Stem Cells

Y-27632 dihydrochloride (Y-27632 2HCl) is an orally potent, ATP-competitive inhibitor of ROCK-I and ROCK-II. Y-27632 dihydrochloride also inhibits isolation-induced apoptosis in mouse prostate stem or progenitor cells.

CHIR-99021 (CT99021) is an activator of the Wnt/β-catenin signaling pathway and a GSK-3α/β inhibitor (IC50=10/6.7 nM) with selective and oral activity.CHIR-99021 induces cellular autophagy, which enhances self-renewal in mouse and human embryonic stem cells.

Y-27632 (Y-27632) is an orally potent, ATP-competitive inhibitor of ROCK-I and ROCK-II. Y-27632 also inhibits isolation-induced apoptosis in mouse prostate stem or progenitor cells.

SB-431542 is an inhibitor of ALK5 TGF-β type I Receptor (IC50=94 nM) and is selective. SB 431542 also has inhibitory activity against ALK4 and ALK7 but not other proteins. SB 431542 can be used for induced differentiation of stem cells.

Diclofenac Potassium (CGP-45840B) is a nonsteroidal anti-inflammatory drug taken to reduce inflammation and as an analgesic reducing pain in certain conditions.

SB 202190 (FHPI) is a p38 MAPK inhibitor that inhibits p38α and p38β2 (IC50=50/100 nM) selectively and cell-permeably. SB 202190 has antitumor activity and also induces the differentiation of human embryonic stem cells into cardiomyocytes.

Benzyl butyl phthalate (1,2-benzenedicarboxylic acid) is used as a plasticizer for PVC.

Estradiol (E2) is a naturally occurring steroidal sex hormone that is essential for female fertility and maintenance of secondary sexual characteristics. Estradiol upregulates IL-6 expression through estrogen receptor beta (ERβ).

BPDA2 is a selective and potent SHP2 inhibitor with IC50 values of 92.0 nM, 33.39 μM, and 40.71 μM for SHP2, SHP1, and SHP1B, respectively.DBDA2 possesses anticancer and antitumor activity and inhibits anchorage-independent growth of breast cancer cells and cancer stem cell properties in a concentration-dependent manner.BPDA2 can be used to study of breast cancer.

Octapeptide-2 Acetate, as a hair growth promotion active, is a double-layered encapsulated biomimetic peptide that helps increase cell growth and migration. It promotes hair growth by activating the stem cells of the hair follicles. Octapeptide-2 is more stable and prolongs action than native proteins.

Acetyl Ser-Asp-Lys-Pro is formed in bone marrow cells by enzymatic processing of thymosin β4. It inhibits the entry of pluripotent hemopoietic stem cells into S-phase of the cell cycle and protects against Ara-C lethality in mice.

BMS-214662 is a potent and selective farnesyl transferase inhibitor that induces mitochondrial apoptosis in primitive CD34+ chronic myeloid leukemia (CML) stem cells/progenitors, and has the ability to selectively target CML stem cells/progenitors with antitumor activity.

Stemazole is a novel small molecule human stem progenitor cell proliferation activator that promotes the survival of human embryonic stem cells and maintains stemness, and promotes the survival of oligodendrocyte precursor cells in vitro. Stemazole significantly increased cell survival and clone formation in a dose-dependent manner, reduced apoptosis, and promoted recovery of motor dysfunction and myelin repair. Stemazole can be used as a therapeutic agent in demyelinating disorders, promoting OPC survival in vitro and regeneration in vivo.

DJ001 is a highly specific, selective and non-competitive protein tyrosine phosphatase σ (PTPσ) inhibitor with IC50 of 1.43 μM. DJ001 promotes the regeneration of hematopoietic stem cells.

GSK-3484862 is a non-covalent Dnmt1 inhibitor. It induces DNA hypomethylation to against cancer.

1. Poncirin (Isosakuranetin-7-neohesperidoside) shows a significant in vitro inhibitory effect on the growth of the human gastric cancer cells, SGC-791, in a dose-dependent manner. 2. Poncirin prevents adipogenesis, enhances osteoblast differentiation in mesenchymal stem cellsincreased bone mineral density, and improves trabecular microarchitecture likely reflect increases bone formation and decreases bone resorption in GIO mice.

Xanthosine (9-Beta-D-Ribofuranosylxanthine) is a xanthine nucleoside that increases the number of mammary stem cells and milk production in goats and cattle.

CHIR-99021 HCl (Laduviglusib HCl) is a highly potent and selective inhibitor of GSK-3α β, with IC50 values of 10 nM and 6.7 nM respectively. It demonstrates remarkable selectivity for GSK-3, with over 500-fold selectivity over CDC2, ERK2, and other protein kinases. Additionally, CHIR-99021 HCl serves as a robust activator of the Wnt β-catenin signaling pathway. Moreover, it exhibits the ability to enhance self-renewal in both mouse and human embryonic stem cells. Furthermore, CHIR-99021 HCl induces autophagy [1] [2] [3].

Pifithrin-β hydrobromide (Cyclic PFT-α) is an inhibitor of p53; reversibly blocks p53-dependent transcriptional activation and apoptosis. Protects against neuronal death in models of stroke and neurodegenerative disorders. Active in vivo; protects mice from the side-effects of Y therapy associated with p53 induction. Supresses self-renewal of embryonic stem cells. Also aryl hydrocarbon receptor (AHR) agonist, causes upregulation of AHR target gene CYP1A1 (EC50 = 1.1 μM).

1. Pristimerin (Celastrol methyl ester) has anticancer activity , treatment with Pristimerin may be a potential strategy for the suppression of hypoxia-induced metastasis through the reversal of hypoxia-induced stem cell characteristics and EMT in cancer cells. 2. Pristimerin down-regulates the expression of pro-inflammatory mediators through blocking of NF-κB activation by inhibiting interconnected ROS IKK NF-κB signaling pathways, can effectively inhibit both arthritic inflammation and cartilage and bone damage in the joints.

Plerixafor (AMD-3329), a chemokine receptor antagonist, blocks the binding of stromal cell-derived factor (SDF-1alpha) to the cellular receptor CXCR4.

Bestatin (Ubenimex) competitively inhibits many aminopeptidases, including B, N and leucine aminopeptidases. Ubenimex is a microbial metabolite and dipeptide with potential immunomodulatory and antitumor activities. Aminopeptidases has been implicated in the process of cell adhesion and invasion of tumor cells. Therefore, inhibiting aminopeptidases may partially attribute to the antitumor effect of ubenimex. This agent also activates T lymphocyte, macrophage, and bone marrow stem cell as well as stimulates the release of interleukin-1 and -2, thus further enhances its antitumor activity.

7,4'-Dihydroxy-8-methylflavan can significantly promote mesenchymal stem cells (MSCs) osteogenic differentiation by increasing the levels of alkaline phosphatase (ALP) activity. 7,4'-Dihydroxy-8-methylflavan also has free radical scavenging properties.

Zymosan A, derived from Saccharomyces cerevisiae, is a TLR2 agonist and exhibits significant radioprotective effects, mitigating and preventing IR-induced intestinal injury in mice. Furthermore, Zymosan A aids in the regeneration of intestinal stem cells (ISCs) following IR injury [1].

CAY10736 is an anticancer compound.1 It inhibits proliferation in a panel of melanoma and breast, pancreatic, and lung cancer cell lines (IC50s = 0.827-9.89 μM). CAY10736 inhibits migration and epithelial-to-mesenchymal transition (EMT) of A375 and B16/F10 melanoma cells in vitro in a concentration-dependent manner. It reduces the viability of spheroid A375 and B16/F10 cells (IC50s = 2.4 and 1.59 μM, respectively) and increases the production of reactive oxygen species (ROS) in these cells in a concentration-dependent manner. CAY10736 (5 mg/kg) reduces tumor growth in B16/F10 melanoma and Lewis lung carcinoma mouse models and an A375 mouse xenograft model.References1. Liu, X., Li, B., Zhang, Z., et al. Synthesis and discovery novel anti-cancer stem cells compounds derived from the natural triterpenoic acids. J. Med. Chem. 61(23), 10814-10833 (2018). CAY10736 is an anticancer compound.1 It inhibits proliferation in a panel of melanoma and breast, pancreatic, and lung cancer cell lines (IC50s = 0.827-9.89 μM). CAY10736 inhibits migration and epithelial-to-mesenchymal transition (EMT) of A375 and B16/F10 melanoma cells in vitro in a concentration-dependent manner. It reduces the viability of spheroid A375 and B16/F10 cells (IC50s = 2.4 and 1.59 μM, respectively) and increases the production of reactive oxygen species (ROS) in these cells in a concentration-dependent manner. CAY10736 (5 mg/kg) reduces tumor growth in B16/F10 melanoma and Lewis lung carcinoma mouse models and an A375 mouse xenograft model. References1. Liu, X., Li, B., Zhang, Z., et al. Synthesis and discovery novel anti-cancer stem cells compounds derived from the natural triterpenoic acids. J. Med. Chem. 61(23), 10814-10833 (2018).

Eciskafusp alfa, a cis-targeted IL2v immunocytokine, acts on programmed cell death 1 (PDCD1, commonly known as PD-1), preferentially targeting antigen-specific stem-like PD-1+ TCF-1+ CD8+ T cells to differentiate into a more effective effector population. This compound is applicable in the study of cancer and chronic infections [1].

Glomeratide A, a benzophenone C-glucoside, exhibits hepatoprotective properties and safeguards rat liver epithelial stem-like cells from d-galactosamine-induced hepatotoxicity.

ML239 (CID-49843203) is a potent and selective inhibitor of breast cancer stem cells, with an IC50 of 1.16 μM.

13C15-Nivalenol is intended for use as an internal standard for the quantification of nivalenol by GC- or LC-MS. Nivalenol is a trichothecene mycotoxin that has been found inFusarium.1It is lethal to mice (LD50= 6.9 mg/kg).2Nivalenol (5, 10, and 15 mg/kg) also induces thymic, splenic, and Peyer's patch cell apoptosis in mice.3 1.Yang, Z., Concannon, J., Ng, K.S., et al.Tetrandrine identified in a small molecule screen to activate mesenchymal stem cells for enhanced immunomodulationSci. Rep.630263(2016) 2.Yoshizawa, T., and Morooka, N.Studies on the toxic substances in the infected cereals (part 3): Acute toxicities of new trichothecene mycotoxins: Deoxynivalenol and its monoacetateJ. Food Hyg.15(4)261-269(1974) 3.Poapolathep, A., Ohtsuka, R., Kiatipattanasakul, W., et al.Nivalenol-induced apoptosis in thymus, spleen and Peyer's patches of miceExp. Toxicol. Pathol.53(6)441-446(2002)

Glycinol enhances osteogenic differentiation and attenuates the effects of age on mesenchymal stem cells, it could as a potential preventive or treatment for osteoporosis. Glycinol also has antidiuretic activity.

Friedelin-3,4-lactone has a promotion effect on the inducing proliferation of rat mesenchymal stem cells(rMSCs).

BOP is anantagonist of alpha4beta1/alpha9beta1 integrins. BOP rapidly mobilizes long-term multi-lineage reconstituting hematopoietic stem cells (HSC).

Ganglioside GD3 is synthesized by the addition of two sialic acid residues to lactosylceramide and can serve as a precursor to the formation of more complex gangliosides by the action of glycosyl- and sialyltransferases. It induces apoptosis in HuT-78 cutaneous T cell lymphoma cells in a concentration-dependent manner and disrupts the mitochondrial membrane potential when used at a concentration of 200 μM. Expression of ganglioside GD3 in GD3-negative SK-MEL-28-N1 malignant melanoma cells increases both cell proliferation and invasion in vitro. Ganglioside GD3-deficient adult mice exhibit progressive loss of the neural stem cell (NSC) pool and impaired neurogenesis. Ganglioside GD3 mixture contains ganglioside GD3 molecular species with C18:1 and C20:1 sphingoid backbones.

Cyclo(RGDfK(Mal)), a pentapeptide, enhances the attachment and infiltration of human pluripotent stem cells and is utilized in three-dimensional stem cell culture and expansion [1].

BODIPY-aminoacetaldehyde diethyl acetal (BAAA-DA) is a stable precursor to BODIPY-aminoacetaldehyde, a cell-permeable fluorescent substrate for aldehyde dehydrogenase (ALDH).1,2BODIPY-aminoacetaldehyde diethyl acetal is converted under acidic conditions to BODIPY-aminoacetaldehyde (BAAA).2BAAA is cell-permeant and is converted intracellularly by ALDH to BODIPY aminoacetate (BAA), which is retained by cells and can be used to identify cells with high ALDH activity.1BAA is a substrate for the efflux pump P-glycoprotein (P-gp) but co-application of BAAA with a P-gp inhibitor, such as verapamil , inhibits BAA efflux.2BAAA-DA has been used to isolate human hematopoietic progenitor cells, which have high ALDH activity, andviaflow cytometry to sort cancer stem cells that contain high levels of ALDH.1,3BAA used in cells can be excited at 488 nm and displays an emission maximum of 512 nm.4 1.Storms, R.W., Trujillo, A.P., Springer, J.B., et al.Isolation of primitive human hematopoietic progenitors on the basis of aldehyde dehydrogenase activityProceedings of the National Academy of Sciences of the United States of America96(16)9118-9123(1999) 2.Smith, C.A., Colvin, M., Storms, R.W., et al.BODIPY aminoacetaldehyde diethyl acetal08010501.81-15(2010) 3.Leng, Z., Yang, Z., Li, L., et al.A reliable method for the sorting and identification of ALDHhigh cancer stem cells by flow cytometryExp. Ther. Med.(2017) 4.Pomper, M.G., Wang, H., Minn, I., et al.Red fluorescent aldehyde dehydrogenase (ALDH) substrate(2015)

NCT-58 is a potent C-terminal HSP90 inhibitor. NCT-58 does not induce the heat shock response (HSR). NCT-58 elicits anti-tumor activity via the simultaneous downregulation of HER family members as well as inhibition of Akt phosphorylation. NCT-58 kills Trastuzumab-resistant breast cancer stem-like cells. NCT-58 induces apoptosis in HER2-positive breast cancer cells.

Cardiogenol C hydrochloride (Cardiogenol C) can induces the differentiation of ESCs into cardiomyocytes (EC50= 100 nM).

GSK-690 is a selective and potent inhibitor of lysine demethylase 1 (LSD 1), which induces differentiation of leukemic stem cells in acute myeloid leukemia (AML), and can be used in the study of leukemias.

THI0019 is a highly potent agonist of the integrin α4β1 (VLA-4) receptor, with an EC 50 range of 1-2 μM. It effectively promotes the adhesion of stem/progenitor cells. Furthermore, THI0019 successfully modulates adhesion processes mediated by α4β7, α5β1, and αLβ2 integrins.

Elsinochrome A is a perylenequinone fungal metabolite that has been found inHypomycesand has anticancer activity.1Photoactivation of elsinochrome A induces the production of singlet oxygen and apoptosis in R366.4 rhesus monkey embryonic stem cells and HCe-8693 colorectal carcinoma cells when used at concentrations ranging from 1 to 100 μM. 1.Ma, L., Tai, H., Li, C., et al.Photodynamic inhibitory effects of three perylenequinones on human colorectal carcinoma cell line and primate embryonic stem cell lineWorld J. Gastroenterol.9(3)485-490(2003)

Cusatuzumab, a human αCD70 monoclonal antibody, exhibits cytotoxic activity and enhances antibody-dependent cellular cytotoxicity. It reduces leukemia stem cells (LSCs), triggers gene signatures associated with myeloid differentiation and apoptosis, and holds potential for Acute myeloid leukemia (AML) research [1].

VUT-MK142 is a new cardiomyogenic small molecule promoting the differentiation of pre-cardiac mesoderm into cardiomyocytes,which may be useful to differentiate stem cells into cardiomyocytes for cardiac repair.

YB-0158 (Wnt pathway inhibitor 2) is a powerful peptidomimetic compound that effectively targets colorectal cancer stem cells (CSCs) by disrupting the interaction between Sam68 and Src proteins. This compound acts as a reverse-turn agent, inducing apoptosis in CRC cells and displaying strong anti-cancer activities.

Goralatide, isolated from fetal calf bone marrow, exerts a high inhibitory activity on the proliferation of hematopoietic pluripotent stem cells.

FL118 is a novel survivin inhibitor that inhibits cancer stem cell-like properties.FL118 is a novel camptothecin analog with anticancer activity that inhibits epithelial-mesenchymal transition through the Wnt/β-catenin signaling pathway, thereby inhibiting migration and invasion of human breast cancer cells.

ADAM-17 (TACE) and MMP inhibitor (Ki = 120 nM at ADAM-17). Sensitizes cancer stem cells to the lethal effects of 5-FU in vitro. Blocks shedding of TNF-α from cell membranes.

NBD-LLLLpY is a peptide synthesized enzymatically within the nucleus to selectively target and eliminate human induced pluripotent stem cells (hiPSCs).

RIPGBM is a selective inducer of apoptosis in glioblastoma multiforme cancer stem cells (EC50: ≤500 nM).

EPI-X4, an endogenous peptide fragment of human serum albumin (amino acids 408-423), serves as an antagonist to the chemokine (C-X-C motif) receptor 4 (CXCR4). It effectively prevents calcium mobilization and receptor internalization triggered by chemokine (C-X-C motif) ligand 12 (CXCL12) in HEK293 cells with CXCR4 expression, at concentrations between 0.8 and 1,000 µM. Moreover, EPI-X4 hampers the CXCL12-driven migration of both Jurkat T cells and human CD34+ hematopoietic stem cells. In an acute allergic airway hypereosinophilia mouse model, EPI-X4 intrinsically decreases Cxcr4-dependent inflammatory cell infiltration in airways at a dose of 16 µmol/kg. Additionally, increased urinary EPI-X4 levels, inversely related to glomerular filtration rate (GFR), are observed in chronic kidney disease patients, indicating its potential biomarker role.

TWS-119 is an inhibitor of glycogen synthase kinase-3β (GSK-3β) that induces neuronal differentiation in pluripotent murine embryonal carcinoma cells and embryonic stem cells (ESCs).

Nivalenol is a fungal metabolite produced by Fusarium graminearum. Nivalenol induces cell death through caspase and intrinsic apoptotic pathways thus affecting the immune system and causing emesis, growth retardation, and reproductive disorders.