Cancer Targeted Therapy

Mal-amido-PEG2-TFP ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

E3 Ligase Ligand 40 is an E3 ligase ligand and can be used for the synthesis of PROTAC molecules.

Boc-NH-PEG6-CH2COOH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

KG-655 is a ligand that specifically binds to the ARNT PAS-B domain. KG-655 binds to the internal cavity of ARNT PAS-B to restrict its variable folded conformation, disrupts the interaction between ARNT PAS-B and the transcriptional coactivator TACC3, and promotes the homodimerization of ARNT PAS-B. KG-655 is widely applicable to cancer-related research.

Amino-PEG6-amido-bis-PEG5-N3 is a cleavable 11 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Amino-PEG6-amido-bis-PEG5-N3 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.

Mefuparib hydrochloride (MPH) is an orally active, substrate-competitive and selective PARP1/2 inhibitor with IC₅₀s of 3.2 nM and 1.9 nM, respectively. Mefuparib hydrochloride induces apoptosis and possesses prominent anticancer activity in vitro and in vivo.

Pomalidomide 4'-alkylC4-azide (Compound 2) is an azide compound containing a MIDI group and is one of the compounds used to construct a library of MIDI azide compounds. Pomalidomide 4'-alkylC4-azide is an E3 ligase ligand and linker conjugate (E3 Ligase Ligand-Linker Conjugate). Pomalidomide 4'-alkylC4-azide can be used to develop research on PROTAC degraders.

FMK-MEA is a potent and selective p90 Ribosomal S6 Kinase (RSK) inhibitor.

Biotin-PEG11-azide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Biotin-PEG11-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.

GNE-6893 is an orally active, selective HPK1 inhibitor with a K_i < 0.02 nM. GNE-6893 enhances T cell receptor signaling in primary human T cells. GNE-6893 increases IL2 production in stimulated primary human T cells. GNE-6893 can be used for the research of chronic refractory cancers.

CFL-120 is a potent KRas^G12C inhibitor. CFL-120 shows an antiproliferative effect. CFL-120 shows anticancer activity. CFL-120 has the potential for the research of lung cancer.

CAP-100 is a monoclonal antibody that targets CCR7. CAP-100 neutralizes the ligand-binding site and signaling of CCR7. CAP-100 strongly inhibits CCR7-induced migration, extravasation, homing, and survival in chronic lymphocytic leukemia (CLL) samples. CAP-100 triggers potent tumor cell killing, mediated by host immune mechanism. CAP-100 shows a favorable toxicity profile on relevant hematopoietic subsets. CAP-100 is involved in research on anti-tumor and disease such as CLL.

NVS-PAK1-C is a potent, ATP-competitive and specific allosteric PAK1 inhibitor probe with IC₅₀ values of 5 nM and 6 nM for dephosphorylated PAK1 and phosphorylated PAK1, respectively. NVS-PAK1-C is also against dephosphorylated PAK2 (IC₅₀=270 nM) and phosphorylated PAK2 (IC₅₀=720 nM).

hsa-miR-138-5p 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.

SARD279 is a HyT degrader of androgen receptor (AR). SARD279 binds to AR, recruits HSP70, mediates ubiquitin-dependent proteasomal degradation, and competitively inhibits the transactivation of AR. SARD279 exhibits antiproliferative activity in AR-dependent prostate cancer cells and castration-resistant prostate cancer cells, including those harboring the AR^F876L mutation. SARD279 can be used in studies related to prostate cancer and castration-resistant prostate cancer.

SBP-0636457 (SB1-0636457) is a SMAC mimetic, and as an IAP antagonist. SBP-0636457 binds to the BIR-domains of the IAP proteins, with a K_i of 0.27 μM. SBP-0636457 can be used for the research of solid tumors and hematologic cancers.

GSK-3/CDK5/CDK2-IN-1, an imidazole derivative, is an inhibitor of cdk5, cdk2, and GSK-3 extracted from patent WO2002010141A1, example 9a. GSK-3/CDK5/CDK2-IN-1 can be used for the research of cancer, and neurodegenerative diseases.

BCR-ABL1-IN-1 (Example 74) is the inhibitor for ABL1 (64-515) with IC₅₀ of 8.7 nM. BCR-ABL1-IN-1 can be used in research on diseases related to the central nervous system (CNS).

Compound 401 is a synthetic inhibitor of DNA-PK (IC₅₀ = 0.28 μM) that also targets mTOR but not PI3K in vitro.

Kushenol E is a class of flavonoids isolated from Sophora flavescens and is a non-competitive indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor with an IC₅₀ of 7.7 µM and a K_i of 9.5 µM, has anti-tumor activity.