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 (1998):

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

HY-147214

GNE-7883	2648450-42-2	99.54%
GNE-7883 is a pan-TEAD inhibitor that blocks the association of YAP/TAZ with TEAD. GNE-7883 effectively reduces chromatin accessibility at TEAD motifs, inhibits cell proliferation in multiple cell line models, and achieves strong anti-tumor efficacy in vivo. In addition, GNE-7883 effectively overcomes intrinsic and acquired resistance to KRAS (Kirsten rat sarcoma viral oncogene homolog) G12C inhibitors in multiple preclinical models by inhibiting YAP/TAZ activation.

HY-16294

LY2090314	603288-22-8	99.85%
LY2090314 is a potent inhibitor of glycogen synthase kinase-3 (GSK-3) with IC₅₀ values of 1.5 nM and 0.9 nM for GSK-3α and GSK-3β, respectively.

HY-13867

Bisindolylmaleimide I	133052-90-1	98.15%
Bisindolylmaleimide I (GF109203X) is a cell-permeable and reversible PKC inhibitor (IC₅₀ of 20 nM, 17 nM, 16 nM, and 20 nM for PKCα, PKCβI, PKCβII, and PKCγ. Bisindolylmaleimide I is also a GSK-3 inhibitor.

HY-10074

TPCA-1	507475-17-4	99.66%
TPCA-1 is a potent and selective inhibitor of IKK-2 with IC₅₀ of 17.9 nM. TPCA-1 is an effective inhibitor of STAT3 phosphorylation, DNA binding, and transactivation.

HY-13257

Thiazovivin	1226056-71-8	99.57%
Thiazovivin is a potent ROCK inhibitor, which can protect human embryonic stem cells. Thiazovivin improves the efficiency of iPSC generation.

HY-B2163

Astaxanthin	472-61-7	≥98.0%
Astaxanthin, the red dietary carotenoid, is an orally effective and potent antioxidant. Astaxanthin inhibits NF-κB and down-regulates VEGF in blood glucose. Astaxanthin exerts anti-cancer cell proliferation, increases apoptosis, impairs migration and invasion by activating PPARγ and reducing the expression of STAT3. Astaxanthin also has neuroprotective and anti-inflammatory activity and can be used in studies of cancer, diabetic retinopathy, cardiovascular disease, and in the coloring of animal feed.

HY-15185

Nirogacestat	1290543-63-3	99.78%
Nirogacestat (PF-3084014) is a reversible, orally bioavailable, noncompetitive, and selective γ-secretase inhibitor with an IC₅₀ of 6.2 nM. Inhibition of Notch signaling by Nirogacestat while minimizing gastrointestinal toxicity presents a promising approach for research of Notch receptor-dependent cancers.

HY-10256A

Adezmapimod hydrochloride	869185-85-3	99.71%
Adezmapimod (SB 203580; RWJ 64809) hydrochloride is a selective and ATP-competitive p38 MAPK inhibitor with IC₅₀s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. Adezmapimod hydrochloride inhibits LCK, GSK3β and PKBα with IC₅₀s of 100-500-fold higher than that for SAPK2a/p38. Adezmapimod hydrochloride does not disrupt JNK activity and is an autophagy and mitophagy activator.

HY-40354A

Tofacitinib citrate	540737-29-9	99.94%
Tofacitinib citrate is an orally available JAK3/2/1 inhibitor with IC₅₀s of 1, 20, and 112 nM, respectively. Tofacitinib citrate has antibacterial, antifungal and antiviral activities.

HY-19696A

Tauroursodeoxycholate sodium	35807-85-3	98.40%
Tauroursodeoxycholate (Tauroursodeoxycholic acid; TUDCA) sodium is an endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits ERK.

HY-138565

K-975	2563855-03-6	99.89%
K-975 is a potent, selective and orally active TEAD inhibitor, with a strong inhibitory effect against protein-protein interactions between YAP1/TAZ and TEAD. K-975 covalently binds to Cys359 located in the palmitate-binding pocket of TEAD via an acrylamide structure. K-975 exhibits antitumor activity on malignant pleural mesothelioma.

HY-N0751

Scutellarin	27740-01-8	99.04%
Scutellarin, an active flavone isolated from Scutellaria baicalensis, can down-regulates the STAT3/Girdin/Akt signaling in HCC cells, and inhibits RANKL-mediated MAPK and NF-κB signaling pathway in osteoclasts. Scutellarin is active against HIV-1IIIB, HIV-1(74V) and HIV-1KM018 with EC₅₀s of 26 μM, 253 μM and 136 μM, respectively.

HY-P1846A

Jagged-1 (188-204) (TFA)		99.89%
Jagged-1 (188-204) TFA is a fragment of the Jagged-1 (JAG-1) protein with Notch agonist activity. JAG-1 is a Notch ligand highly expressed in cultured and primary multiple myeloma (MM) cells. JAG-1 induces maturation of monocyte-derived human dendritic cells.

HY-123986

CTPI-2	68003-38-3	99.95%
CTPI-2 is a third-generation mitochondrial citrate carrier SLC25A1 inhibitor with a K_D of 3.5 μM. CTPI-2 inhibits glycolysis, PPARγ, and its downstream target the glucose transporter GLUT4. CTPI-2 halts salient alterations of NASH reverting steatosis, preventing the evolution to steatohepatitis, reducing inflammatory macrophage infiltration in the liver and adipose tissue, and starkly mitigating obesity induced by a high-fat diet. Antitumor activity.

HY-10182A

Laduviglusib monohydrochloride	1797989-42-4	99.93%
Laduviglusib (CHIR-99021) monohydrochloride is a potent and selective GSK-3α/β inhibitor with IC₅₀s of 10 nM and 6.7 nM. Laduviglusib monohydrochloride shows >500-fold selectivity for GSK-3 over CDC2, ERK2 and other protein kinases. Laduviglusib monohydrochloride is also a potent Wnt/β-catenin signaling pathway activator. Laduviglusib monohydrochloride enhances mouse and human embryonic stem cells self-renewal. Laduviglusib monohydrochloride induces autophagy.

HY-N0174

Cryptotanshinone	35825-57-1	98.80%
Cryptotanshinone is a natural compound extracted from the root of Salvia miltiorrhiza Bunge that shows antitumor activities. Cryptotanshinone inhibits STAT3 with an IC₅₀ of 4.6 μM.

HY-13919

Napabucasin	83280-65-3	99.94%
Napabucasin (BBI608) is a STAT3 inhibitor which blocks stem cell activity in cancer cells.

HY-108470

Ro5-3335	30195-30-3	99.52%
Ro5-3335, a benzodiazepine, acts as an inhibitor of core binding factor (CBF) leukemia. Ro5-3335 is a RUNX1-CBFβ interaction inhibitor that represses RUNX1/CBFB-dependent transactivation.

HY-N0439

Asiaticoside	16830-15-2	99.84%
Asiaticoside, a trisaccaride triterpene from Centella asiatica, suppresses TGF-β/Smad signaling through inducing Smad7 and inhibiting TGF-βRI and TGF-βRII in keloid fibroblasts; Asiaticoside shows antioxidant, anti-inflammatory, and anti-ulcer properties.

HY-15312

WP1066	857064-38-1	99.77%
WP1066 is an inhibitor of JAK2 and STAT3, and also shows effect on STAT5 and ERK1/2, without affecting JAK1 and JAK3.

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