Cellules souche et Dérivés

GSK-3β inhibitor20 (compound 3A) is an effective inhibitor of GSK-3β, exhibiting an IC50 value of 74.4 nM.

PF-06648671 is a γ-secretase modulator for the treatment of neurodegenerative and/or neurological disorders.

TEAD-IN-10 (compound 15), a covalent inhibitor, exhibits selective and potent inhibitory activity against TEAD1 (IC 50 =14 nM), TEAD2 (IC 50 =179 nM), and TEAD3 (IC 50 =4 nM). This compound is utilized in cancer research [1].

JAK3-IN-11: potent oral JAK3 inhibitor (IC50=1.7 nM), noncytotoxic, >588-fold selectivity, blocks T-cell growth; useful in autoimmune research.

JAK1-IN-9 (compound 23a) is a potent, selective inhibitor of JAK1, demonstrating an IC50 of 72 nM.

JAK1/TYK2-IN-3, orally active, selectively inhibits TYK2 (IC50: 6 nM), JAK1 (37 nM), JAK2 (140 nM), JAK3 (362 nM), and has anti-inflammatory effects.

JAK2 JH2 binder-1: potent, selective, Ki=37.1 nM, potential for studying myeloproliferative neoplasms.

γ-Secretase modulator 11 hydrochloride is a potent, orally active γ-secretase modulator (IC50: 0.029 μM).

BPN-15606 besylate is a potent oral γ-secretase regulator reducing Aβ42 and Aβ40 with good pharmacokinetics. IC50: 7 nM (Aβ42), 17 nM (Aβ40).

"JAK-IN-23: oral dual JAK/STAT & NF-κB inhibitor; JAK1 (IC50: 8.9 nM), JAK2 (15 nM), JAK3 (46.2 nM); for IBD research."

Ten01 exhibits a 5.0 nM inhibition of JAK1 kinase.

<p>CDD-1431 is a highly selective BMPR2 kinase inhibitor with a Kiapp of 20.6 nM. It inhibits BRE reporter gene activity, exhibiting an IC50 of 4.87 μM. BMPs regulate cellular processes across various tissue types such as the kidneys, skeletal muscle, heart, and reproductive organs, and can induce ectopic bone formation.</p>

Notch inhibitor 1 blocks Notch 1/3 (IC50: 7.8/8.5 nM) and aids cancer research.

CEE321 is an effective pan-JAK inhibitor with an IC50 of 54 nM. It effectively inhibits biomarkers associated with atopic dermatitis.

PF-06263276 selectively inhibits pan-JAK with IC50: JAK1 (2.2 nM), JAK2 (23.1 nM), JAK3 (59.9 nM), TYK2 (29.7 nM).

TGFβ1-IN-1 is a TGF-β1 inhibitor that inhibits the production of TGF-β1-induced fibrosis markers (α-SMA and fibronectin) and can be used in cancer research.

<p>iBFAR2, an inhibitor of BFAR, restores the CD8+ tumor-resident memory T cell subset against solid tumors. It promotes the binding of JAK2-STAT1 and enhances the phosphorylation of STAT1.</p>

JAK-IN-19 inhibits JAK (pIC50: 7.2, 7.7), less so for VEGFR2 (7.0) and Aurora B (5.8).

TEAD-IN-20 is a TEAD inhibitor with IC50 values of 0.021 μM in TEAD4 FRET and 0.044 μM in TEAD4 MCF7-Tead cell lines. It has potential applications in cancer research.

<p>Lirucitinib is a JAK inhibitor known for its anti-inflammatory properties.</p>

TYK2ligand 2 is the TYK2 ligand of PROTACTYD-68. TYD-68 is a highly potent and selective CRBN-recruiting TYK2 PROTAC degrader with a DC50 value of 0.42 nM.

Aβ42-IN-1, compound 1v, is a novel, potent and orally active γ-secretase modulator (GSM).

Tyk2-IN-3 is an inhibitor of Tyk2 pseudokinase (IC50: 485 nM).

AJI-214 functions as a dual-target inhibitor that specifically blocks Aurora kinase A and JAK2. By directly inhibiting Aurora kinase A, AJI-214 prevents mitotic progression and cell polarity in T cells while concurrently suppressing JAK2 activation to reduce STAT3 phosphorylation. This inhibition decreases the differentiation of TH1 and TH17 cells. AJI-214 is utilized in research focused on the modulation of immune responses and the prevention of graft-versus-host disease (GVHD).

PMMB-187, a selective STAT3 inhibitor, exhibits an IC50 of 1.81 μM in MDA-MB-231 cells. This compound induces apoptosis in MDA-MB-231 cells by inhibiting STAT3 transcriptional activity and nuclear translocation, reducing mitochondrial membrane potential, increasing reactive oxygen species (ROS) production, and upregulating the expression of apoptosis-related proteins. PMMB-187 is useful for research in the field of cancer.

CP-352664 is a JAK inhibitor with potency against JAK3, exhibiting an EC50 value of 210 nM. It holds potential for use in research related to organ transplant rejection and autoimmune diseases, such as rheumatoid arthritis.

YLIU-4-105-1 is a type II JAK2 inhibitor. Demonstrating in vivo pharmacological activity, YLIU-4-105-1 reduces splenic weight, decreases blood reticulocyte counts in a dose-dependent manner, and inhibits pSTAT5.

Cenacitinib is an effective inhibitor of Janus kinase (Janus kinase) and possesses anti-inflammatory activity.

Tyk2-IN-20 (Example 289) is an effective inhibitor of Tyk2 with an IC50 value below 5 nM. Additionally, it inhibits JAK1, JAK2, and JAK3 with IC50 values under 100 nM. This compound is utilized for the research of inflammatory diseases.

WZ-2-033 is a potent STAT3 inhibitor. It inhibits proliferation, colony survival, migration, and invasion of MDA-MB-231, HCC70, and MDA-MB231-4175 cells, with IC50 values of 0.7, 1.3, and 1.3 μM respectively.

Casein kinase1δ-IN-13 (compound 401) is an inhibitor of Casein kinase1δ. It is utilized in the research of neurodegenerative diseases.

GDC-9918 (compound GDC-9918) is an inhibitor of Janus kinases.

Kartogenin (KGN) sodium acts as an inducer of chondrogenic tissue formation (EC 50: 100 nM). It promotes chondrogenesis by binding to fibrin A, disrupting its interaction with the transcription factor core binding factor beta subunit (CBFβ), and modulating the CBFβ-RUNX1 transcriptional program. Additionally, Kartogenin sodium aids tendon-bone junction (TBJ) wound healing by stimulating collagen synthesis. It is extensively utilized in cell-free therapies for cartilage regeneration and protection, tendon-bone healing, wound healing, and limb development. The compound is also vital for cartilage repair, coordinating limb development, and osteoarthritis (OA) research [1] [2] [3] [4].

Tyk2-IN-10 acts as an inhibitor of the Tyrosine Kinase 2 (Tyk2)-mediated signaling pathway, which plays a role in inflammation regulation.

<p>Carboxylesterase-IN-3 is a potent inhibitor of Carboxylesterase Notum (IC50 ≤ 10 nM).Carboxylesterase-IN-3 has the potential to study cancer diseases.</p>

TEAD-IN-1 (Compound 2) is an effective inhibitor of TEAD auto-palmitoylation with an IC50 of 603 nM. It enhances the interaction between TEAD and VGLL4, while diminishing the interaction between YAP and TEAD. TEAD-IN-1 is applicable for cancer research.

PF-06442609 is an orally active γ-secretase modulator with an IC50 value of 6 nM for Aβ42. It exhibits good CNS permeability.

Londamocitinib (JAK1-IN-7) is a selective and potent JAK1 inhibitor with anti-inflammatory activity.

JAK3 Covalent Inhibitor-1 is a compound characterized by its potent and selective inhibition of Janus kinase 3 (JAK3), possessing an IC50 of 11 nM and

HDAC6-IN-9 is a γ-secretase modulator that can significantly reduce the level of Aβ42 in mouse brain and can be used to study neurological diseases.

<p>LNK01004 is a JAK inhibitor that exhibits potent inhibitory effects on JAK1 (IC50: 10 nM), JAK2 (IC50: ＜0.51 nM), and TYK2 (IC50: 1.0 nM). It can concurrently inhibit multiple cytokine-induced p-STAT signaling pathways and is applicable for research on diseases such as atopic dermatitis.</p>

MYF-03-176 is an orally active TEAD1/3/4 inhibitor with IC₅₀ values of 47/32/71 nM. inhibits TEAD transcriptional activity and cancer cell growth, antitumour.

<p>Tyk2-IN-15 (Compound 97) is a selective inhibitor of tyrosine kinase 2 (Tyk2) with an IC50 value ≤ 10 nM for Tyk2-JH2. It is utilized in the research of inflammatory and autoimmune diseases [1].</p>

<p>Tyk2-IN-17 (compound 185) effectively inhibits TYK2 [1].</p>

(3S,4R)-Tofacitinib is an less active enantiomer of Tofacitinib. Tofacitinib is a JAK3 inhibitor(IC50 : 1 nM).

<p>Milpecitinib (Compound 21a) is a potent and selective Janus tyrosine kinase (JAK) inhibitor with anti-inflammatory properties. It shows promise for research in cancer and inflammatory diseases.</p>

Tyk2-IN-14, a small molecule inhibitor of TYK2, is significant in treating inflammatory diseases and conditions linked to hypersecretion of IFNa and interferons [1].

STAT3-IN-35 is a STAT3 inhibitor that binds to the SH2 domain. This compound inhibits the phosphorylation of STAT3 and exhibits antiproliferative activity in triple-negative breast cancer (TNBC) cell lines. Additionally, STAT3-IN-35 has demonstrated toxicity and potent antitumor activity in TNBC xenograft models.

DAPM (gamma-Secretase Inhibitor XVI) is a Notch pathway inhibitor with anticancer activity and antiproliferative effects.

(Rac)-SAG, an isoform of SAG, is a potent Smoothened (Smo) receptor agonist (EC₅₀ = 3 nM; Kd = 59 nM) that activates the Hedgehog signaling pathway and counteracts Cyclopamine's inhibition of Smo [1] [2] [3].

JAK1/TYK2-IN-4 serves as a dual inhibitor targeting both JAK and TYK2, displaying IC50 values of 39 nM and 21 nM, respectively. It is also orally bioavailable [1].

YAP/TAZ inhibitor-3 (Compound 24) is a YAP/TAZ inhibitor applicable for relevant research within the life sciences field.

NRX-103095 increases β-catenin binding to SCFβ-TrCP E3 ligase; EC50 is 163 nM for pSer33/Ser37 affinity boost.

Zelasudil (RXC007) is a Rho-related (ROCK) kinase inhibitor for the study of idiopathic pulmonary fibrosis and inflammation.

JDTic, a 4-phenylpiperidine derivative distantly related to analgesics like meperidine and ketobemidone and more closely to the mu opioid antagonist alvimopan, exhibits a notably long duration of action, maintaining effects in animals for weeks following a single dose. This duration is not due to irreversible binding to the kappa opioid receptor but rather to altered activity of c-Jun N-terminal kinases. As a highly selective antagonist for the κ-opioid receptor, without influencing the μ- or δ-opioid receptors, JDTic has shown potential in animal studies for producing antidepressant and anxiolytic effects. It also demonstrates promise in treating addiction to substances such as cocaine and morphine, distinguishing itself structurally from other kappa antagonists like norbinaltorphimine.

TGFβRI-IN-3 inhibits TGFβR1 with an IC 50 of 0.79 nM with 2000-fold selectivity against MAP4K4.

CK2 Inhibitor 2, characterized as a potent, selective, and orally active inhibitor of CK2, demonstrates an impressive IC50 value of 0.66 nM.

Luspatercept (ACE-536), a recombinant modified ActRIIB fusion protein, selectively binds to transforming growth factor β superfamily ligands, thereby enhancing erythrocyte production and advancing the maturation of erythroid precursors. Moreover, by binding with GDF11, it inhibits Smad2/3 signaling. This compound is instrumental in anemia research [1].

(3R,4S)-Tofacitinib, the less active enantiomer of Tofacitinib, is a JAK3 inhibitor with an IC50 of 1 nM.

<p>This ELISA kit uses the Sandwich-ELISA principle. The micro ELISA plate provided in this kit has been pre-coated with an antibody specific to Human S100B. Samples (or Standards) are added to the micro ELISA plate wells and combined with the specific antibody and biotinylated detection antibody specific for Human S100B. Then Avidin-Horseradish Peroxidase (HRP) conjugate are added successively to each micro plate well and incubated. Free components are washed away. The substrate solution is added to each well. Only those wells that contain Human S100B, biotinylated detection antibody and Avidin-HRP conjugate will appear blue in color. The enzyme-substrate reaction is terminated by the addition of stop solution and the color turns yellow. The optical density (OD) is measured spectrophotometrically at a wavelength of 450 nm. The OD value is proportional to the concentration of Human S100B. You can calculate the concentration of Human S100B in the samples by comparing the OD of the samples to the standard curve.</p>

<p>This ELISA kit uses the Sandwich-ELISA principle. The micro ELISA plate provided in this kit has been pre-coated with an antibody specific to Human S100B. Samples (or Standards) are added to the micro ELISA plate wells and combined with the specific antibody and biotinylated detection antibody specific for Human S100B. Then Avidin-Horseradish Peroxidase (HRP) conjugate are added successively to each micro plate well and incubated. Free components are washed away. The substrate solution is added to each well. Only those wells that contain Human S100B, biotinylated detection antibody and Avidin-HRP conjugate will appear blue in color. The enzyme-substrate reaction is terminated by the addition of stop solution and the color turns yellow. The optical density (OD) is measured spectrophotometrically at a wavelength of 450 nm. The OD value is proportional to the concentration of Human S100B. You can calculate the concentration of Human S100B in the samples by comparing the OD of the samples to the standard curve.</p>

<p>This ELISA kit uses the Sandwich-ELISA principle. The micro ELISA plate provided in this kit has been pre-coated with an antibody specific to Rat cTnT/TNNT2. Samples (or Standards) are added to the micro ELISA plate wells and combined with the specific antibody and biotinylated detection antibody specific for Rat cTnT/TNNT2. Then Avidin-Horseradish Peroxidase (HRP) conjugate are added successively to each micro plate well and incubated. Free components are washed away. The substrate solution is added to each well. Only those wells that contain Rat cTnT/TNNT2, biotinylated detection antibody and Avidin-HRP conjugate will appear blue in color. The enzyme-substrate reaction is terminated by the addition of stop solution and the color turns yellow. The optical density (OD) is measured spectrophotometrically at a wavelength of 450 nm. The OD value is proportional to the concentration of Rat cTnT/TNNT2. You can calculate the concentration of Rat cTnT/TNNT2 in the samples by comparing the OD of the samples to the standard curve.</p>

<p>This ELISA kit uses the Sandwich-ELISA principle. The micro ELISA plate provided in this kit has been pre-coated with an antibody specific to Rat TNNI3/cTn-I. Samples (or Standards) are added to the micro ELISA plate wells and combined with the specific antibody and biotinylated detection antibody specific for Rat TNNI3/cTn-I. Then Avidin-Horseradish Peroxidase (HRP) conjugate are added successively to each micro plate well and incubated. Free components are washed away. The substrate solution is added to each well. Only those wells that contain Rat TNNI3/cTn-I, biotinylated detection antibody and Avidin-HRP conjugate will appear blue in color. The enzyme-substrate reaction is terminated by the addition of stop solution and the color turns yellow. The optical density (OD) is measured spectrophotometrically at a wavelength of 450 nm. The OD value is proportional to the concentration of Rat TNNI3/cTn-I. You can calculate the concentration of Rat TNNI3/cTn-I in the samples by comparing the OD of the samples to the standard curve.</p>

<p>This ELISA kit uses the Sandwich-ELISA principle. The micro ELISA plate provided in this kit has been pre-coated with an antibody specific to Mouse TNNI3/cTn-I. Samples (or Standards) are added to the micro ELISA plate wells and combined with the specific antibody and biotinylated detection antibody specific for Mouse TNNI3/cTn-I. Then Avidin-Horseradish Peroxidase (HRP) conjugate are added successively to each micro plate well and incubated. Free components are washed away. The substrate solution is added to each well. Only those wells that contain Mouse TNNI3/cTn-I, biotinylated detection antibody and Avidin-HRP conjugate will appear blue in color. The enzyme-substrate reaction is terminated by the addition of stop solution and the color turns yellow. The optical density (OD) is measured spectrophotometrically at a wavelength of 450 nm. The OD value is proportional to the concentration of Mouse TNNI3/cTn-I. You can calculate the concentration of Mouse TNNI3/cTn-I in the samples by comparing the OD of the samples to the standard curve.</p>

<p>This ELISA kit uses the Sandwich-ELISA principle. The micro ELISA plate provided in this kit has been pre-coated with an antibody specific to Human cTnT/TNNT2. Samples (or Standards) are added to the micro ELISA plate wells and combined with the specific antibody and biotinylated detection antibody specific for Human cTnT/TNNT2. Then Avidin-Horseradish Peroxidase (HRP) conjugate are added successively to each micro plate well and incubated. Free components are washed away. The substrate solution is added to each well. Only those wells that contain Human cTnT/TNNT2, biotinylated detection antibody and Avidin-HRP conjugate will appear blue in color. The enzyme-substrate reaction is terminated by the addition of stop solution and the color turns yellow. The optical density (OD) is measured spectrophotometrically at a wavelength of 450 nm. The OD value is proportional to the concentration of Human cTnT/TNNT2. You can calculate the concentration of Human cTnT/TNNT2 in the samples by comparing the OD of the samples to the standard curve.</p>

<p>This ELISA kit uses the Sandwich-ELISA principle. The micro ELISA plate provided in this kit has been pre-coated with an antibody specific to Human S100B. Samples (or Standards) are added to the micro ELISA plate wells and combined with the specific antibody and biotinylated detection antibody specific for Human S100B. Then Avidin-Horseradish Peroxidase (HRP) conjugate are added successively to each micro plate well and incubated. Free components are washed away. The substrate solution is added to each well. Only those wells that contain Human S100B, biotinylated detection antibody and Avidin-HRP conjugate will appear blue in color. The enzyme-substrate reaction is terminated by the addition of stop solution and the color turns yellow. The optical density (OD) is measured spectrophotometrically at a wavelength of 450 nm. The OD value is proportional to the concentration of Human S100B. You can calculate the concentration of Human S100B in the samples by comparing the OD of the samples to the standard curve.</p>

<p>This ELISA kit uses the Sandwich-ELISA principle. The micro ELISA plate provided in this kit has been pre-coated with an antibody specific to Human TNNI3/cTn-I. Samples (or Standards) are added to the micro ELISA plate wells and combined with the specific antibody and biotinylated detection antibody specific for Human TNNI3/cTn-I. Then Avidin-Horseradish Peroxidase (HRP) conjugate are added successively to each micro plate well and incubated. Free components are washed away. The substrate solution is added to each well. Only those wells that contain Human TNNI3/cTn-I, biotinylated detection antibody and Avidin-HRP conjugate will appear blue in color. The enzyme-substrate reaction is terminated by the addition of stop solution and the color turns yellow. The optical density (OD) is measured spectrophotometrically at a wavelength of 450 nm. The OD value is proportional to the concentration of Human TNNI3/cTn-I. You can calculate the concentration of Human TNNI3/cTn-I in the samples by comparing the OD of the samples to the standard curve.</p>

<p>This ELISA kit uses the Sandwich-ELISA principle. The micro ELISA plate provided in this kit has been pre-coated with an antibody specific to Mouse cTnT/TNNT2. Samples (or Standards) are added to the micro ELISA plate wells and combined with the specific antibody and biotinylated detection antibody specific for Mouse cTnT/TNNT2. Then Avidin-Horseradish Peroxidase (HRP) conjugate are added successively to each micro plate well and incubated. Free components are washed away. The substrate solution is added to each well. Only those wells that contain Mouse cTnT/TNNT2, biotinylated detection antibody and Avidin-HRP conjugate will appear blue in color. The enzyme-substrate reaction is terminated by the addition of stop solution and the color turns yellow. The optical density (OD) is measured spectrophotometrically at a wavelength of 450 nm. The OD value is proportional to the concentration of Mouse cTnT/TNNT2. You can calculate the concentration of Mouse cTnT/TNNT2 in the samples by comparing the OD of the samples to the standard curve.</p>

<p>Compound A8, known as JAK2-IN-9, is a selective JAK2 inhibitor with an IC50 of 5 nM.</p>

<p>ROCK2-IN-6 (Comp A) is a selective inhibitor of ROCK2, applicable in the study and treatment of ROCK-mediated, autoimmune, and inflammatory diseases [1].</p>

<p>JAK1-IN-11 (compound 11) serves as a potent inhibitor of Janus kinases, exhibiting nanomolar inhibitory concentrations with IC50 values of 0.02 nM (JAK1) and 0.</p>

<p>JAK1-IN-10 (compound 9), a cyano-substituted cyclic hydrazine derivative, functions as a potent and selective inhibitor of JAK1 [1].</p>

<p>JAK-IN-34 (compound 11n) is a potent inhibitor of Janus kinases (JAKs), demonstrating IC50 values of 0.40 nM for JAK1, 0.83 nM for JAK2, 2.10 nM for JAK3,</p>

<p>DPP, a Platinum(IV) complex with a pterostilbene-derived axial ligand, inhibits the JAK2-STAT3 pathway in breast cancer (BC) cells, demonstrating</p>

<p>JAK-IN-27, also known as compound 1, is an orally active, potent inhibitor of the JAKS family kinases, displaying inhibitory concentrations (IC50s) of 3.0 nM</p>

<p>STAT3-IN-18 (compound SPP), a platinum (IV) complex featuring an axial ligand from sandalwood, suppresses the JAK2-STAT3 pathway in breast cancer (BC) cells and</p>

<p>DCN1-IN-2, a DCN1 inhibitor, exhibits potent activity with an IC 50 of 2.96 nM. It effectively mitigates Ang II/TGFβ-induced activation of cardiac fibroblasts and diminishes ISO-induced cardiac fibrosis and remodeling in mice through the selective inhibition of cullin 3.</p>

<p>ROCK-IN-6, a selective ROCK2 inhibitor, exhibits potent inhibition with an IC50 of 2.19 nM and holds promise for research into glaucoma and retinal diseases [1</p>

<p>WHN-88, a Porcupine (PORCN) inhibitor, disrupts the palmitoylation of Wnt ligands, which inhibits their secretion and subsequent Wnt/β-catenin signaling. This compound has shown efficacy in reducing cancer cell stemness and suppressing the progression and development of breast tumors in MMTV-Wnt1 transgenic mice.</p>