Cellule staminali e Derivati

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

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

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

<p>ROCK/HDAC-IN-1 (Compound 10h) serves as an orally effective inhibitor of ROCK/HDAC. This compound suppresses ROCK1/2 (IC50: 254.9 nM, 58.18 nM) and HDAC1/2/3/6/8 (IC50: 9.09, 8.03, 6.26, 0.41, 7.69 nM). It stimulates the activation of DAMPs, notably calreticulin (CRT) exposure and HMGB1 release, suggesting its potential as an inducer of immunogenic cell death (ICD). ROCK/HDAC-IN-1 exhibits antiproliferative effects against breast cancer cells (IC50: 0.37 μM for MDA-MB-231 cells), inhibits tumor growth, activates T cells, and shows no significant toxicity.</p>

<p>MGD-28 is a Cullin-CRBN-dependent IKZF family protein degrader for IKZF1 (Ikaros), IKZF2 (Helios), IKZF3 (Aiolos) ,and CK1α, antiproliferative.</p>

<p>(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].</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>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].</p>

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

<p>AZ-3 is a potent and selective JAK1 inhibitor (IC50: 34 nM).</p>

<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>

<p>Ten01 exhibits a 5.0 nM inhibition of JAK1 kinase.</p>

<p>GDC-9918 (compound GDC-9918) is an inhibitor of Janus kinases.</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>(+)-ITD-1 is an inhibitor of TGF-β, effectively inhibiting TGF-β2 with an IC50 of 0.46 μM. It promotes the degradation of the TGF-β type II receptor (TGFBR2) and the differentiation of cardiomyocytes. Additionally, it suppresses the formation of the mesoderm during the early differentiation of mouse embryonic stem cells (mESCs).</p>

<p>STAT3-IN-36 (compound 11g) is a tritarget inhibitor that selectively targets LRPPRC, STAT3, and CDK1, exhibiting potent anticancer activity. This compound binds to LRPPRC, STAT3, and CDK1, demonstrating more effective anticancer effects than those of TMF or Capecitabine. Additionally, STAT3-IN-36 exhibits an IC50 value of 1.8 μM in HGC27 cells.</p>

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

<p>dCK1α-2 is an orally effective CK1α molecular glue (Molecular Glue) degrader that targets p53 pathway-related targets. It demonstrates antitumor efficacy in mouse models by enhancing the expression of p53-related genes.</p>

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

<p>NRX-103095 increases β-catenin binding to SCFβ-TrCP E3 ligase; EC50 is 163 nM for pSer33/Ser37 affinity boost.</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>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>(3R,4S)-Tofacitinib, the less active enantiomer of Tofacitinib, is a JAK3 inhibitor with an IC50 of 1 nM.</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>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>Compound A8, known as JAK2-IN-9, is a selective JAK2 inhibitor with an IC50 of 5 nM.</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>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>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>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-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>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>

<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>