Cancer Targeted Therapy

PhiKan 083 hydrochloride is a carbazole derivative, which binds to the surface cavity and stabilizes Y220C (a p53 mutant), with a K_d of 167 μM, and a relative binding affinity (K_d) of 150 μM in Ln229 cells.

Bromoacetamido-PEG3-C2-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

γ-Linolenic Acid methyl ester (Methyl GLA) is an esterified version of γ-Linolenic Acid (GLA), which is an ω-6 fatty acid, serves as melanoma cell proliferation inhibitors. γ-Linolenic Acid methyl ester inhibits ADP-induced blood platelet aggregation and induces apoptosis.

Zevontabart (MYTX-011 Antibody; Q-397) is a pH-dependent anti-c-MET antibody. Zevontabart regulates the trafficking process of c-MET to reduce receptor recycling, and enhances its own endocytosis and accumulation in c-MET-expressing cells. Zevontabart induces cytotoxicity in solid tumor cells and exerts anti-tumor activity in a non-small cell lung cancer xenograft mouse model. Zevontabart can be used to synthesize ADC, such as: MYTX-011. Zevontabart can be used in studies related to non-small cell lung cancer, with its corresponding isotype control being Human IgG1 kappa, Isotype Control (HY-P99001).

hsa-miR-199a-3p inhibitors are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA inhibitors have full-length nucleotide 2'-methoxy modification. The miRNA inhibitors strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning.

(+)-Tetrabenazine ((+)-TBZ) is the enantiomer of Tetrabenazine (HY-B0590) and is also a Vesicular Monoamine Transporter 2 (VMAT2) inhibitor with a rat K_i of 4.61 nM. (+)-Tetrabenazine inhibits monoamine uptake into granular vesicles of presynaptic neurons. (+)-Tetrabenazine is 3 times more active than (-)-Tetrabenazine. (+)-Tetrabenazine can be used for the research of Huntington's disease and hyperkinetic movement disorders (including chorea).

PLK4-IN-1 is a spiro cyclopropyl indolinone compound and PLK4 inhibitor with inhibitory activity against Aurora A and Aurora B kinases .PLK4-IN-1 can be used for the research of cancer .

WSF1-IN-1 (compound 136), an orally active WSF1 inhibitor, can be used in the study for WSF1 (Wolfram syndrome) related tumors, with IC₅₀ values of 0.33 μM and >27 μM in HepG2 parental and HepG2 WFS1 KO cell lines, respectively.

4-(Benzo[d]oxazol-2-yl)aniline is a potent antitumor agent. 4-(Benzo[d]oxazol-2-yl)aniline has inhibitory activity against mammary carcinoma cell lines.

OMS14 is exhibits inhibitory activity for phosphoinositide 3-kinase γ (PI3Kγ) and PIK3CD/PIK3R1, which inhibits 19% PI3Kγ and 65% PIK3CD/PIK3R1 activity at 100 μM. OMS14 exhibits anticancer efficacy in various cancer cells.

Azido-PEG3-SS-PEG3-azide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Azido-PEG3-SS-PEG3-azide is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.

CDK9-IN-12 displays the optimal CDK9 inhibitory activity with an IC₅₀ value of 5.41 nM.

Istiratumab (M-6495) is bispecific monoclonal antibody targeting IGF-1R and ErbB3. Istiratumab induces IGF-1R and ErbB3 receptor degradation through the proteasome pathway Istiratumab can be used for research of cancers.

m-PEG8-Br is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

JAK/HDAC-IN-1 is a potent JAK2/HDAC dual inhibitor, exhibits antiproliferative and proapoptotic activities in several hematological cell lines. JAK/HDAC-IN-1 shows IC₅₀s of 4 and 2 nM for JAK2 and HDAC, respectively.

LL-K9-3 is a selective CDK9-cyclin T1 HyT degrader, with DC₅₀ values of 0.662 μM and 0.589 μM for CDK9 and Cyclin T1, respectively. LL-K9-3 lacks an E3 ligand moiety and induces polyubiquitination and proteasome-mediated synchronous degradation of CDK9 and cyclin T1 via a hydrophobic tag-mediated mechanism. LL-K9-3 downregulates the protein levels of androgen receptor (AR) and c-Myc, and exhibits antiproliferative and pro-apoptotic (apoptosis) activity in prostate cancer cells. LL-K9-3 can be used in studies related to prostate cancer.

Rhamnazin is an orally active inhibitor of VEGFR2 signaling with an IC₅₀ of 4.68 μM against VEGFR2 kinase. Rhamnazin shows potent antiangiogenic activity and antitumor efficacy. Rhamnazin shows antioxidant and anti-inflammatory properties.

Tetrazine-PEG4-SS-NHS is a cleavable 4 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Tetrazine-PEG4-SS-NHS is a click chemistry reagent, it contains a Tetrazine group that can undergo an inverse electron demand Diels-Alder reaction (iEDDA) with molecules containing TCO groups.

(R,S,S)-VH032 is Ligand for E3 Ligase used in the synthesis of PROTACs. VH032 is a VHL ligand and VHL/HIF-1α interaction inhibitor that recruits von Hippel-Lindau (VHL) proteins. (R,S,S)-VH032 synthesizes the tau-targeting small molecule PROTAC C004019 (HY-138669).

EZH2-IN-13 is a potent EZH2 inhibitor, for details please refer to compound 73 in patent WO2017139404. EZH2-IN-13 can be used to study cancers or precancerous lesions associated with EZH2 activity.