Cellule staminali e Derivati

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

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

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

<p>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>

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

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

<p>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.</p>

<p>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.</p>

<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>

<p>AJI-100 serves as a dual-target inhibitor, effectively blocking Aurora kinase A and JAK2, with respective IC50 values of 12.7 nM and 18.5 nM. It inhibits T cell mitosis and cell polarity by directly targeting Aurora kinase A and reduces STAT3 phosphorylation by inhibiting JAK2 activation, consequently diminishing the differentiation of TH1 and TH17 cells. This compound is utilized in researching immune response regulation and the prevention of graft-versus-host disease (GVHD).</p>

<p>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.</p>

<p>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).</p>

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

<p>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.</p>

<p>JAK2-IN-11 (Example 6) is a JAK2 kinase inhibitor with potent antitumor activity, exhibiting an IC50 of ≤10 nM against JH2 BIND WT/V617F. This compound effectively suppresses tumor growth.</p>

<p>YAP/TAZ-TEAD-IN-2 (Compound 51) is a YAP/TAZ-TEAD inhibitor that disrupts the interaction between YAP/TAZ and TEAD. It inhibits the transcriptional activity of TEAD with an IC50 of 1.2 nM. Additionally, YAP/TAZ-TEAD-IN-2 suppresses the expression of target genes (Cyr61, CTGF, AXL, and Survivin) and the proliferation of breast cancer cells.</p>

<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>

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

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

<p>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.</p>

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

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

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

<p>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].</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 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 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 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>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 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 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 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>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>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>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>JAK1-IN-10 (compound 9), a cyano-substituted cyclic hydrazine derivative, functions as a potent and selective inhibitor of JAK1 [1].</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>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>DPP, a Platinum(IV) complex with a pterostilbene-derived axial ligand, inhibits the JAK2-STAT3 pathway in breast cancer (BC) cells, demonstrating</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>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>

<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>