Cancer Stem Cells

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.

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.

Belumosudil-d₇ (KD025-d₇) is deuterium labeled Belumosudil. Belumosudil (KD025) is a selective inhibitor of ROCK2 with IC₅₀s of 105 nM and 24 μM for ROCK2 and ROCK1, respectively. Anti-fibrotic properties.

CCT070535 blocks TCF-dependent transcription at the TCF level, with GI₅₀ values of 17.6 μM, 11.1 μM, 11.8 μM and 13.4 μM in HT29 (APC mutant), HCT116 (oncogenic β-catenin), SW480 (APC mutant) and SNU475 (Axin mutant) cells, respectively.

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.

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).

Salinomycin (Standard) is the analytical standard of Salinomycin. This product is intended for research and analytical applications. Salinomycin (Procoxacin), a polyether potassium ionophore antibiotic, selectively inhibits the growth of gram-positive bacteria. Salinomycin is a potent inhibitor of Wnt/β-catenin signaling, blocks Wnt-induced LRP6 phosphorylation. Salinomycin shows selective activity against human cancer stem cells[1][2][3].

Trimebutine maleate (Standard) is the analytical standard of Trimebutine maleate (HY-B0380A). This product is intended for research and analytical applications. Trimebutine maleate is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine maleate inhibits L-type Ca²⁺ channels and large-conductance calcium-activated potassium channels (BK_Ca channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine maleate also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine maleate also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine maleate also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS).

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.

P18IN011 is an inhibitor that specifically targets the interaction between p18(INK4C) and CDK6, with an IC₅₀ of 3.61 μM against mouse p18INK4C. P18IN011 relieves p18-mediated CDK6 inhibition, thereby effectively regulating the G1 phase cell cycle checkpoint. P18IN011 significantly enhances the proliferation, self-renewal and bone marrow reconstitution abilities of hematopoietic stem cells, and increases the frequency of primitive hematopoietic cells to promote cobblestone area formation. Acting specifically on p18-expressing hematopoietic cells via CDK4/6, P18IN011 not only supports the ex vivo expansion of human umbilical cord blood hematopoietic stem cells, but also maintains their long-term reconstitution capacity during in vitro culture to enable multi-lineage transplantation.

Cyclo (L-Ile-D-Leu) (Compound 15) is a STAT3 inhibitor. Cyclo (L-Ile-D-Leu) is isolated from the culture broth of Lactococcus lactis KR-050L. Cyclo (L-Ile-D-Leu) inhibits IL-6-induced STAT3 activation in cancer cells. Cyclo (L-Ile-D-Leu) is applicable to hepatocellular carcinoma research.

Benzyl salicylate (Standard) (NSC 6647 (Standard)) is the analytical standard of Benzyl salicylate (HY-B1556). This product is intended for research and analytical applications. Benzyl salicylate (NSC 6647)?is a salicylic acid benzyl ester. It can be used as a fragrance additive or UV light absorber.

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

MRT-92 is a Smoothened (Smo) antagonist (K_i=0.7 nM) with anticancer activity. MRT-92 inhibits Hedgehog signaling pathway and rodent cerebellar granule cell proliferation by blocking overlapping binding sites in the transmembrane domain of the Smoothened receptor (IC₅₀=0.4 nM). MRT-92 can be used in the study of cerebellar glioma.

AR-A014418 (Standard) is the analytical standard of AR-A014418. This product is intended for research and analytical applications. AR-A014418 is a potent, selective and ATP-competitive GSK3β inhibitor (IC50=104 nM; Ki=38 nM).

Human POU class 5 homeobox 1 (POU5F1) mRNA encodes a transcription factor containing a POU homeodomain that plays a key role in embryonic development and stem cell pluripotency. Aberrant expression of this gene in adult tissues is associated with tumorigenesis.

TM-233 is an inhibitor of the JAK/STAT and NF-κB signaling pathways, exhibiting significant antitumor activity. TM-233 reduces the expression of the anti-apoptotic protein Mcl-1 by inhibiting the phosphorylation of JAK2 and STAT3, and regulates its transcription by directly binding to the Mcl-1 gene promoter. Additionally, TM-233 prevents the translocation of NF-κB from the cytoplasm to the nucleus by inhibiting its DNA-binding activity, thereby reducing nuclear NF-κB expression. TM-233 shows potential in overcoming Bortezomib (HY-10227) resistance and can be applied in research related to multiple myeloma.

Cenisertib (AS-703569) benzoate is an ATP-competitive multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3. Cenisertib benzoate induces major growth-inhibitory effects by blocking the activity of several different molecular targets in neoplastic mast cells (MC). Cenisertib benzoate inhibits tumor growth in xenograft models of pancreatic, breast, colon, ovarian, and lung tumors and leukemia.

Benfluron hydrochloride is an Apoptosis inducer and inhibitor of the HIV-1 Rev-RRE complex, with an IC₅₀ of 5.0 μM against the HIV-1 Rev-RRE complex. Benfluron hydrochloride induces p53 activation, and triggers phosphorylation of Chk1 at serine 345, Chk2 at threonine 68, as well as ERK1/2 at threonine 202 and tyrosine 204. Benfluron hydrochloride activates Caspase 8, Caspase 9 and Caspase 3/7, inhibits HIV-1 viral transcription, and acts as a substrate for 11β-HSD 1 and cytosolic carbonyl reductase. Benfluron hydrochloride can be used in research related to leukemia and HIV-1 infection.