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

MBP146-78 is a potent and selective inhibitor of cGMP dependent protein kinases.

IWP-2 is an inactivator of Porcn function and inhibitor of Wnt production, and blocks beta-catenin accumulation. Wnt/b-catenin ('canonical') pathway maintains transcriptional programs that enable stem cells to remain multipotent.

PF-5274857 is a novel Smo antagonist that specifically binds to Smo with a K(i) of 4.6 ?? 1.1 nmol/L and completely blocks the transcriptional activity of the downstream gene Gli1 with an IC(50) of 2.7 ?? 1.4 nmol/L in cells.

Forskolin is a cell-permeable diterpenoid that possesses anti-hypertensive, positive inotropic, and adenylyl cyclase activating properties.

Hh-Ag1.5 is one of the most potent and selective small-molecule agonists of the Hedgehog pathway, targeting Smoothened (Smo) with an EC50 ~1 nM.

JK184 is potent downstream hedgehog (Hh) signaling inhibitor that prevents Gli-dependent transcriptional activity (IC50 = 30 nM).