Cancer Stem Cells

Bragsin2 (Standard) is the analytical standard of Bragsin2 (HY-111550). This product is intended for research and analytical applications. Bragsin2 is a potent, selective and noncompetitive nucleotide exchange factor BRAG2 inhibitor, with an IC₅₀ of 3 μM. Bragsin2 binds at the interface between the PH domain of BRAG2 and the lipid bilayer, leads BRAG2 unable to activate lipidated Arf GTPase. Bragsin2 affects breast cancer stem cells.

DB1255 is an ERG inhibitor that binds to the minor groove of DNA, with K_D values of 26 nM and 86 nM for the ATGA and AATT sequences, respectively. DB1255 targets and binds to specific DNA minor grooves (single GC/AT-rich sequences), forming a hydrogen bond network with G bases and AT pairs via its thiophene group and amidino group, respectively, thereby blocking the binding of transcription factors. DB1255 can be used in the research of leukemia and prostate cancer.

Phenformin (Phenethylbiguanide) (Standard) is the analytical standard of Phenformin (HY-16397). This product is intended for research and analytical applications. Phenformin (Phenethylbiguanide) is an orally active biguanide hypoglycemic agent. Phenformin inhibits mitochondrial respiratory chain complex I, leading to an increased AMP/ATP ratio, activation of AMPK, and subsequent inhibition of the mTOR pathway, thereby suppressing cell proliferation, inducing apoptosis and autophagy. Phenformin inhibits cancer stem cells (CSCs) and possesses potent antitumor potential.

SHP2-IN-31 is a SHP2 inhibitor, with IC₅₀s of 13 nM (Wild-type SHP2), >10000 nM (SHP1), >10000 nM (SHP2 E76K) . SHP2-IN-31 inhibits pERK in a panel of tumor cells. SHP2-IN-31 inhibits tumor growth in RTK/KRAS-driven xenograft models.

AZD-1480 (Standard) is the analytical standard of AZD-1480 (HY-10193). This product is intended for research and analytical applications. AZD-1480 is an ATP-competitive inhibitor of JAK1 and JAK2 with IC₅₀s of 1.3 nM and <0.4 nM, respectively.

Sonidegib (Standard) is the analytical standard of Sonidegib. This product is intended for research and analytical applications. Sonidegib (Erismodegib) is a potent and selective Smo antagonist with IC50 of 1.3 nM and 2.5 nM for mouse and human Smo in binding assay, respectively.

Indazole (Standard) is the analytical standard of Indazole. This product is intended for research and analytical applications. Indazole, also called isoindazole, a heterocyclic aromatic organic compound. Its derivatives display a broad variety of biological activities including anti-inflammatory, antibacterial, anti-HIV, antiarrhythmic, antifungal and antitumour properties. Indazole and its derivatives can be used for research of cancer, neurological disorders, cardiovascular diseases, gastrointestinal diseases.

O-Methylbulbocapnine is an aporphine alkaloid that acts as an inhibitor of LPS-induced inflammatory signaling and a dopamine D1R antagonist. O-Methylbulbocapnine inhibits LPS-induced phosphorylation of p38, ERK1/2, c-Jun, NF-κB p65 at Ser536, and Akt, decreases MyD88 protein levels, and reduces NF-κB nuclear translocation and DNA-binding activity. O-Methylbulbocapnine inhibits LPS-induced production of IL-6, TNF-α, PGE₂, and NO, and decreases COX-2 and iNOS expression. O-Methylbulbocapnine can be used for research on Alzheimer's disease, cervical cancer, breast cancer, and malaria.

Silmitasertib (sodium salt) (Standard) is the analytical standard of Silmitasertib (sodium salt). This product is intended for research and analytical applications. Silmitasertib sodium salt is an orally bioavailable, highly selective and potent CK2 inhibitor, with IC50 values of 1 nM against CK2α and CK2α'.

NMS-P953 (compound 28) is an orally active JAK2 inhibitor (IC₅₀=0.008 μM) with antitumor activity.

6-Bn-cAMP is a site-selective activator of cAMP-dependent protein kinase (PKA) which does not activate Epac. 6-Bn-cAMP increases hydrolytic stability against PDE, esterases, amidases and considerably higher membrane permeability compared to cAMP.

GYY4137 (Standard) is the analytical standard of GYY4137 (HY-107632). This product is intended for research and analytical applications. GY4137 is a sustained-release H2S donor possessing vasodilatory, antihypertensive, and anti-inflammatory activities. GY4137 can inhibit cell growth, induce apoptosis, and cause cell cycle arrest by blocK_ing the STAT3 pathway, demonstrating potent anticancer activity.

exo-IWR-1 (Standard) is the analytical standard of exo-IWR-1 (HY-108437). This product is intended for research and analytical applications. exo-IWR-1, an inactive stereoisomer of Endo-IWR-1, is a negative control of IWR-1 (HY-12238). IWR-1 is a tankyrase inhibitor which inhibits Wnt/β-catenin signaling pathway.

TDP-665759 is an inhibitor for HDm2:p53 complex, and thus activates p53, inhibits STAT3 signaling pathway (EC₅₀ of 5.90 μM) and the cell viability of p53 expressing A549R (IC₅₀ of 7.02 μM). TDP-665759 induces apoptosis in HepG2. TDP-665759 exhibits antitumor efficacy in mouse models.

Lazertinib (Standard) is the analytical standard of Lazertinib (HY-109061). This product is intended for research and analytical applications. Lazertinib (YH25448) is a potent, selective, CNS-penetrant, orally available and irreversible EGFR tyrosine K_inase inhibitor, exhibiting high selectivity for activating (EGFRm) and T790M resistance mutations. Lazertinib inhibits phosphorylation of EGFR, AKT and ERK, leading to apoptosis and suppression of tumor growth in mouse H1975-luc brain metastasis xenograft models. Lazertinib can be used in the study of non-small cell lung cancer.

SMO-IN-2 is a potent smoothened (SMO) inhibitor with an IC₅₀ value of 123.4 nM for hedgehog (Hh) signaling pathway. SMO-IN-2 has antiproliferative activity against human medulloblastoma cell line Daoy. Anticancer activity.

IM-12 (Standard) is the analytical standard of IM-12. This product is intended for research and analytical applications. IM-12 is an inhibitor of GSK-3β, with an IC50 of 53 nM, and also enhances Wnt signalling.

Atiprimod (Azaspirane) hydrochloride is a STAT3 inhibitor with antitumor, anti-inflammatory, and anti-angiogenic activities. Atiprimod blocks the signaling pathways of IL-6 and VEGF by inhibiting the phosphorylation of signal transducer and activator of STAT3. Atiprimod blocks the JAK-STAT signaling pathway by inhibiting the phosphorylation of JAK2 and JAK3. Atiprimod also inhibits cell proliferation, induces cell cycle arrest, and induces autophagy and apoptosis. Atiprimod triggers persistent ER stress-mediated apoptosis in breast cancer cells by activating the PERK/eIF2α/ATF4/CHOP axis and inhibiting the nuclear translocation of STAT3/NF-κB. Atiprimod shows great anti-tumor activities in tumor xenograft mouse models. Atiprimod can be used for the study of pituitary adenoma, breast cancer, multiple myeloma and acute myeloid leukemia (AML).

CK2-IN-18 is a protein kinase CK2 inhibitor with an IC₅₀ of > 30 μM against protein kinase CK2. CK2-IN-18 can be used in studies related to CK2-mediated signaling pathways, such as various cancers including lung cancer and breast cancer.

ROCK-IN-18 is a blood-brain barrier-permeable selective inhibitor of the ROCK2 protein kinase. ROCK-IN-18 is applicable to research related to cardiovascular diseases, neurological diseases, breast cancer, colon cancer, pancreatic cancer and other disorders.