Cancer Targeted Therapy

hsa-miR-221-5p 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.

m-PEG6-CH2CH2CHO is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). m-PEG6-CH2CH2CHO is also a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

Fluvastatin-d₆ (sodium) is deuterium labeled Fluvastatin sodium. Fluvastatin sodium (XU 62320) is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM.

SM1-71-R is a reversible analog o SM1-71 (HY-136848). SM1-71-R lacks the acrylamide warhead and therefore cannot form a covalent bond with the kinase. SM1-71-R can be used as a control compound for SM1-71.

NHPI-PEG4-C2-NHS ester is an ADC Linker, which can be used to synthesize antibody-drug conjugates (ADCs).

hsa-miR-181a-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.

VinclozolinM2-2204 is a androgen receptor (AR) AUTOTAC degrader, with an DC₅₀ of 200 nM in LNCaP prostate cancer cells. VinclozolinM2-2204 induces the formation of AR⁺LC3⁺ autophagic membranes. VinclozolinM2-2204 can be used for the research of cancer.(Pink: AR inhibitor (HY-168296); Black: linker (HY-128833); Blue: CRBN Ligand (HY-168293))

hsa-miR-9985 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.

SIRT1-IN-3 (compound 3j) is a potent and selective SIRT1 inhibitor, with an IC₅₀ of 4.2 μM.

Liarozole (R75251) dihydrochloride is an imidazole derivative and orally active retinoic acid (RA) metabolism-blocking agent (RAMBA). Liarozole dihydrochloride inhibits the cytochrome P450 (CYP26)-dependent 4-hydroxylation of RA (IC₅₀=7 μM), resulting in increased tissue levels of RA. Liarozole dihydrochloride shows antitumoral properties.

NAE-IN-M22 is a potent, selective and reversible inhibitor of NEDD8 activating enzyme (NAE), with potency in micromolar range. NAE-IN-M22 inhibits multiple cancer cell lines and induces apoptosis in A549 cells. NAE-IN-M22 also can inhibit tumor growth in vivo.

(1E)-CFI-400437 dihydrochloride is a potent PLK4 (IC₅₀= 0.6 nM) inhibitor and selective against other members of the PLK family (>10 μM). (1E)-CFI-400437 dihydrochloride inhibits Aurora A, Aurora B, KDR and FLT-3 with IC₅₀s of 0.37, 0.21, 0.48, and 0.18 μM, respectively. Antiproliferative activity.

MC-Val-Cit-PAB-Indibulin is a agent-linker conjugate for ADC with potent antitumor activity by using Indibulin (an orally applicable inhibitor of tubulin assembly), linked via the ADC linker MC-Val-Cit-PAB.

GPX4-IN-6 (Compound C25) is a GPX4 covalent inhibitor with an IC₅₀ value of 0.13 μM. GPX4-IN-6 (Compound C25) can induce ferroptosis for the research of triple-negative breast cancer (TNBC) .

Conteltinib tetrahydrochloride (CT-707 tetrahydrochloride) is the tetrahydrochloride salt form of Conteltinib (HY-109084). Conteltinib tetrahydrochloride is the inhibitor for FAK (IC₅₀=1.6 nM), ALK, and Pyk2. Conteltinib tetrahydrochloride exhibits a synergistic anti-tumor efficacy with Cabozantinib (HY-13016).

PROTAC AURKA degrader 2 (compound D) is a potent and selective PROTAC AURKA degrader with an IC₅₀ of 3.58 nM. PROTAC AURKA degrader 2 exhibits 21.6-fold selectivity for AURKA over AURKB (IC₅₀ = 77.2 nM). PROTAC AURKA degrader 2 specifically depletes AURKA on the mitotic spindle.

Toralactone, isolated from Cassia obtusifolia, mediates hepatoprotection via an Nrf2-dependent anti-oxidative mechanism.

Theasaponin E1 is an orally effective tea saponin. Theasaponin E1 inhibits the proliferation of cancer cells by activating apoptosis. Theasaponin E1 inhibits angiogenesis in ovarian cancer cells and HUVECs by reducing the expression of VEGF. Theasaponin E1 upregulates the phosphorylation level of ATM protein and the expression level of PTEN protein in cancer cells, decreases the phosphorylation levels of Akt, mTOR, p70S6K and 4E-BP1 proteins, downregulates the expression of HIF-1α and NF-κB, and reduces the protein expression of Notch ligands Dll4 and Jagged1. Theasaponin E1 exerts neuroprotective effects by inhibiting the activity of acetylcholinesterase, activating α-secretase and neprilysin, reducing the concentration of Aβ, and inhibiting the activities of β-secretase and γ-secretase. Theasaponin E1 exhibits toxic effects on cancer cells and quinone reductase-inducing activity, and inhibits tumor growth in vivo. Theasaponin E1 induces ferroptosis in Pomacea canaliculata by synergistically disrupting cholesterol homeostasis and sphingolipid metabolism. Theasaponin E1 possesses anti-biofilm activity against Candida albicans. Theasaponin E1 can be used in the research of ovarian cancer, obesity, Alzheimer's disease and fungal infections.

Thalidomide-O-C6-azide is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide (HY-14658) based cereblon ligand and a linker used in PROTAC technology. Thalidomide-O-C6-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.

Keliximab (SB-210396) is a chimeric human/macaque IgG1 anti-CD4 monoclonal antibody with a K_i value of 1.0 nM for soluble CD4. Keliximab blocks T cell proliferation and inhibits IL-2 production. Keliximab can be used for cancer research.