Cancer Targeted Therapy

Pim-1/2 kinase inhibitor 1 is an orally active pim-1/2 kinase inhibitor. Pim-1/2 kinase inhibitor 1 blocks the ability of Pim kinases to phosphorylate peptides, and inhibits the pim protein kinase directed phosphorylation of 4E-BP1 and p27^Kip1. Pim-1/2 kinase inhibitor 1 can be used in study of cancer, especially prostate cancer.

Neorauflavane is a tyrosinase inhibitor with mushroom tyrosinase IC₅₀ values of 30 nM and 500 nM, and K_i values of 19 nM and 130 nM. Neorauflavane inhibits monophenolase and diphenolase activities, binds to tyrosinase’s active site via its B-ring resorcinol motif and A-ring methoxy group. Neorauflavane reduces melanin synthesis in melanoma cells. Neorauflavane can be used for the research of skin hyperpigmentation.

PARP1-IN-56 (Compound RCY) is an I-labeled poly(ADP−ribose) polymerase (PARP1) inhibitor. PARP1-IN-56 can be radiolabeled with ²¹¹At or ¹²⁵I for use as an α-emitting radiotherapeutic agent. PARP1-IN-56 can be used for the research of cancer.

WX2-43 is a PRMT5-KLF4 inhibitor (K_d of 11.0 nM). WX2-43 binds to the region between amino acids L400-M500 on PRMT5. WX2-43 efficiently intercepts the interaction between KLF4 and PRMT5, and blocks KLF4 methylation. WX2-43 decreases p21 levels and increases Bax levels. WX2-43 suppresses triple negative breast tumor progression. WX2-43 can be used in the research of triple-negative breast cancer and colorectal cancer.

Dasatinib carbaldehyde (BMS-354825 carbaldehyde), the Dasatinib (ABL inhibitor) based moiety, binds to IAP ligand via a linker to form SNIPER .

StRIP16, bioavailable StRIP3 analogue, is a double-stapled peptide which can bind to Rab8a GTPase, with a K_d of 12.7 μM.

CVM-05-002 is a selective pan-phosphatidylinositol 5-phosphate 4-kinase (PI5P4K) inhibitor, with IC₅₀ values of 0.27 μM and 1.69 μM against PI5P4Kα and PI5P4Kβ, respectively. CVM-05-002 binds non-covalently to the ATP-binding pocket of PI5P4Kα, forming hydrophobic interactions and hydrogen bonds with pocket residues. CVM-05-002 can be used in tumor-related research.

Mal-PEG2-Val-Cit-PAB-OH is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Mal-PEG2-Val-Cit-PAB-OH also can be used as a PROTAC linker that can be used in the synthesis of PROTACs.

tert-Butyl N-[3-(piperazin-1-yl)propyl]carbamate is a linker that can be used for synthesis of PROTAC degrader TrimTAC1 (HY-169355).

Acid-PEG5-mono-methyl ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

N3-PEG3-CH2CH2-Boc is a cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). N3-PEG3-CH2CH2-Boc is also a PEG- and Alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs. N3-PEG3-CH2CH2-Boc 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.

GDC-6036-NH is from patent WO2020097537A2, and a precursor of compound 17 a/b. Compound 17 a/b is a RAS inhibitor and can be used in cancer research.

CaMKP inhibitor sodium (compound 5) is an inhibitor of Ca²⁺/neutral protein-dependent protein concentration (CaMKP) and its nuclear type (CaMKP-N) (IC50: 6.4 μM, CaMKP; 6.6 μM, CaMKP-N). CaMKP is one type of Ser/Thr protein, which can be passed through to remove the oxidized oxidized protein (CaMK). CaMKP inhibitor sodium inhibits CaMKP mediated phospho-CaMKI hydrolysis, unaffectes protein phosphoric acid 2C (PP2C) and calcineurin (CaN).

Dihydrobaicalein is a PLK1 Inhibitor with an IC₅₀ of 6.3 μM. Dihydrobaicalein also inhibits VRK2 and PLK2. Dihydrobaicalein is a natural product that can be isolated from Scutellaria scandens.

S-acetyl-PEG4-amine (TFA) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

BAY 1135626 is used to synthesize BAY 1129980, and use to anti-tumor research. BAY 1129980 is a Auristatin-based anti-C4.4A (LYPD3) antibody–agent conjugate (ADC), is used to non–small cell lung cancer (NSCLC) research.

Polθ-IN-4 is an orally active prodrug of a DNA polymerase θ (Polθ) inhibitor with K_ms of 3.7, 3.7 and 5.2 μM in human, mouse and rat recombinant alkaline phosphatases. Polθ-IN-4 that inhibits Polθ activity by targeting its ATP-dependent helicase domain. Polθ-IN-4 demonstrates significant anti-tumor activity in multiple animal experiments. Polθ-IN-4 can be used for the studies of breast cancer and ovarian cancer.

HPH-15 is an anti-migration compound that inhibits cell migration by binding to hnRNP U or suppressing TGF-β signaling. In addition, HPH-15 can also inhibit epithelial-mesenchymal transition (EMT). HPH-15 holds promise for research in the fields of anti-tumor metastasis and anti-fibrosis.

AMG-595 Antibody is a EGFRvIII targeting antibody. AMG-595 Antibody can be used for synthesis of ADC AMG-595.

PROTAC BRD4 ligand-2 hydrochloride is a ligand for target BRD4 protein for PROTAC CFT-2718.