Cancer Stem Cells

Cancer stem cells (CSCs) are populations of cancer cells that have the properties of stem cells i.e. self-renewal and ability to generate differentiated progenies. CSCs have high plasticity, which changes their phenotypic and functional appearance. They have important roles in tumor development, expansion, resistance, relapse and metastasis. Multiple studies have shown that CSCs originate from non-malignant stem or progenitor cells. Inhibition of developmental signaling pathways that are critical for stem and progenitor cell homeostasis and function has important implications in strategies to target CSCs in cancer research.

Studies have shown that CSCs develop several mechanisms to protect themselves from toxins and genotoxic stress, including enhanced DNA damage repair capacity, increased expression of drug transporters, maintenance of a low reactive oxygen species (ROS) environment, and recruitment of a protective niche. Therefore, targeting signaling pathways that are required to maintain stem cells is the current therapeutic strategy for CSCs. For example, hedgehog pathway, Notch and Wnt signaling pathways.

Newly developed drugs targeting surface markers of CSCs opens the new avenues for cancer therapy, such as CD44, CD133, EpCAM, Sox2, and Oct-3/4.

Cancer Stem Cells Related Products (2046):

Cat. No.	Product Name	CAS No.	Purity	Chemical Structure

HY-15108G

Purmorphamine (GMP)	483367-10-8
Purmorphamine (GMP) is Purmorphamine (HY-15108) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Purmorphamine is a smoothened/Smo receptor agonist with an EC₅₀ of 1 μM.

HY-111930

5-Iodo-indirubin-3'-monoxime	331467-03-9	99.50%
5-Iodo-indirubin-3'-monoxime is a potent GSK-3β, CDK5/P25 and CDK1/cyclin B inhibitor, competing with ATP for binding to the catalytic site of the kinase, with IC₅₀s of 9, 20 and 25 nM, respectively.

HY-B0497S1

Niclosamide-¹³C₆	1325808-64-7	≥99.0%
Niclosamide-¹³C₆ is the ¹³C₆ labeled Niclosamide. Niclosamide (BAY2353) is an orally bioavailable chlorinated salicylanilide, with anthelmintic and potential antineoplastic activity. Niclosamide (BAY2353) inhibits STAT3 with IC50 of 0.25 μM in HeLa cells and inhibits DNA replication in a cell-free assay.

HY-156095

F7H	897109-93-2	99.42%
F7H is a Frizzled receptor FZD7 antagonist (IC₅₀: 1.25 μM). Frizzled receptors (FZDs) influence Wnt signaling, mediating embryonic development and tissue homeostasis. F7H is a potent ligand for the FZD7 transmembrane domain (TMD).

HY-N2338

Cholesterol myristate	1989-52-2	≥98.0%
Cholesterol myristate is a natural steroid present in traditional Chinese medicine. Cholesterol myristate binds to several ion channels such as the nicotinic acetylcholine receptor, GABAA receptor, and the inward-rectifier potassium ion channel.

HY-107417

Hypothemycin	76958-67-3	≥98.0%
Hypothemycin, a fungal polyketide, is a multikinase inhibitor with K_is of 10/70 nM, 17/38 nM, 90 nM, 900 nM/1.5 μM, and 8.4/2.4 μM for VEGFR2/VEGFR1, MEK1/MEK2, FLT-3, PDGFRβ/PDGFRα, and ERK1/ERK2, respectively.

HY-156450

ERK5-IN-5	2318792-30-0	99.05%
ERK5-IN-5 (compound 4a) is an ERK5 kinase inhibitor with anticancer activity. ERK5-IN-5 exhibits good anti-proliferative activity with the IC₅₀ value of 6.23 µg/mL for A549 cells.

HY-147651

β-catenin-IN-4	2353536-67-9	99.84%
β-catenin-IN-4 (Compound 39) is a β-catenin inhibitor with a K_i of 0.64 μM. β-catenin-IN-4 reduces the protein expression levels of cyclin D1 and c-Myc.

HY-D1474

WNT7A-IN-1 sodium	33628-03-4
WNT7A-IN-1 sodium (1365-0109), a WNT7A inhibitor, disrupts the protein-protein interaction between WNT7A and its receptor FZD5, resulting in the upregulation of MHC-I expression. WNT7A-IN-1 sodium significantly increases the expression of MHC-I and p-p65,while concurrently reducing the expression of active β-catenin. WNT7A-IN-1 sodium (compound F) is also a photographic sensitizer in the green spectral region.

HY-P1985A

Notch 1 TFA
Notch 1 TFA (Notch homolog 1, translocation-associated) can encode a member of the NOTCH family of proteins. Members of this Type I transmembrane protein family share structural characteristics including an extracellular domain consisting of multiple epidermal growth factor-like (EGF) repeats, and an intracellular domain consisting of multiple different domain types.

HY-112465

H-8 dihydrochloride	113276-94-1	99.00%
H-8 (dihydrochloride) is a cell-permeable, reversible and ATP-competitive PKA inhibitor.

HY-116116

Tafetinib	1032265-57-8
Tafetinib (SIM010603) is an oral multi-targets receptor tyrosine kinases inhibitor. Tafetinib inhibitsstem cell factor receptor (Kit),vascular endothelial growth factor receptor-2 (VEGFR-2),platelet-derived growth factor receptor-β (PDGFR-β),glial cell line-derived neurotrophic factor receptor (Rearranged during Transfection; RET), andFms-like tyrosine kinase-3 (FLT3)withIC₅₀values between 5.0 and 68.1 nmol/l. Tafetinib inhibits the phosphorylation ofPDGFR-βandVEGFR-2. Tafetinib inhibits endothelial cell proliferation, endothelial cells chemotaxis, and corneal angiogenesis.

HY-10193A

(1R)-AZD-1480	935666-99-2
(1R)-AZD-1480 is the (1R) chiral isomer of AZD-1480, an ATP competitive JAK1 and JAK2 inhibitor.

HY-N1584C

Halofuginone lactate	82186-71-8	98.32%
Halofuginone lactate, a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a K_i of 18.3 nM. Halofuginone lactate is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity. Halofuginone lactate is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca²⁺ channels. Halofuginone lactate has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects.

HY-100791

NSC23005 sodium	1796596-46-7	99.05%
NSC23005 sodium is a novel and effective p18 inhibitor (ED₅₀=5.21 nM) in promoting Hematopoietic stem cells (HSCs) expansion in both murine and human models.

HY-40354S

Tofacitinib-¹³C₃
Tofacitinib-¹³C₃ is the ¹³C-labeled Tofacitinib. Tofacitinib is an orally available JAK3/2/1 inhibitor with IC50s of 1, 20, and 112 nM, respectively.

HY-106449

Recoflavone	203191-10-0	≥98.0%
Recoflavone (DA-6034 (free acid)), a synthetic derivative of the flavonoid Eupatilin (HY-N0783), is orally active. Recoflavone can inhibit the NF-κB pathway and induce [Ca(²⁺)]_i increase in epithelial cells. Recoflavone exhibits activities such as anti-inflammation, anti-tumor effects, protection of gastric and intestinal mucosa, and promotion of secretion in the ocular surface and salivary glands. Recoflavone can be used for the research of diseases such as dry eye, gastric injury, and intestinal injury.

HY-P1597

Malantide	86555-35-3
Malantide is a synthetic dodecapeptide derived from the site phosphorylated by cAMP-dependent protein kinase (PKA) on the β-subunit of phosphorylase kinase. Malantide is a highly specific substrate for PKA with a K_m of 15 μM and shows protein inhibitor (PKI) inhibition >90% substrate phosphorylation in various rat tissue extracts. Malantide is also an efficient substrate for PKC with a K_m of 16 μM.

HY-N0247

Saikosaponin B1	58558-08-0	99.42%
Saikosaponin B1 is a bioactive constituent of Radix Bupleuri. Saikosaponin B1 is an agonist of the 5-HT_2C receptor with an EC₅₀ of 147.41 μM. Saikosaponin B1 inhibits the Hedgehog (Hh) signaling pathway by targeting the transmembrane protein SMO. Sailosaponin B1 can reduce liver fibrosis. Saikosaponin B1 has anti-cancer activities thus can be studies in research for cancers such as Medulloblastoma (MB).

HY-107594

Benzene hexabromide	1837-91-8	≥98.0%
Benzene hexabromide, a bromohydrocarbon, is a potent inhibitor of JAK2 tyrosine kinase autophosphorylation.

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