Cellule staminali

ML115 is a potent and selective activator of transcription 3 (STAT3), with abn EC50 of 2.0 nM, and is inactive against the related STAT1 and NFκB anti-targets.

<p>ROCK-IN-1 is a potent ROCK inhibitor that inhibits ROCK2-mediated signaling with an IC50 value of 1.2 nM.ROCK-IN-1 can be used in the study of neurological</p>

STAT6-IN-2(R)-84 is a STAT6 inhibitor that inhibits the secretion of eotaxin-3 and the tyrosine phosphorylation of STAT6.

H-1152 2HCl: ROCK inhibitor, IC50=12 nM, Ki=1.6 nM. Blocks PKA, PKC, PKG, Aurora A, CaMKII with higher IC50s.

<p>GNE-7883 is an inhibitor targeting TEAD transcription factor, inhibits cell proliferation and suppresses YAP/TAZ activation, and can be used to study YAP/TAZ-dependent tumors.</p>

JAK-IN-3 is a potent JAK inhibitor that inhibits JAK3, JAK1, TYK2, and JAK2, and can be used for the study of immune system disorders.

GSK-3 inhibitor 1 is a GSK-3 inhibitor.

<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>

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>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>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>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.</p>

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>"STAT3-IN-8 (compound H172) is a potent inhibitor of STAT3 with potential applications in cancer research [1]."</p>

M3686 (Compound 29) is a potent and selective TEAD1 inhibitor with an IC50 value of 51 nM. It exhibits weaker binding activity toward TEAD3. M3686 significantly inhibits the cellular activity of YAP-dependent NCI-H226 cell lines, with an IC50 value of 0.06 μM, and demonstrates strong antitumor effects in the NCI-H226 xenograft model.

<p>GDC-9918 (compound GDC-9918) is an inhibitor of Janus kinases.</p>

<p>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.</p>

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

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.

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.

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

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

<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>

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

(R)-9b is an effective inhibitor of the ACK1 tyrosine kinase (IC50=56 nM) and exhibits anticancer activity. It selectively targets ACK1 but also inhibits kinases in the JAK family, specifically JAK2 and Tyk2. (R)-9b is used in research related to hormone-regulated cancers, such as prostate cancer and breast cancer.

<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>JAK3-IN-7 is a potent and selective JAK3 inhibitor (IC50&lt;0.01 μM) for the treatment of rejection in organ transplantation, graft-versus-host reaction after</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>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>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>

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

<p>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].</p>

CDK8-IN-11 is a CDK8 inhibitor that demonstrates anti-proliferative activity against colon cancer cell lines and inhibits the activation of WNT/β-catenin.

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

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).

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].

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

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

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

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

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].

<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 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>