Cancer Stem Cells

ABC1183 (Standard) is the analytical standard of ABC1183 (HY-100950). This product is intended for research and analytical applications. ABC1183 is an orally active selective dual GSK3 and CDK9 inhibitor. ABC1183 inhibits GSK3β, GSK3α and CDK9/cyclin T1 with the IC50 values of 657 nM, 327 nM and 321 nM, respectively. ABC1183 has anti-inflammatory and anti-tumor activities.

KYA1797K (Standard) is the analytical standard of KYA1797K (HY-101090). This product is intended for research and analytical applications. KYA1797K is a potent and selective Wnt/β-catenin inhibitor with an IC50 of 0.75 µM.

Acenocoumarol-d₅ is the deuterium labeled Acenocoumarol (HY-B1014). Acenocoumarol is an anticoagulant that functions as a Vitamin K antagonist. Acenocoumarol inhibits MAPK/ERK/JNK signaling pathway, reduces the nuclear translocation of NF-κB p65, activates Akt/GSK3β signaling pathway. Acenocoumarol induces apoptosis in cell A549, arrests cell cycle at S phase.

Gliquidone sodium (AR-DF 26 sodium) can bind to the pancreatic β-cells and increases insulin release to regulate blood glucose levels. Gliquidone sodium significantly decreases LPS (HY-D1056)-induced proinflammatory responses and inhibits ERK/STAT3/NF-κB phosphorylation in BV2 microglial cells. Gliquidone sodium can suppress microgliosis, microglial hypertrophy mediated by LPS, and proinflammatory cytokine COX-2 and IL-6 levels in murine model. Gliquidone sodium also exhibits good anticancer activity in lung carcinoma cells. Gliquidone sodium has antioxidant property. Gliquidone sodium can be studied in research for type 2 diabetes and cancers.

AX-15836 (Standard) is the analytical standard of AX-15836 (HY-101846). This product is intended for research and analytical applications. AX-15836 is a potent and selective ERK5 inhibitor with an IC₅₀ of 8 nM.

SB 202190 (Standard) is the analytical standard of SB 202190. This product is intended for research and analytical applications. SB 202190 is a selective p38 MAP kinase inhibitor with IC50s of 50 nM and 100 nM for p38α and p38β2, respectively. SB 202190 binds to the ATP pocket of the active recombinant human p38 kinase with a Kd of 38 nM. SB 202190 has anti-cancer activity and rescued memory deficits. SB202190 induces autophagy.

Iridin (Standard) is the analytical standard of Iridin. This product is intended for research and analytical applications. Iridin is an orally active natural isoflavone. Iridin inhibits the PI3K/AKT and PKM2 signaling pathways, and downregulates the JAK/STAT and NF-κB pathways. Iridin induces Fas-mediated extrinsic apoptosis, G2/M cell cycle arrest, and inhibits cell proliferation. Iridin reduces inflammation, inhibits ROS production, suppresses glycolysis, and also exhibits antioxidant and antidiabetic activities. Iridin can be used in research related to gastric cancer and acute lung injury.

MK-2206 dihydrochloride (MK-2206 2HCl) (Standard) is the analytical standard of MK-2206 dihydrochloride (HY-10358). This product is intended for research and analytical applications. MK-2206 dihydrochloride is an orally active pan-AKT inhibitor, with IC₅₀ values of 8 nM, 12 nM and 65 nM against AKT1, AKT2 and AKT3, respectively. MK-2206 dihydrochloride inhibits the Akt/mTOR signaling pathway and reduces the levels of downstream GSK3β and Mcl-1 via proteasomal degradation. MK-2206 dihydrochloride induces G1-phase cell cycle arrest, apoptosis, epithelial-mesenchymal transition, fibroblast activation and extracellular matrix deposition. MK-2206 dihydrochloride causes transient hyperglycemia and hyperinsulinemia in animals. MK-2206 dihydrochloride can be used in research related to solid tumors, renal fibrosis and hypercholesterolemia.

Fedratinib (hydrochloride hydrate) (Standard) is the analytical standard of Fedratinib (hydrochloride hydrate). This product is intended for research and analytical applications. Fedratinib hydrochloride hydrate (TG-101348 hydrochloride hydrate) is a potent, selective, ATP-competitive and orally active JAK2 inhibitor with IC50s of 3 nM for both JAK2 and JAK2V617F kinase. Fedratinib hydrochloride hydrate shows 35- and 334-fold selectivity over JAK1 and JAK3, respectively. Fedratinib hydrochloride hydrate induces cancer cell apoptosis and has the potential for myeloproliferative disorders research.

Cytochalasin D (Standard) is the analytical standard of Cytochalasin D (HY-N6682). This product is intended for research and analytical applications. Cytochalasin D (Zygosporin A) is a potent actin polymerization inhibitor, could be derived from fungus. Cytochalasin D has cell-permeable activity. Cytochalasin D inhibits the G-actin–cofilin interaction by binding to G-actin. Cytochalasin D also inhibits the binding of cofilin to F-actin and decreases the rate of both actin polymerization and depolymerization in living cells. Cytochalasin D can reduce exosome release, in turn reducing the amount of survivin present in the tumour environment. Cytochalasin D induces phosphorylation and cytoplasmic retention of Yap.

TACR1-IN-1 is a TACR1 inhibitor. TACR1-IN-1 attenuates Substance P-driven ERK phosphorylation and downstream malignant programs. TACR1-IN-1 reduces PGP9.5-positive tumor innervation in orthotopic PDAC models. TACR1-IN-1 increases antigen presentation and immune chemokine-related transcript expression under Substance P treatment conditions. TACR1-IN-1 reverses Substance P-associated reduction in Gemcitabine (HY-17026) sensitivity. TACR1-IN-1 can be used for research on pancreatic ductal adenocarcinoma.

DC-120 is an ATP-competitive AKT inhibitor, with particular activity against AKT1 (an IC₅₀ of 0.153 μM). DC-120 functionally blocks AKT kinase activity and reduces the phosphorylation levels of FOXO3a and GSK-3β. DC-120 induces cancer cell apoptosis (apoptosis) and inhibits cancer cell proliferation. DC-120 activates the mTORC1 pathway via the Ca²⁺/calmodulin (calmodulin)/hVps34 signaling pathway. DC-120 abrogates AKT-mediated inhibition of CRAF, thereby activating the MEK/ERK MAPK pathway. DC-120 exerts anti-tumor activity in a nude mouse hepatocellular carcinoma xenograft model. DC-120 can be used for hepatocellular carcinoma-related research.

AG490 (Standard) is the analytical standard of AG490 (HY-12000). This product is intended for research and analytical applications. AG490 (Tyrphostin AG490) is a tyrosine K_inase inhibitor that inhibits EGFR, Stat-3 and JAK2/3.

TC-E 5003 (Standard) is the analytical standard of TC-E 5003 (HY-107574). This product is intended for research and analytical applications. TC-E 5003 is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC₅₀ of 1.5 µM against hPRMT1. TC-E 5003 modulates the lipopolysaccharide (LPS) (HY-D1056)-induced AP-1 and NF-κB signaling pathways with anti-inflammatory properties. TC-E 5003 also upregulates the expression of Ucp1 and Fgf21, activates protein K_inase A signaling and lipolysis in primary subcutaneous adipocytes from both mouse and humans. TC-E 5003 is promising for research of obesity and associated metabolic disorders, oxidative stress, inflammation and cancers.

VT3989 (Standard) is the analytical standard of VT3989 (HY-400902). This product is intended for research and analytical applications. VT3989 is an orally active pan-TEAD autopalmitoylation inhibitor that modulates the Hippo signaling pathway. VT3989 directly binds to TEAD transcription factors to block their palmitoylation modification, thereby disrupting the formation of YAP/TAZ-TEAD complexes and inhibiting downstream oncogenic transcriptional activity. VT3989 effectively inhibits the growth of NF2-deficient schwannoma and meningioma cells and reverses the Schwann cell phenotype. In addition, VT3989 exerts a synergistic effect when combined with Osimtinib (HY-15772) in EGFR-mutant non-small cell lung cancer models, significantly delaying tumor recurrence and prolonging survival. VT3989 can be used for the research of epithelioid hemangioendothelioma, malignant pleural mesothelioma, type 2 neurofibromatosis and related advanced solid tumors.

7-keto-25-Hydroxycholesterol (7-keto-25-OHC), a oxysterol, is a Smoothened (Smo) activator. 7-keto-25-Hydroxycholesterol binds to the extracellular cysteine-rich domain (CRD) of Smo.

PF-4942847 is an orally active HSP90 inhibitor with an IC₅₀ of approximately 50 nM. PF-4942847 induces apoptosis in osteosarcoma cells, increases the proportion of cells in the sub-G1 phase and PARP cleavage, reduces the expression of Akt, Erk, MYC, c-MET and STAT-3, and regulates HSP expression. PF-4942847 can be used in studies related to osteosarcoma and HSP90.

Fluorofenidone-d₃ (AKF-PD-d3) is deuterium labeled Fluorofenidone (AKF-PD) (HY-121246). Fluorofenidone is an orally active compound with anti-fibrotic, antioxidant, and anti-inflammatory pharmacological effects. Fluorofenidone downregulates the expression of ACSL4, upregulates GPX4 expression and inhibits the NF-κB signaling pathway to alleviate inflammation and fibrosis. Fluorofenidone ameliorates cholestasis and fibrosis by inhibiting hepatic Erk/-Egr-1 signaling and Tgfβ1/Smad pathway in mice. Fluorofenidone demonstrates protective effects against chronic lung injury in mice. Fluorofenidone can be used for the study of chronic obstructive pulmonary disease (COPD), pulmonary interstitial fibrosis (PIF) and non-small cell lung cancer (NSCLC).

SMANT hydrochloride (Standard) is the analytical standard of SMANT (hydrochloride) (HY-108508). This product is intended for research and analytical applications. SMANT hydrochloride is a Smoothened (Smo) signaling inhibitor. SMANT hydrochloride is antagonist of Smo accumulation within the primary cilium (PC). SMANT hydrochloride has an equivalent activity in inhibiting SmoM2 (oncogenic form of Smo) and wild-type Smo.

Combretastatin A-1 (Standard) is the analytical standard of Combretastatin A-1. This product is intended for research and analytical applications. Combretastatin A-1 is a microtubule polymerization inhibitor that binds to the colchicine-binding site of tubulin. Combretastatin A-1 inhibits the Wnt/β-catenin pathway through tubulin depolymerization mediated AKT deactivation. Combretastatin A-1 exhibits anti-tumor and anti-vascular effects.