Apoptose

<p>CSN5-IN-2 (Compound 31) is a CSN5 inhibitor with an IC50 of 0.36 μM. It increases Cullin 1 neddylation levels in cancer cells and downregulates the expression of RAD51 and PD-L1. CSN5-IN-2 exhibits antitumor activity, which is enhanced when used in combination with Talazoparib.</p>

<p>HDAC-IN-88 (Compound HJ-9) is a potent inhibitor of HDAC, effectively targeting HDAC6, HDAC1, HDAC2, HDAC8, and HDAC3 with IC50 values of 0.226, 1.103, 2.308, 3.255, and 3.864 μM, respectively. This compound suppresses the proliferation of cancer cells HepG2, HCT116, and MV4-11 with IC50 values of 5.47, 9.78, and 0.38 μM, respectively. Additionally, it inhibits the migration of HCT116 cells, causes cell cycle arrest at the G0/G1 phase, and induces apoptosis and autophagy in MV4-11 cells. HDAC-IN-88 reduces ROS levels and mitochondrial membrane potential and demonstrates antimalarial activity by inhibiting Plasmodium falciparum 3D7 with an EC50 of 165 nM. Furthermore, HDAC-IN-88 exhibits anti-angiogenic properties.</p>

<p>RET Ligand-Linker Conjugate-1 consists of a complex formed by a RET ligand and a linker, which can be utilized in the synthesis of QZ2135.</p>

<p>EGFR-IN-144 (Compound 4B) inhibits EGFR (IC50=0.639 µg/mL) and tubulin polymerization (IC50=7.339 µg/mL). It exhibits cytotoxicity in various cancer cells with a GI50 at the nanomolar level. EGFR-IN-144 reduces the expression of mTOR, TNF-α, and IL-6, causes G1/S phase cell cycle arrest, and induces apoptosis.</p>

<p>Tebentafusp (IMCgp100) is a protein that targets gp100 with potential anti-tumor activity.</p>

<p>Tubulin polymerization-IN-72 (Compound 4a4) is a microtubule synthesis inhibitor with anticancer properties. By binding to the colchicine site, it disrupts the polymerization of tubulin, resulting in the arrest of cancer cells at the G2/M phase and inducing apoptosis (Apoptosis). The IC50 for its activity against cancer cells is 0.4-2.7 nM.</p>

<p>Necroptosis-IN-5 (Compound 26) is an orally active inhibitor of necroptotic cell death (necroptosis). This compound also exhibits potent inhibitory activity against receptor-interacting protein kinase 1 (RIPK1). It can be utilized in research related to inflammatory diseases, neurodegenerative disorders, and cancer associated with necroptosis.</p>

<p>STAT3-D11-PROTAC-VHL (Compound D11-PROTAC) is a PROTAC degrader targeting signal transducer and activator of transcription 3 (STAT3). It demonstrates anti-tumor activity with IC50 values of 1335 nM in HeLa cells and 1973 nM in MCF-7 cells. The compound binds to the DNA binding domain of STAT3, recruits the E3 ligase VHL to form a ternary complex, leading to ubiquitination and subsequent proteasomal degradation of STAT3. Additionally, STAT3-D11-PROTAC-VHL inhibits tumor cell growth, induces cell cycle arrest and apoptosis (apoptosis), and suppresses tumor immune evasion.</p>

<p>Siomycin A: thiopeptide antibiotic, selectively inhibits FOXM1, anti-tumor, induces apoptosis.</p>

<p>Necroptosis-IN-4 is an effective inhibitor of necroptosis, specifically targeting RIP kinase 1 (RIPK1) without inhibitory activity against RIPK3. It exhibits weak inhibitory effects on VEGFR1/2 and PDGFR-α.</p>

<p>5-Fluorouracil-13C,15N2 is a standard for quantifying 5-fluorouracil via GC/LC-MS and blocks DNA synthesis, causing cell apoptosis.</p>

<p>YB-0158 inhibits Wnt, targets colorectal CSCs, disrupts Sam68/Src, induces apoptosis, and has anti-cancer properties.</p>

<p>BGC4 is a gold(III) complex based on biphenyl. It inhibits human recombinant thioredoxin reductase (TrxR) with an IC50 of 10.7 μM, exhibits cytotoxicity with an IC50 of 5.4 μM in MDA-MB-231 cells, and induces apoptosis. Additionally, BGC4 demonstrates antitumor activity in mouse models.</p>

<p>CDC20-IN-2 (14c) is an inhibitor of Cdc20 with a KD of 7.65 μM, inducing G2/M phase arrest, promoting DNA damage accumulation, and stabilizing key substrates such as Cyclin B1 and Bim. This leads to enhanced apoptosis, as well as inhibition of tumor cell proliferation and migration.</p>

<p>Atibuclimab is a chimeric monoclonal antibody targeting CD14, consisting of a mouse variable region and a human IgG4 Fc region.</p>

<p>PD-L1 inhibitor IV, a polypeptide, competitively blocks hPD-1 with a Kd of 1.38 μM, preventing hPD-1/hPD-L1 interaction.</p>

<p>TRK-IN-30 (Compound C11) is an inhibitor of tropomyosin receptor kinases (TRK), effectively inhibiting TRKA, TRKB, TRKC, and the resistant mutant TRKAG595R, with IC50 values of 1.8, 0.98, 3.8, and 54 nM, respectively. It also suppresses the activation of downstream PI3K/AKT and MEK/ERK signaling pathways. TRK-IN-30 hinders colony formation and cell migration of Km-12, induces cell cycle arrest at the G0/G1 phase, and triggers apoptosis in Km-12 cells.</p>

<p>(+)-Mcl-1 inhibitor 21 (Example 1-37) is a chemical compound that acts as an Mcl-1 inhibitor with an IC50 value of 172 nM. It demonstrates pro-apoptotic and antiproliferative activities in SUDHL5 and SUDHL10 cell lines, making it useful for cancer research.</p>

<p>MitoTam bromide hydrobromide is an electron transport chain (ETC) inhibitor.</p>

<p>TopoisomeraseIIα-IN-10 (Compound 13r) is a topoisomerase IIα inhibitor that binds to the active site of DNA when complexed with topoisomerase IIα. This binding is stabilized through interactions with DNA base pairs and amino acid residues. By intercalating into DNA, TopoisomeraseIIα-IN-10 induces apoptosis and disrupts the mitochondrial membrane potential in HCT116 cells, effectively inhibiting their growth with an IC50 of 4.37 μM. It is applicable for cancer research studies.</p>