Apoptosis Activator

EGFR/BRAFV600E-IN-1 (Compound 23) is a potent EGFR and BRAF^V600E dual inhibitor with IC₅₀s of 0.08 and 0.15 µM, respectively. EGFR/BRAFV600E-IN-1 induces apoptosis and cell cycle arrest in both pre-G1 and G2/M phases. EGFR/BRAFV600E-IN-1 exhibits antiproliferative activity againist A-549, MCF-7, Panc-1, HT-29 with IC₅₀s of 1.2, 0.79, 1.3, and 1.23 µM, respectively.

CPT-Se4, a selenoproagent of Camptothecin (CPT), shows improved potency in killing cancer cells and inhibiting tumor growth. CPT-Se4 decreases the GSH/GSSG ratio and total thiols, elevates the ROS level in Hep G2 cells, and eventually induces apoptosis of cancer cells. CPT-Se4 shows cytotoxicity against HeLa, Hep G2, A549, and SMMC-7721 cells (IC₅₀= 2.54-6.4 μM).

Apoptosis inducer 61 (Compound 4E) is an Apoptosis inducer. Apoptosis inducer 61 significantly downregulates the expression of BIRC3 and activates Apoptosis. Anticancer agent 313 exhibits anticancer activity against ER⁺ breast cancer cells, triple-negative breast cancer cells, and gastric cancer cells.

PeS-9 is an Androgen Receptor (AR) degrader that induces androgen receptor degradation PeS-9 induces mitochondrial and ER stress by promoting cytotoxic ROS production, leading to the release of mitochondrial cytochrome C and AIF. PeS-9 subsequently activates caspases-9 and -3, causing DNA fragmentation and apoptotic cell death. PeS-9 has anticancer activity against prostate cancer and exerts in vivo antitumor and antimetastatic activity with minor side effects. PeS-9 can be used for the study of targeting monotherapy against GLUT-1-overexpressing tumors.

Auristatin S TFA is a potent Auristatin payload. Auristatin S TFA binds to the vinca-binding site on tubulin, thereby inhibiting microtubule assembly and inducing cell cycle arrest and apoptosis. Auristatin S TFA acts as a cytotoxic component of antibody-drug conjugates (ADCs) and exerts target-specific cytotoxicity against cancer cells. Auristatin S TFA can be used in the research of lymphoma, anaplastic large cell lymphoma and Hodgkin lymphoma.

FGFR1/VEGFR2-IN-2 (compound 6l) is a VEGFR2/FGFR1 dual inhibitor. The IC₅₀ values for VEGFR2 and FGFR1 are 0.025 µM and 0.026 µM respectively, and for EGFR and PDGFR-β, the IC₅₀ values are 0.106 µM and 0.077 µM. FGFR1/VEGFR2-IN-2 showes significant anti-cancer activity (GI=60.38%) on NCI-60 cell line, with an IC₅₀ of 8.51 µM in T-47D cell line and anti-migration. FGFR1/VEGFR2-IN-2 acts to arrest cells in the G1 phase and promote apoptosis and necrosis; the IC₅₀ for MCF-7 cell line exceeds 100 µM, and the IC₅₀ for MDA-MB-231 is 69.17 µM, non-toxic to normal cells.

STAT3-IN-53 (Compound L20) is a STAT3 inhibitor with a K_d value of 6.16 μM. STAT3-IN-53 binds directly to the SH2 domain of STAT3, inhibits phosphorylation at the Y705 site without affecting the total STAT3 protein level, and suppresses the IL-6/JAK/STAT3 pathway. STAT3-IN-53 downregulates the transcription and expression of cyclin-D1 and c-Myc. STAT3-IN-53 induces cell cycle arrest and promotes Apoptosis. STAT3-IN-53 exhibits anticancer activity against colorectal cancer.

Kurarinol is a flavanone found in the root of Sophora flavescens. Kurarinol is a competitive tyrosinase inhibitor, with IC₅₀ of 0.1 μM for mushroom tyrosinase.

Top/HDAC-IN-1 (Compound 29b) is a topoisomerase/HDAC dual inhibitor with IC₅₀s of 18, 230, 790, 87, and 5250 nM for HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8, respectively. Top/HDAC-IN-1 exhibits potent antitumor activities against the HCT116 cell line with the IC₅₀ of 180 nM. Top/HDAC-IN-1 efficiently induces apoptosis with G2 cell cycle arrest in HCT116 cells.

Antitumor agent-42 (Compound 15h) is a bifunctional agent exhibiting both tubulin polymerized inhibition and NO-releasing activities, resulting in potent anti-angiogenesis, colony formation inhibition, cell cycle arrest and apoptosis induction effects.

FGFR4-IN-7 (Compound C3) is a covalent reversible FGFR4 inhibitor with an IC₅₀ value of 0.42 μM. FGFR4-IN-7 induces apoptosis via the FGFR4 signaling pathway blockage. FGFR4-IN-7 can be used for the research of hepatocellular carcinoma (HCC).

RFRP-3 (mouse) is a functional ortholog of avian gonadotropin inhibitory hormone (GnIH), binding to GPR147. RFRP-3 (mouse) reduces Progesterone synthesis by inhibiting FSHR and key enzymes involved in steroidogenesis (P450scc, 3β-HSD, StAR). RFRP-3 (mouse) induces Apoptosis (increase of p53). RFRP-3 (mouse) also suppresses the ERK signaling pathway. RFRP-3 (mouse) can be used for research of follicular development.

Uridine 5'-monophosphate-¹³C₉,¹⁵N₂ (5'- Uridylic acid-¹³C₉,¹⁵N₂) dilithium is ¹³C and ¹⁵N-labeled Uridine 5'-monophosphate (HY-101981). Uridine 5'-monophosphate (5'-Uridylic acid) is an orally active mitochondrial ATP-dependent potassium channel activator that has a protective effect on the heart. Uridine 5'-monophosphate can promote the synthesis of CDP-choline and induce apoptosis in intestinal epithelial cells, which is beneficial for gut development and reduces diarrhea.

ABL-L induces apoptosis of human laryngocarcinoma cells through p53-dependent pathway.

CB-184 is a selective ligand for sigma-2 (σ2), with K_i values of 7436 nM for σ1 and 13.4 nM for σ2. CB-184 promotes apoptosis and has antitumor activity.

EGFR-IN-207 (Compound 5h) is an epidermal growth factor receptor (EGFR) kinase inhibitor with an IC₅₀ of 0.21 μM. EGFR-IN-207 induces cell cycle arrest at the Sub-G1 phase and promotes Apoptosis. EGFR-IN-207 exhibits anticancer activity against lung cancer. EGFR-IN-207 shows extremely low toxicity in non-cancerous cell lines. EGFR-IN-207 can be used in lung cancer-related research.

CPT-Se3, a selenoproagent of Camptothecin (CPT), shows improved potency in killing cancer cells and inhibiting tumor growth. CPT–Se3 decreases the GSH/GSSG ratio and total thiols, elevates the ROS level in Hep G2 cells, and eventually induces apoptosis of cancer cells. CPT-Se3 shows cytotoxicity against HeLa, Hep G2, A549, and SMMC-7721 cells (IC₅₀= 2.19-4.7 μM).

IRAK4-IN-27 (Compound 22) is a potent, selective inhibitor of IRAK4, with IC₅₀ of 8.7 nM. IRAK4-IN-27 inhibits cell growth, and promotes apoptosis in MYD88 L265P diffuse large B-cell lymphoma (DLBCL) cell line. IRAK4-IN-27 can be used for DLBCL study.

Pasireotide (aspartate) TFA, a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pK_i=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide (aspartate) TFA can suppress GH, IGF-I and ACTH secretion, indicating potential efficacy in acromegaly and Cushing's disease. Pasireotide (aspartate) TFA also exhibits antisecretory, antiproliferative, and proapoptotic activity.

Minnelide free base is a prodrug of Triptolide (HY-32735) that shows potent antitumor activity in a number of tumor types, particularly in pancreatic cancer. Minnelide free base promotes apoptosis.