Apoptosis

VEGFR-2-IN-14 (Compound 5) is a potent inhibitor of VEGFR-2, which inhibits the growth of HepG2 cells in the Pre-G1 phase and induces apoptosis.

Potent dual c-Met/HDAC inhibitor, IC50: HDAC1 5.4 nM, c-Met 18.49 nM; anti-cancer, induces apoptosis, G2/M arrest in HCT-116.

PBX-7011, an active camptothecin derivative, binds to the DDX5 protein in cells and induces cell death through DDX5 protein degradation [1].

PD-1/PD-L1-IN-16 is a potent inhibitor of PD-1/PD-L1 (IC50: 53.2 nM) and has shown research potential for tumour immunotherapy.

D18: Dual agonist for TLR7/8, boosts PD-L1, aids tumor sensitivity to PD-1/PD-L1 inhibitors, and is a cytotoxin for ADC HE-S2.

SPI-001 is a selective inhibitor of PPM1D (IC50=0.48 µM) that exhibits anticancer activity. The compound inhibits the phosphatase activity of PPM1D in human breast cancer cells overexpressing PPM1D and enhances the phosphorylation of p53. Additionally, SPI-001 suppresses cell proliferation by inducing apoptosis.

SL-176, a WIP1 inhibitor, when combined with GSK-J4, can induce cell cycle arrest and apoptosis (apoptosis), thereby inhibiting tumor growth both in vitro and in vivo.

p53 Activator 8 (compound 5), a potent p53 activator, exhibits significant anti-proliferative effects on MCF7 breast cancer cell lines, demonstrating an IC 50 value of 0.5 μM [1] [2].

Lepidozin G blocks cancer growth (IC50=4.2-5.7μM) and triggers apoptosis in PC-3 cells via mitochondria.

CDK2/9-IN-1 (compound 20a) is an orally active dual inhibitor of CDK2 and CDK9, with IC50 values of 0.004 μM and 0.009 μM for CDK2 and CDK9, respectively. It induces apoptosis by regulating G2/M cell cycle arrest and exhibits antitumor activity.

CCT369260 (compound 1), an orally active inhibitor targeting B-cell lymphoma 6 (BCL6), demonstrates anti-tumor efficacy with an IC50 value of 520 nM [1].

HDAC-IN-34 inhibits HDAC1 (IC50: 0.022 μM) & HDAC6 (IC50: 0.45 μM), binds DNA causing damage, and halts HCT-116 cell growth (IC50: 1.41 μM).

Antitumor agent-58 suppresses tumor growth, colony formation, cell migration, and induces mitochondrial dysfunction in MGC-803 cells.

TfR-1-IN-1 is a TfR-1 inhibitor, also a Fe(III) salivary phenol complex, inducing apoptosis and inhibiting tumor and normal cell growth.

RIP1 kinase inhibitor 1 is an orally available and brain-penetrating inhibitor of RIP1 kinase with pKi of 9.04.

HDAC-IN-37 inhibits HDACs 1, 3, 8, & 6, induces histone acetylation, halts G1 to S phase, and triggers early apoptosis.

Evo312 is an inhibitor of protein kinase C beta I (PKCβI) with an IC50 of 117.34 nM and exhibits dose-dependent characteristics. It acts by inhibiting the expression of the PKCβI protein, which leads to cell cycle arrest and apoptosis in PANC-GR (gemcitabine-resistant pancreatic cancer cells). Evo312 also demonstrates antiproliferative effects in pancreatic cancer cells PANC-1 and PANC-GR, with IC50 values of 0.08 μM and 0.07 μM respectively, while presenting an IC50 of 2.95 μM in normal human pancreatic ductal epithelial cells HPDE6-c7. Additionally, Evo312 has shown antitumor activity in a mouse xenograft model using PANC-GR cells.

<p>N-ω-chloroacetyl-L-ornithine (NCAO) serves as a powerful reversible competitive inhibitor of ornithine decarboxylase (ODC), displaying cytotoxic and antiproliferative properties against various tumor cell lines, with EC50 values spanning from 1 to 50.6 µM. In vitro studies reveal that NCAO promotes Apoptosis and restricts tumor cell migration. Additionally, it demonstrates significant antitumor efficacy in a mouse model, targeting both solid and ascitic tumors using the myeloma (Ag8) cell line. NCAO holds promise in the development of antitumor agents.</p>

INNO-220 is an orally active, CRBN-dependent molecular glue degrader that targets CK1α. By degrading CK1α, INNO-220 induces cell cycle arrest at the G0/G1 phase and triggers apoptosis (Apoptosis). It disrupts the assembly and function of the CARD11/BCL10/MALT1 complex, inhibiting the NF-κB signaling pathway in T cells and lymphoma cells with activating mutations in CARD11. INNO-220 offers a novel direction for lymphoma research.

VEGFR-2-IN-52 (compound 14d) serves as a powerful inhibitor of VEGFR-2, exhibiting an IC 50 of 191.1 nM. It effectively reduces the protein expression levels of p-VEGFR-2, MMP9, p-ERK1/2, and p-MEK1. In addition, VEGFR-2-IN-52 demonstrates cytotoxic properties by inducing apoptosis and arresting the cell cycle at the G0/G1 phase, and it enhances the levels of ROS.