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<p>PI3K/HDAC-IN-4 (Compound 31f) is a dual inhibitor targeting PI3K and HDAC, with an IC50 of 0.2μM. It demonstrates high selectivity for HDAC1-3, with IC50 values of 75.5 nM, 70.9 nM, and 1.9 nM, respectively. As a potent pan-PI3K inhibitor, PI3K/HDAC-IN-4 has IC50 values of 2.5 nM, 80.5 nM, 10.0 nM, and 57.2 nM for PI3Kα, β, δ, and γ, respectively. This compound effectively induces apoptosis in tumor cells by concurrently inhibiting the PI3K/AKT/mTOR signaling pathway and HDAC1-3. It shows significant antiproliferative activity across various tumor cell lines, such as MV4-11, Jeko-1, HL60, and MCF-7, with IC50 values of 0.2, 0.9, 0.8, and 1.5 μM, respectively. PI3K/HDAC-IN-4 is applicable in the study of lymphoma and leukemia.</p>

Carbonic anhydrase inhibitor32 (compound 5B) is an orally active, selective inhibitor of hCA (carbonic anhydrase) II/VII, with Ki values of 6.3 nM for hCA II, 10.1 nM for hCA VII, and 681 nM for hCA I. It shows potential for neuroprotection and anticonvulsant effects by reducing mTOR activation and increasing hippocampal KCC2 levels.

<p>OT-R agonist 1 TFA (compound 5) is an oxytocin receptor (OT-R) agonist with an EC50 value of 0.39 nM. It exhibits V1A antagonist activity, with an EC50 value of 2432 nM, and can be utilized in studies related to central nervous system diseases.</p>

Difenoxuron, a herbicide, can control wild oats and other weeds.

JTT-553 is a DGAT1 inhibitor with an IC50 of 2.38 nM. It effectively reduces plasma levels of glucose, insulin, non-esterified fatty acids (NEFA), total cholesterol (TC), and liver triglycerides (TG). JTT-553 enhances insulin-dependent glucose absorption and glucose intolerance in the adipose tissue of diet-induced obese (DIO) mice. In KK-Ay mice, it lowers TNF-α mRNA levels and elevates GLUT4 mRNA levels in adipose tissue. By contributing to weight loss, JTT-553 improves insulin resistance in adipose tissue and overall glucose metabolism. This compound is useful for research on obesity and type 2 diabetes mellitus (T2DM).

GSK-3β/CK-1δ-IN-1 (8d) is a dual inhibitor of GSK-3β and CK-1δ that can cross the blood-brain barrier, with IC50 values of 0.77 μM and 0.57 μM, respectively. GSK-3β/CK-1δ-IN-1 (8d) is applicable in neuroblastoma research.

<p>N-0920 is a potent TMPRSS2 inhibitor with an IC50 value of 0.35 nM. It effectively inhibits the entry of SARS-CoV-2 variants [EG.5.1] and [JN.1] into Calu-3 cells, exhibiting EC50 values of 300 pM and 90 pM, respectively.</p>

<p>Quorum sensing-IN-10 (10p) is an antimicrobial adjuvant that significantly inhibits the virulence, biofilm formation, and motility of Pseudomonas aeruginosa, while exhibiting low toxicity. It is applicable for research related to drug-resistant Pseudomonas aeruginosa infections.</p>

Adavosertib (MK-1775) is a small molecule inhibitor of the checkpoint kinase WEE1 (IC50: 5.2 nM). It hinders the G2 DNA damage checkpoint.

<p>BAY32-5915 is a selective inhibitor of IKKalpha.</p>

<p>FGA139 is an inhibitor of cysteine proteases, specifically targeting cathepsin B and L with IC50 values of 4.98 μM and 3.14 μM, respectively. It reduces the production of NO in LPS-induced RAW264.7 cells and lowers TNFα levels in microglia, demonstrating antioxidant and anti-inflammatory properties. Additionally, FGA139 enhances the secretion of neuroprotective metabolites such as purines and linoleic acid in LPS-stimulated microglia. This compound is applicable in the study of neuroinflammatory diseases.</p>

CXCR2/CCR7 antagonist-1 (compound 6) is a potent dual antagonist of CXCR2 and CCR7, with IC50 values of 0.0046 μM and 0.0014 μM, respectively. It is valuable for research in tumor metastasis and autoimmune diseases.

SARS-CoV-2 3CLpro-IN-32 (compound B16) is a potent inhibitor of the SARS-CoV-2 3CLpro enzyme, with an IC50 of 0.109 μM. It also demonstrates antiviral activity against the coronavirus HCoV-OC43, with an EC50 of 1.99 μM.

TRF1-TIN2 interaction-IN-1 (Compound 40) is an inhibitor of the TRF1-TIN2 interaction. It binds to the TRFH domain of TRF1 (KD= 29 μM) and competitively inhibits the binding of the TIN2 peptide (IC50= 67 μM). By occupying a hotspot at the TRF1-TIN2 interface, TRF1-TIN2 interaction-IN-1 disrupts the interaction between TRF1 and TIN2. This compound can remove TRF1 from the shelterin complex, making it useful for research on shelterin-related cancers.

Lissamine rhodamine B, a new Radiotracer, is used for Imaging Tumors by Positron Emission Tomography.

Fluoxetine-Conjugated Platinum(IV) prodrug-1 is an eEF2K inhibitor that can hinder the proliferation of cancer cells, induce DNA damage, and cause cell cycle arrest at the S phase, leading to apoptosis (Apoptosis). It also promotes the accumulation of reactive oxygen species (ROS) and disrupts mitochondrial function. This prodrug inhibits the migration and invasion of TNBC cells by suppressing MMP-2 activity and induces autophagy in TNBC cells through AMPK activation. In the 4T1-Luc mouse model, it exhibits antitumor activity and triggers immune suppression. Fluoxetine-Conjugated Platinum(IV) prodrug-1 is relevant for research in triple-negative breast cancer (TNBC).

<p>SIK2-IN-3 is an orally active selective inhibitor of SIK1/2 with IC50 values of 0.128/0.084 μM. It hinders the phosphorylation of CRTC3 and suppresses the production of pro-inflammatory factors in myeloid cells. Additionally, SIK2-IN-3 alleviates systemic and tissue inflammatory responses in a mouse anti-CD40 colitis model.</p>

<p>Crufomate, an insecticide, is used extensively for the control of hornflies, cattle grubs and cattle lice.</p>

Polθ-IN-8 (example 77) is a DNA polymerase θ (Polθ) inhibitor with an IC50 for Polθ ATPase activity of less than 100 nM. Polθ-IN-8 is useful for researching diseases related to Polθ activity, such as cancer.

<p>PARP14 inhibitor2 (Compound 3) is an orally active and highly selective PARP14 inhibitor with an IC50 value of less than 30 nM. It effectively inhibits the mono ADP-ribosyltransferase activity of PARP14 and modulates IFN-γ and IL-4 signaling, thereby reversing pro-tumor macrophage polarization and suppressing anti-tumor inflammatory responses. PARP14 inhibitor2 holds potential for research in PARP14-related conditions such as tumors, atopic dermatitis, and autoimmune diseases.</p>