Stem Cells/Wnt

KY02111 is a potent and selective Wnt signaling pathway inhibitor discovered by a cell-based screening, which promotes differentiation of hESCs/iPSCs to cardiomyocytes when used at the second stage of differenitation.

TBB is a highly selective, ATP/GTP-competitive inhibitor of casein kinase-2 (CK2)with IC50s of 0.9 and 1.6 uM for rat liver and human recombinant CK2 respectively).

FH535 is an inhibitor of Wnt/β-catenin and PPAR, with anti-tumor activities.

BMS 299897 is an orally active, potent γ-secretase inhibitor (IC50 = 12 nM). Inhibits Aβ40 and Aβ42 formation in vitro (IC50 values are 7.4 and 7.9 nM respectively) and reduces Aβ in the brain, plasma and cerebrospinal fluid in vivo.

AR-A 014418 is a selective glycogen synthase kinase 3 (GSK-3) inhibitor (IC50 = 104 nM). Exhibits specificity for GSK-3 over cdk2 and cdk5 (IC50 values are > 100 μM) and over 26 other kinases. Inhibits β-amyloid-mediated neurodegeneration in hippocampal slices.

Valproic acid is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2; Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches.

SB202190 is a highly selective, potent and cell-permeable inhibitor of p38 MAP kinase.

LY294002 is a PI3k inhibitor (cell IC50 about 10 μM) and a casein kinase II inhibitor.

Trichostatin A (TSA) inhibits the HDACs 1, 3, 4, 6 and 10 with IC50 values around 20 nM.

XAV 939 is a TNKS inhibitor (IC50 values are 0.011 and 0.004 μM for TNKS1 and TNKS2 respectively).

Dorsomorphin, also known as BML-275, is a selective small molecule inhibitor of BMP signaling, which promotes cardiomyogenesis in embryonic stem cells. Dorsomorphin reverses the mesenchymal phenotype of breast cancer initiating cells by inhibition of bone morphogenetic protein signaling.

LY-411575 is a selective, cell permeable, small molecule gamma secretase inhibitor.

CIL56 (CA3) is a potent inhibitor of YAP1/TEAD transcriptional activity, selectively targeting YAP1-high, therapy-resistant esophageal adenocarcinoma cells with cancer stem cell (CSC) characteristics. It induces ferroptosis through iron-dependent reactive oxygen species (ROS) generation, offering a novel approach for overcoming resistance in aggressive tumors.

RO4929097 is an orally bioavailable, small-molecule gamma secretase (GS) inhibitor with an IC50 of 4 nM.

ICG-001 is a specific inhibitor of Wnt/β-catenin signaling pathway that inhibits β-catenin/cyclic AMP response element-binding (CREB) protein transcription (IC50=3 microM) .

BC2059 is an orally bioavailable and potent beta-catenin inhibitor.

RepSox (SJN 2511) is a selective inhibitor of the TGF-β type I receptor ALK5 (IC50 values are 0.004 and 0.023 μM for ALK5 autophosphorylation and ALK5 binding respectively).

Kenpaullone is a potent inhibitor of CDK inhibitor (IC₅₀ values are 0.4, 0.68, 7.5, 0.85 µM for CDK1/cyclinB, CDK2/cyclinA, CDK2/cyclinE and CDK5/p25 respectively). Also inhibits GSK-3β and LCK (IC₅₀ values are 0.23 and 0.47 µM respectively) Displays reduced activity for other kinases (IC₅₀ values are 15, 20, 20, 9 µM for c-src, casein kinase 2, ERK1 and ERK2 respectively). Also Generates iPSCs. Displays antiproliferative properties.

Wnt-C59 is a very potent and highly selective Wnt signaling antagonist with an IC50 ~ 74 pM in the Wnt signaling reporter assay.

LDN193189 is a highly potent small molecule BMP inhibitor that inhibits BMP type I receptors ALK2 (IC50: 5 nM), ALK3 (IC50: 30 nM) and ALK6 (TGFβ1/BMP signaling) and subsequent SMAD phosphorylation.

SB 431542 is a potent and specific inhibitor of transforming growth factor-β superfamily type I ALK receptors ALK4, ALK5, and ALK7 .

CX-4945 is a potent and selective orally bioavailable small molecule inhibitor of CK2 that inhibits human umbilical vein endothelial cell migration, tube formation, and blocks CK2-dependent hypoxia-induced factor 1 alpha (HIF-1α) transcription in cancer cells.

Verteporfin is a small molecule that inhibits TEAD, YAP association and YAP-induced liver overgrowth. It is also a potent second-generation photosensitizing agent derived from porphyrin.

SB 203580 is a specific inhibitor of p38α and p38β which suppresses downstream activation of MAPKAP kinase-2 and heat shock protein 27.

Azacitidine is a chemical analogue of the cytosine nucleoside used in DNA and RNA that is mainly used in the treatment of myelodysplastic syndrome (MDS).

CHIR99021 is an aminopyrimidine derivative that inhibits GSK3α and GSK3β with IC50 values of 10 and 6.7 nM, respectively.

Y-27632 is an ATP-competitive inhibitor of ROCK-I and ROCK-II, with Ki of 220 nM and 300 nM for ROCK-I and ROCK-II, respectively.

AZD1080 is a novel GSK3 inhibitor, rescues synaptic plasticity deficits in rodent brain and exhibits peripheral target engagement in humans.

FLI-06 is a Notch inhibitor and the early secretory pathway inhibitor. FLI-06 disrupts the Golgi apparatus in a manner distinct from that of brefeldin A and golgicide A.

DMH-1 is a selective inhibitor of the bone morphogenic protein (BMP) ALK2 receptor (IC50 = 108 nM).

DAPT (GSI-IX) is an inhibitor of γ-secretase that causes a reduction in Aβ40 and Aβ42 levels in human primary neuronal cultures with IC50 values of 115 and 200 nM for total Aβ and Aβ42 respectively.

LGK974 is a highly potent, selective and orally bioavailable Porcupine inhibitor (Wnt signaling antagonist) with an IC50 <1 nM in the Wnt signaling reporter assay and Porcupine binding assay.

Tideglusib is a GSK-3 inhibitor currently in phase II clinical trials for the treatment of Alzheimer disease and progressive supranuclear palsy

XMU-MP-1 is a reversible and selective MST1/2 inhibitor with IC50 values of 71.1??12.9 nM and 38.1 ?? 6.9 nM against MST1 and MST2, respectively.

YO-01027 is a dipeptidic γ-secretase inhibitor, an antiAlzheimer agent.

Wortmannin is a potent, selective, cell-permeable and irreversible inhibitor of phosphatidylinositol 3-kinase (PI 3-kinase) (IC50 = 2 - 4 nM) which also potently inhibits polo-like kinase 1 (PLK1) (IC50 = 5.8 nM).

JW74 is an efficient and specific inhibitor of the canonical Wnt signaling. JW74 shows a reduction of canonical Wnt signaling in the ST-Luc assay with IC50 values of 790 nM.

MK-2206 2HCl is a highly selective inhibitor of Akt1/2/3 with IC50 of 8 nM/12 nM/65 nM, respectively.

Semagacestat (LY450139) is a γ-secretase blocker for Aβ42, Aβ40 and Aβ38 with IC50 of 10.9 nM, 12.1 nM and 12.0 nM, respectively. Semagacestat also inhibits Notch signaling with IC50 of 14.1 nM.

Y-27632 is a Rho-Associated Coil Kinase (ROCK) inhibitor that increases the cloning efficiency of human embryonic stem cells (hESCs).

BML-275 is a cell-permeable pyrazolopyrimidine compound shown to be an AMP-activated protein kinase (AMPK) and fatty acid synthase inhibitor.

IWR-1-endo is a potent inhibitor of the Wnt response, blocking a cell-based Wnt/β-catenin pathway reporter response with an IC50 value of 180 nM. Wnt proteins bind to receptors on the cell surface, initiating a signaling cascade that leads to β-catenin activation of gene transcription.

LY2090314 is a potent inhibitor of glycogen synthase kinase-3 (GSK-3) which plays an important role in many pathways, including initiation of protein synthesis, cell proliferation, cell differentiation, and apoptosis.

A83-01 is a selective inhibitor of the transforming growth factor-beta type I receptor ALK5, the Nodal receptor ALK4, and the nodal receptor ALK7

Manzamine A is a selective inhibitor of glycogen synthase kinase 3 beta (GSK-3β) and cyclin-dependent kinase 5 (CDK-5), with respective IC50 values of 10.2 μM and 1.5 μM. This compound exhibits significant biological activity, including antimalarial and anticancer effects, and has been shown to inhibit autophagy in pancreatic cancer cells by targeting vacuolar ATPases. Additionally, Manzamine A demonstrates potent antiviral properties against herpes simplex virus type 1 (HSV-1), making it a valuable reagent for diverse research applications in cancer, autophagy, and virology studies.

Manzamine A hydrochloride is an orally active beta-carboline alkaloid that specifically inhibits GSK-3β and CDK-5, with IC50 values of 10.2 μM and 1.5 μM, respectively. This compound demonstrates significant antimalarial and anticancer properties, with additional effects such as inhibiting vacuolar ATPases and autophagy processes in pancreatic cancer cells. Furthermore, Manzamine A hydrochloride exhibits potent activity against HSV-1, making it valuable for various research applications in cancer biology and virology.

Protein kinase G inhibitor-1 is a selective inhibitor targeting protein kinase G (PKG) with an IC50 of 0.9 μM. This compound is utilized primarily in research related to mycobacterial infections, providing insights into the mechanisms of pathogenesis and potential therapeutic approaches. Its efficacy in inhibiting PKG activity makes it a valuable tool for exploring mycobacterial biology and developing novel treatments.

WNT7A-IN-1 sodium is a selective inhibitor of WNT7A that disrupts the interaction between WNT7A and its receptor FZD5, leading to enhanced expression of MHC-I. This reagent is known to significantly increase levels of MHC-I and phosphorylated p65 while decreasing active β-catenin expression. Additionally, WNT7A-IN-1 sodium acts as a photosensitizer in the green spectral region, making it suitable for applications in photodynamic therapy and immunological studies.

Hedgehog IN-9 is a potent Hedgehog inhibitor that primarily targets the inhibition of GLI1 expression. It has been shown to enhance BRD2 protein levels in cells and effectively inhibit the growth of medulloblastoma spheroid cells. Additionally, Hedgehog IN-9 can be utilized for the synthesis of photoaffinity labeling probes, making it a valuable tool in cancer research and related biochemical applications.

Indirubin-3′-oxime (IDR3O) is a synthetic derivative of indirubin that functions as a potent inhibitor of cyclin-dependent kinases (CDKs), glycogen synthase kinase 3β (GSK3β), and all three isoforms of c-Jun N-terminal kinases (JNK1, JNK2, JNK3). It demonstrates inhibitory activity with IC50 values of 0.8 μM, 1.4 μM, and 1.0 μM for each JNK isoform, respectively. Indirubin-3′-oxime is also known to promote chondrocyte height growth through the activation of Wnt/β-catenin signaling, making it relevant for studies in cellular growth and differentiation.