Cancer Targeted Therapy

DBCO-PEG3-acid is a non-cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). DBCO-PEG3-acid contains a DBCO group that can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing Azide groups.

TTK ligand 2 is a monopolar spindle 1 (TTK) ligand that can be used in the synthesis of PROTACT (HY-168540).

TFCP2L1-IN-1 is a specific small molecule targeting TFCP2L1’s active domain with anti-cancer activity. TFCP2L1-IN-1 synergizes with Sorafenib (HY-10201) to induce Apoptosis and reduces cell proliferation, invasion, metastasis, clonal formation and sphere-forming capacity in hepatocellular carcinoma cells.

CDDO-3P-Im is an analogue of CDDO-Imidazolide with chemopreventive effect. CDDO-3P-Im can reduce the size and the severity of the lung tumors in mouse lung cancer model. CDDO-3P-Im is a orally active necroptosis inhibitor that can be used for the research of ischemia/reperfusion (I/R).

N3-PEG5-C6-Cl is a PEG PROTAC linker, can be used for synthesis of HALo PROTAC.

Farnesylthioacetic acid is a competitive, non-substrate inhibitor of Prenylcysteine α-carboxyl methyltransferase. It acts as a non-substrate competitive inhibitor of Arabidopsis thaliana Prenylcysteine α-carboxyl methyltransferase and blocks methyltransferase activity. Farnesylthioacetic acid does not inhibit protein farnesyltransferase activity in Arabidopsis. It induces Apoptosis. Farnesylthioacetic acid regulates the subcellular localization of Ras protein, reducing the proportion of cytoplasmic Ras protein without disrupting membrane binding. It enhances ABA-induced seed dormancy, delays seed germination, and promotes maximum stomatal closure at lower exogenous ABA concentrations. Farnesylthioacetic acid can be used in studies related to promyelocytic leukemia.

HDAC6-IN-23 (compound 9) is an orally active HDAC6 inhibitor.

YLIU-4-105-1 is a Type II JAK2 inhibitor. YLIU-4-105-1 binds to the ATP-binding pocket of JH1. YLIU-4-105-1 has in vivo pharmacodynamic activity as evidenced by inhibiting pSTAT5, reducing spleen to body weight, and lowering blood reticulocyte counts in a dose-dependent manner.

Diazo Biotin-PEG3-alkyne is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Diazo Biotin-PEG3-alkyne is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

hsa-miR-200b-3p antagomirs are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA antagomirs have 2 phosphorothioates at the 5' end, 4 phosphorothioates at the 3' end, 1 cholesterol group at the 3' end, and full-length nucleotide 2'-methoxy modification. The miRNA antagomirs strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning. Stability of miRNA antagomirs appears to be significantly higher than miRNA inhibitors, they exhibits enhanced cellular uptake, stability and regulatory activity in vivo.

AurAP14 is an Aurora A PROTAC degrader (DC₅₀ = 120 nM). AurAP14 can form a stable ternary complex with Aurora A kinase and HSP90, recruiting cullin family E3 ubiquitin ligases and MDM2 to mediate the ubiquitination and proteasome degradation of Aurora A kinase. AurAP14 increases p53 levels and decreases C-MYC levels; AurAP14 induces Apoptosis. AurAP14 can be used in the study of non-small cell lung cancer.

D-Proline, 4-hydroxy-, methyl ester hydrochloride is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). D-Proline, 4-hydroxy-, methyl ester hydrochloride is also a alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[2

Bromo-PEG6-bromide is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.

(S,R,S)-AHPC-Boc derivative 1 (VH032-Boc derivative 1) is a derivative of (S,R,S)-AHPC-Boc (HY-123109), which is applicable to research related to PROTAC synthesis.

APTSTAT3-9R, a specific STAT3-binding peptide, inhibits STAT3 activation and downstream signaling by specifically blocking STAT3 phosphorylation. APTSTAT3-9R exerts antiproliferative effects and antitumor activity.

BPHA is a potent and orally active MMP-2, MMP-9 and MMP-14 inhibitor with IC₅₀s of 12 nM, 16 nM and 17 nM, respectively. BPHA does not inhibit MMP-1, -3, and -7 (the IC₅₀s are 974, >1000, and 795 nM, respectively). BPHA has antiangiogenic and antitumor effects.

5-Hydroxyuridine (OHUrd) is a purine nucleoside analogue. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc.

BX-320 is a selective, ATP-competitive, orally acitive, and direct PDK1 inhibitor with an IC₅₀ of 30 nM in a direct kinase assay format. BX-320 also induces apoptosis. Anticancer effect.

Anti-Mouse BTLA/CD272 Antibody (6A6) is an Armenian hamster-derived anti-mouse BTLA/CD272 IgG κ type antibody inhibitor. Anti-Mouse BTLA/CD272 Antibody (6A6) can be used for the researches of cancer and immunology, such as graft versus host disease (GVHD) and WF-3/Luc tumor.

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