STAT1^SER727 with an IC₅₀ of 17.9 nM in SW620 cell, inhibits WNT signaling pathway with an IC₅₀ of 7.2 nM in 7dF3 cell. CDK8-IN-16 exhibits good pharmacokinetic characteristics in rat models with an oral bioavailability of 57%.

Ceftriaxone (sodium hydrate) (Standard) is the analytical standard of Ceftriaxone (sodium hydrate). This product is intended for research and analytical applications. Ceftriaxone sodium hydrate (Ro 13-9904 sodium hydrate) is a broad spectrum β-lactam third-generation cephalosporin antibiotic, which has good antibacterial activity against a variety of gram-negative and positive bacteria. Ceftriaxone sodium hydrate is a covalent inhibitor of GSK3β with IC₅₀ value of 0.78 μM. Ceftriaxone sodium hydrate is an inhibitor of Aurora B. Ceftriaxone sodium hydrate has anti-inflammatory, antitumor and antioxidant activities. Ceftriaxone sodium hydrate can be used in the study of bacterial infections and meningitis.

H-89 dihydrochloride (Standard) is the analytical standard of H-89 dihydrochloride (HY-15979A). This product is intended for research and analytical applications. H-89 dihydrochloride is a potent and selective inhibitor of protein K_inase A (PKA) with an IC₅₀ of 48 nM and has weak inhibition on PKG, PKC, Casein K_inase.

DTP3 (Standard) is the analytical standard of DTP3 (HY-100538). This product is intended for research and analytical applications. DTP3 TFA is a potent and selective GADD45β/MKK7 inhibitor. DTP3 TFA targets an essential, cancer-selective cell-survival module downstream of the NF-κB pathway.

MEDI0639 (21H3RK) is a human monoclonal antibody (mAb) targeting DLL4. MEDI0639 inhibits Notch1 binding to Dll4. MEDI0639 reverses Notch1-mediated growth inhibition of human umbilical vein endothelial cells in vitro. MEDI0639 promotes human angiogenesis and reduces the number of vessels covered by smooth muscle actin-positive mural cells. MEDI0639 can be used in Small cell lung cancer and solid tumors research.

FTI-277 TFA is a farnesyltransferase (FTase) inhibitor. FTI-277 TFA inhibits Ras farnesylation, blocks the phosphorylation of downstream ERK1/2 and mTOR, and reduces membrane-bound active N-ras protein. FTI-277 TFA activates caspase 3, upregulates Bim expression, induces cell apoptosis, suppresses regulatory T cell expansion, enhances macrophage phagocytosis, and improves bacterial clearance. FTI-277 TFA activates the PI3K/Akt signaling pathway, inhibits osteoblast differentiation, and reduces the proliferation ability of neuroblastoma cells. FTI-277 TFA can be used in research related to head and neck squamous cell carcinoma, neuroblastoma, sepsis, and vascular calcification.

AH057 is an orally active JAK1 and JAK2 inhibitor. AH057 blocks IL-6-, IFN-α- and IFN-γ-induced JAK/STAT signaling, reduces cancer cell proliferation, invasion and colony formation, and induces apoptosis and G1 cell-cycle arrest. AH057 can be used for cervical cancer research.

Y-33075 (dihydrochloride) (Standard) is the analytical standard of Y-33075 (dihydrochloride) (HY-10069). This product is intended for research and analytical applications. Y-33075 dihydrochloride is a selective ROCK inhibitor with an IC50 of 3.6 nM.

WAY-262611 (Standard) is the analytical standard of WAY-262611 (HY-11035). This product is intended for research and analytical applications. WAY-262611 is a Wnt/β-Catenin agonist that increases bone formation rate with an EC₅₀ of 0.63 μM in TCF-Luciferase assay. WAY-262611 is also a Dkk1 inhibitor.

RUSKI-201 is a potent and specific Hedgehog acyltransferase (Hhat) inhibitor, with an IC₅₀ of 0.20 μM. RUSKI-201 is able to block Hh signaling from Shh overexpressing cells and inhibits Hh palmitoylation. RUSKI-201 is potential Hhat chemical probe in cells and can used in studies of Hhat catalytic function.