Angiogénesis

<p>TYD-68 is a potent and selective CRBN-recruiting TYK2 PROTAC degrader, with a DC50 value of 0.42 nM. This compound effectively inhibits IL-12 and IFN-α-induced phosphorylation of STAT4 and STAT1, thereby blocking TYK2-dependent signaling pathways. TYD-68 is applicable in psoriasis research.</p>

<p>JH-XI-10-02 selectively degrades CDK8 (IC50: 159 nM) through proteasome, sparing CDK8 mRNA and CDK19.</p>

<p>CS-VIP 8 TFA is a selective allosteric inhibitor of the WDR5 protein (Ki= 0.008 μM). It induces a conformational change in the MLL1 complex, leading to the dissociation of MLL1 from the complex, thereby inhibiting the MLL1 histone methyltransferase activity and modulating HOX gene expression. CS-VIP 8 TFA shows potential for research in hematological disorders such as leukemia.</p>

<p>Potent PROTAC EGFR degrader 2; IC50: 4.0 nM, DC50: 36.51 nM; inhibits cell growth; for NTR-responsive synthesis.</p>

<p>MLK3-IN-1 (Compound 37) is a selective inhibitor of mixed-lineage kinase 3 (MLK3) with an IC50 of less than 1 nM. It also inhibits FAK with an IC50 of 15.5 μM. In both murine and human liver microsomes, MLK3-IN-1 demonstrates excellent metabolic stability.</p>

<p>FLT3 Ligand-Linker Conjugate 1 consists of an FLT3 ligand and a PROTAC linker that can recruit E3 ligase VHL. This conjugate is useful for synthesizing PROTAC RSS0680, a bifunctional compound designed for targeted protein degradation of kinases.</p>

<p>BDK-IN-1 (compound (-)-43) is a BDK inhibitor with an IC50 of 0.23 μM and a maximum inhibition rate of 90%. It reduces phosphorylated-E1 levels and is useful in the study of cardiac metabolic diseases.</p>

<p>PROTAC ALK degrader-3 (4B) is an orally active PROTAC-based ALK degrader, efficiently inducing sustained degradation of ALK fusion protein and significant inhibition of downstream pathways in Karpas 299 cells with an IC50 of 119.33 nM. This compound exhibits antitumor activity.</p>

<p>BV02 blocks 14-3-3 interactions, useful in chronic myeloid leukemia research, targets T315I mutant and wild-type Bcr-Abl cells.</p>

<p>AZ12672857 is an inhibitor of EphB4 with IC50 of 1.3 nM.</p>

<p>MHES0488A is a selective humanized antibody targeting HER2, with a KD value of 0.8 nM. It constitutes the antibody portion of DHES0815A. Upon cellular internalization, MHES0488A is transported to lysosomes, releasing PBD-monoamide into the nucleus, where it alkylates DNA, inducing DNA damage and apoptosis. It shows potential for research in cancers such as HER2-positive breast cancer and gastric cancer.</p>

<p>PACAP-38 (31-38), human, mouse, rat demonstrates potent, efficacious, and sustained stimulatory effects on sympathetic neuronal NPY and catecholamine production</p>

<p>hCA/VEGFR-2-IN-1 (compound 13a) is a potent dual inhibitor targeting both Carbonic Anhydrase (CA) IX/XII and Vascular Endothelial Growth Factor Receptor 2 (</p>

<p>SNIPER(ABL)-058, a compound that links Imatinib (ABL inhibitor) with a derivative of LCL161 (IAP ligand) through a linker, effectively decreases BCR-ABL protein</p>

<p>Tephrosin induces degradation of of EGFR and ErbB2 by inducing internalization of the receptors, has potent antitumor activities.</p>

<p>SJ988497: PROTAC JAK2 degrader, inhibits CRLF2r cell growth, degrades GSPT1, combines Ruxolitinib, linker, Pomalidomide; researched for ALL.</p>

<p>Ibrutinib dimer is an impurity of Ibrutinib. IIbrutinib dimer is a Dimer of Ibrutinib. Ibrutinib is an irreversible Btk inhibitor (IC50: 0.5 nM).</p>

<p>PROTAC BCR-ABL Degrader-1 (compound PROTAC 1), featuring a 2-oxoethyl linker, promotes Bcr-Abl degradation through the ubiquitin-proteasome pathway and</p>

<p>BMS-599626 2HCL (AC480 2HCl) is a BMS-599626 derivative.</p>

<p>MC-Val-Cit-PAB-Amide-TLR7 agonist 4 Conjugate is a conjugate formed by linking MC-Val-Cit-PAB-Amide and TLR7 agonist 4, useful for cancer research.</p>

<p>JAK1/TYK2-IN-1 is a dual inhibitor of TYK2 and JAK1 ( IC 50 = 29 and 41 nM respectively).</p>

<p>SIAIS100, a potent BCR-ABL PROTAC degrader, demonstrates a DC50 value of 2.7 nM, highlighting its efficacy.</p>

<p>AT-533 inhibits Hsp90, HSV, hinders HIF-1α/VEGF/VEGFR-2, Erk1/2, FAK, Akt/mTOR/p70S6K, and blocks tumor growth, angiogenesis, and HUVEC activities.</p>

<p>EGFR-IN-110 (Compound 6) is a covalent inhibitor of EGFR, demonstrating pIC50 values of 9.2 for the EGFR enzyme and 8.7 for EGFR cells. It exhibits strong efficacy in targeting EGFR and maintains good kinase selectivity.</p>

<p>Tyrosine kinase substrate peptide</p>

<p>Potent PROTAC degrader for FLT3/CDK9, induces apoptosis, and shows promise for FLT3-ITD mutated AML research.</p>

<p>PTD10, a highly potent PROTAC BTK degrader, exhibits a DC50 of 0.5 nM and a KD of 2.28 nM.</p>

<p>Rinucumab (REGN 2176) is an anti-PDGF IgG4-like monoclonal antibody that can be used to study age-related macular degeneration.</p>

<p>JAK/HDAC-IN-2, a potent 2-amino-4-phenylaminopyrimidine dual-target inhibitor, effectively suppresses JAK1/2 and HDAC3/6 at nanomolar concentrations.</p>

<p>CNX-500: covalent Btk inhibitor linked to biotin, IC50 0.5 nM, low effect on EGFR and Src kinases.</p>

<p>Efruxifermin, a modified FGF21 with IgG1 Fc, has increased stability and affinity. Used in non-alcoholic steatohepatitis research.</p>

<p>DP-C-4 is a Cereblon-based dual PROTAC for simultaneous degradation of EGFR and PARP[1].</p>

<p>A unique collection of 1353 proangiogenic and antiangiogenic compounds for new targets identification, research in mechanisms of angiogenesis, and high</p>

<p>BCR-ABL-IN-3 irreversibly inhibits Bcr-Abl with &lt;100 nM IC50, showing significant anti-cancer effects.</p>

<p>EGFR/CDK2-IN-2 (compound 6a) serves as a dual inhibitor targeting both EGFR and CDK-2, exhibiting IC50 values of 19.6 nM and 87.9 nM, respectively.</p>

<p>SJF620 hydrochloride is a PROTAC that utilizes a lenalidomide analog to recruit CRBN and ligands to target Btk, exhibiting a DC50 of 7.9 nM [1].</p>

<p>Phage display selected Affibody ligands for HER2/neu from a protein library based on a 58-residue Staphylococcal protein A Z domain.</p>

<p>SJ10542: potent JAK2/3-targeting PG-PROTAC; DC50s: JAK2 - 14 nM, JAK3 - 11 nM, JAK2-fusion ALL - 24 nM; CRBN recruiter.</p>

<p>Sotiburafusp alfa is a humanized bispecific fusion protein comprising a VEGFR-1 extracellular domain fragment (129-228, 1-100 in the current sequence) connected</p>

<p>SC209, a STRO-002 metabolite from patent WO2021247798, synthesizes anti-EGFR ADCs.</p>

<p>Coumermycin A1 is a JAK2 signal activator. Coumermycin A1 inhibits DNA Gyrase which thereby inhibits cell division in bacteria.</p>

<p>FLT3-IN-28 (Compound 12y) is an orally active FLT3 inhibitor with antitumor properties. It selectively targets cancer cells with FLT3 internal tandem duplication (ITD) mutations, demonstrating IC50 values of 85, 290, 130, 65, and 220 nM against BaF3-FLT3-ITD, BaF3-TEL-VEGFR2, MV4-11, MOLM-13, and MOLM-14 cell lines, respectively. These lines include acute myeloid leukemia (AML) cells harboring FLT3-ITD mutations such as MV4-11 and MOLM-13/14. The compound also reduces phosphorylation levels of FLT3 and STAT5 in MOLM-13 cells, leading to cell cycle arrest and apoptosis. With an oral bioavailability of 19.2% in SD rats, FLT3-IN-28 extends survival in a dose-dependent manner in MOLM-13 xenografted NSG mouse models. It holds promise for research in FLT3-ITD-related cancer studies.</p>

<p>Erlotinib-13C6 (CP-358774-13C6), a 13C-labeled direct EGFR inhibitor, IC50: 2 nM.</p>

<p>Fazpilodemab (BFKB8488A) is a humanized bispecific antibody that targets and activates the Klotho β and fibroblast growth factor receptor 1c receptor complex.</p>

<p>Compound 13b, a potent EGFR degrader, inhibits and induces apoptosis in NSCLC cells with a DC50 of 13.2 nM.</p>

<p>ML 2-23 is a potent BCR-ABL degrader operating as a PROTAC, exhibiting selective proteasome-dependent degradation of BCR-ABL within leukemia cells [1].</p>

<p>Caxmotabart is a humanized IgG1κ antibody targeting ERBB2, with HumanIgG1kappa, Isotype Control as its corresponding isotype control.</p>

<p>Wu-5 is a potent USP10 inhibitor that inhibits FLT3 and AMPK pathways, promoting the breakdown of FLT3-ITD and inducing apoptosis.</p>

<p>HIF-1 inhibitor-4 (HIF-1 inhibitor-4) is a HIF-1 inhibitor with IC50 of 560 nM.</p>

<p>Dacomitinib metabolite M2 is also known as Dacomitinib cysteine conjugate. Dacomitinib inhibits both the wild-type (WT) EGFR and EGFR T790M.</p>