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.

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.

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.

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.

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'.

Flonoltinib maleate is a potent and orally active dual JAK2/FLT3 inhibitor with IC₅₀ values of 0.7 nM, 4 nM, 26 nM and 39 nM for JAK2, FLT3, JAK1 and JAK3, respectively. JAK2/FLT3-IN-1 has anti-cancer activity.

Fludarabine (Standard) is the analytical standard of Fludarabine. This product is intended for research and analytical applications. Fludarabine (NSC 118218) is a DNA synthesis inhibitor and a fluorinated purine analogue with antineoplastic activity in lymphoproliferative malignancies. Fludarabine inhibits the cytokine-induced activation of STAT1 and STAT1-dependent gene transcription in normal resting or activated lymphocytes.

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.

Thioridazine-d₃ 2-Sulfone is the deuterium labeled Thioridazine hydrochloride. Thioridazine hydrochloride, an orally active antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine hydrochloride is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine hydrochloride shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs).

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.

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.

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.

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).

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.

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.

C188-9 (Standard) is the analytical standard of C188-9 (HY-112288). This product is intended for research and analytical applications. C188-9 (TTI-101) is a STAT3 inhibitor with a K_d value of 4.7 nM. C188-9 targets the SH2 domain of STAT3, blocks the processes of STAT3 ligand binding, receptor recruitment, homodimerization and phosphorylation, and regulates STAT3-mediated genes associated with tumorigenesis and radioresistance. C188-9 regulates STAT1-mediated genes related to radioresistance and reduces the activation level of STAT1. C188-9 downregulates the expression of DNMT1, enhances DAC-induced demethylation and re-expression of RASSF1A, and simultaneously potentiates the anti-tumor effect of DAC on pancreatic cancer cells. C188-9 inhibits both anchorage-dependent and anchorage-independent growth of cancer cells, induces Apoptosis, blocks the growth of tumor xenografts, and suppresses muscle atrophy. C188-9 maintains muscle mass, increases body weight and improves grip strength in tumor-bearing mice. C188-9 can be used in research related to head and neck squamous cell carcinoma, pancreatic cancer, sepsis-related skeletal muscle wasting, non-small cell lung cancer, acute myeloid leukemia and cancer cachexia.

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.