Apoptosis

<p>RIPK3-IN-3 (compound 20) is a selective RIPK3 inhibitor that demonstrates potent activity with an IC50 value of 10 nM.</p>

Shepherdin 79-87: Amino acid fragment 79-87 of Hsp90/Survivin antagonist with anticancer properties.

<p>USP7-IN-9 is a potent USP7 inhibitor (IC50 = 40.8 nM), induces apoptosis, arrests RS4;11 cells, and modulates key oncoproteins.</p>

<p>HMGB1-IN-1 (compound 6) exhibits potent inhibition of NO production in RAW264.7 cells, with an IC50 of 15.9 ± 0.6 μM, and effectively disrupts the HMGB1/NF-κB/</p>

MitoEbselen-2 mitigates radiation, cuts lipid hydroperoxides, blocks cell death, and boosts survival in irradiated mice.

<p>Moracin N, a ferroptosis inhibitor derived from mulberry leaves, exhibits neuroprotective activity by mitigating oxidative stress [1].</p>

<p>VEGFR-2-IN-68 (13b) is an inhibitor of VEGFR-2 with an IC50 value of 41.51 nM. It can induce apoptosis and cause G2/M cell cycle arrest, as well as exhibit anti-cancer metastasis properties.</p>

<p>Ferumoxytol is an iron oxide nanoparticle with anti-leukemia properties, specifically against acute myeloid leukemia (AML) cells with low ferroportin (FPN) expression. By increasing intracellular iron levels, Ferumoxytol induces the Fenton reaction to produce reactive oxygen species (ROS), resulting in oxidative stress and ferroptosis. It selectively kills leukemia cells with low FPN expression while sparing normal cells, making it useful for studying leukemia targeting iron metabolism abnormalities.</p>

MS78, an acetylation targeting chimera (AceTAC), specifically acetylates the p53Y220C mutant by recruiting the histone acetyltransferase p300/CBP.

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

<p>DS-5272 is a potent and orally active inhibitor of p53-MDM2 interaction.</p>

<p>hCAIX-IN-23 (Compound 27) is a human carbonic anhydrase (hCA) inhibitor with Ki values of 10.4 nM for hCA IX and 8.5 nM for hCA XII. It not only inhibits hCA activity but also releases NO, exerting dual anti-tumor effects. By reducing the expression of hCA IX and iron regulatory proteins, hCAIX-IN-23 regulates mitochondrial caspase activity and the ferroptosis pathway, thereby inducing apoptosis. This compound is utilized in research focused on renal cancer.</p>

<p>iNOs-IN-5 (Compound BN-4) is an inhibitor of iNOS with an IC50 value of 0.1707 μM, effectively reducing NO expression in RAW264.7 cells stimulated by LPS (HT-D1056). It further diminishes the expression of ROS and lactate dehydrogenase induced by hypoxic injury, displaying anti-necrotic and anti-apoptotic properties. In an SD rat model, iNOs-IN-5 exhibits neuroprotective effects against cerebral ischemia and is capable of crossing the blood-brain barrier.</p>

<p>Relfovetmab is an anti- NGF monoclonal antibody (mAb) [1] .</p>

Fuscin, a quinonoid from O. fuscum, inhibits ADP/ATP translocase, depletes glutathione, disrupts NADH oxidation, and blocks MIP-1α/CCR5 binding (IC50: 21µM).

<p>Cuprichydroxide exhibits inhibitory activity against Ralstonia solanacearum and A549 cells and has acute pulmonary toxicity.</p>

<p>NCT-58 is a potent HSP90 inhibitor that blocks Akt, downregulates HER family, and induces apoptosis in HER2+ breast cancer without triggering HSR.</p>

KWCN-41, a RIPK1 inhibitor with 88 nM IC50, blocks necrosis, spares apoptosis, and is anti-inflammatory.

Lisaftoclax, an oral Bcl-2/Bcl-xl inhibitor (IC50: 2 nM & 5.9 nM), treats CLL by promoting leukemia cell death.

<p>TNF-α-IN-6 is an orally efficacious allosteric inhibitor of TNFα ( K D = 6.8 nM).</p>

<p>A unique collection of 420 compounds targeting PI3K/Akt/mTOR signaling for research in PI3K/Akt/mTOR signaling, and drug discovery in diseases involved with</p>

Theophyllol (theophylline sodium acetate) can alter calcium levels in subcellular fractions of rat brain cortex.

<p>CDK9-IN-36 (Compound T7) is a potent, selective, and metabolically stable CDK9 inhibitor with an IC50 value of 1.2 nM. It effectively suppresses the proliferation of Osimertinib-resistant NSCLC cells by downregulating Mcl-1, reducing colony formation, and inducing apoptosis. Additionally, CDK9-IN-36 exhibits antitumor activity in xenograft models.</p>

<p>Scr-IN-1 (Compound 4e) is a tyrosine kinase inhibitor demonstrating inhibitory activity against HCT-116 and MIA-PaCa-2 cells, with IC50 values of 0.16 μM and 1.16 μM, respectively. It shows selectivity towards HCT-116 cells and MIA-PaCa-2 cells, with a selectivity index (SI) greater than 625 and 86. Scr-IN-1 induces apoptosis in HCT-116 colon cancer cells without altering the proportion of necrotic cells and is a potential novel SRC kinase inhibitor for HCT-116 cells. This compound is suitable for cancer research.</p>

Antitumor agent-61, a potent Irinotecan derivative, exhibits IC50s of 0.92-3.23 μM in 6 cancer cells, inducing apoptosis via mitochondrial pathways.

<p>KSRP-IN-1 (compound 8) acts as an inhibitor of KSRP, inducing cell cycle arrest and apoptosis (Apoptosis). This compound demonstrates antitumor activity.</p>

<p>Tubulin polymerization-IN-76 (compound 20b) is a potent and orally active inhibitor of tubulin polymerization. It acts at the colchicine binding site to inhibit tubulin polymerization with an IC50 value of 2.505 μM, effectively disrupting the intracellular microtubule network and interfering with mitosis. Tubulin polymerization-IN-76 shows significant inhibitory effects on MGC-803 and HGC-27 cells, with IC50 values of 1.61 and 1.82 nM, respectively. It effectively suppresses colony formation and cell migration activities in these cell lines, inducing G2/M phase cell cycle arrest and apoptosis (Apoptosis). Furthermore, Tubulin polymerization-IN-76 exhibits broad-spectrum antiproliferative activity.</p>

<p>Apoptosisinducer 28 (Compound X1) is an apoptosis inducer with demonstrated in vitro anticancer activity. It arrests the cell cycle at the G1 phase, promoting cell death and inducing apoptosis by disrupting the mitochondrial membrane potential.</p>

Thalidomide-O-PEG4-NHS ester is a polyethylene glycol (PEG)-based linker, commonly employed for the synthesis of proteolysis-targeting chimeras (PROTACs)[1].

<p>EM 163是一种 TIR-TIR 相互作用抑制剂，它是MyD88蛋白的TIR（Toll/白细胞介素-1受体）结构域拟态。EM 163针对IL-1受体中的TIR 结构域，阻断与MyD88的相互作用。EM 163抑制葡萄球菌肠毒素B（SEB）引起的体内炎症细胞因子的产生。EM 163能保护小鼠免受SEB 冲击引起的死亡。在体外的大鼠海马神经元中，EM 163阻断p38的激活和IL-1β对化学诱导的长期电位（LTP）引发的蛋白质合成的抑制作用。</p>

<p>Etoposide phosphate disodium, a prodrug of etoposide, is a powerful anticancer drug inhibiting DNA topoisomerase II.</p>

<p>EPZ020411 hydrochloride is a selective and potent small molecule PRMT6 inhibitor with an IC50 value of 10 nM.</p>

<p>NYY-6a is a ferroptosis (Ferroptosis) inhibitor, demonstrating significant suppression of RSL3-induced ferroptosis in 786-O and HT-1080 cells, with EC50 values of 52 nM and 50 nM, respectively. As a radical-trapping antioxidant (RTA), NYY-6a effectively reduces lipid peroxidation, comparable to ferrostatin-1 and liproxstatin-1, making it useful for research into ferroptosis-related pathologies.</p>

<p>CQ1373 is a potent RET inhibitor that demonstrates cellular activity against BaF3 cells expressing CCDC6-RET, CCDC6-RET-G810C, and CCDC6-RET-G810R, with IC50 values of 13.0, 25.7, and 28.4 nM, respectively. It shows excellent selectivity for wild-type RET and solvent front mutants G810C/R, with IC50 values of 4.2, 7.1, and 32.4 nM. CQ1373 inhibits RET phosphorylation and downstream signaling through SHC. Additionally, it induces apoptosis (Apoptosis) and cell cycle arrest in BaF3 cells. CQ1373 possesses antitumor efficacy, making it a candidate for cancer research.</p>

HDAC6degrader-5 (Compound 6) exhibits inhibitory and degradative activity against HDAC6, with an IC50 of 4.95 nM and a DC50 of 0.96 nM. It suppresses the release of TNF-α, IL-1β, and IL-6, and prevents apoptosis in liver cells. Additionally, HDAC6degrader-5 demonstrates anti-inflammatory properties in a mouse model of APAP-induced liver injury.

<p>OA-Br-1 is an orally active, selective inhibitor of PTP1B with an IC50 value of 7.08 μM. It induces apoptosis and exhibits broad-spectrum anti-cancer cell proliferation activity. OA-Br-1 exerts anti-breast cancer effects both in vitro and in vivo through the PTP1B/PI3K/AKT signaling pathway.</p>

SHP1 activator 1 (Compound 3n) is an activator of protein tyrosine phosphatase 1 containing the src homology-2 domain (SHP1), with an EC50 of 17.66 μM. It inhibits the proliferation of ABC-DLBCL cells and induces apoptosis by suppressing the STAT3 signaling pathway. In MDA-MB-231 cells, SHP1 activator 1 emits blue and green fluorescent signals, making it suitable as a cellular imaging agent.

PROTAC CARM1/IKZF3 degrader-1 (Compound 074) inhibits CARM1, reducing the methylation level of its substrate BAF155. This PROTAC degrader works by degrading IKZF 1/3 via a CRBN-dependent mechanism. It suppresses MYC protein expression, thereby inhibiting the proliferation of various multiple myeloma cells. Additionally, PROTAC CARM1/IKZF3 degrader-1 can induce apoptosis in H929 cells and overcomes resistance to immunomodulatory drugs (IMiDs, such as pomalidomide). It is applicable for cancer and immunology research. (Pink: ligand for target protein CARM1/IKZF3 ligand 1; Active form of target protein ligand: EZM 2302; Black: linker; Blue: ligand for E3 ligase Cereblon Thalidomide 4-fluoride)

ReACp53 acetate could inhibit p53 amyloid formation and rescue p53 function in cancer cell lines.

<p>NF-κB-IN-19 (Compound 8) is an NF-κB inhibitor. It effectively induces DNA damage in tumor cells through the NF-κB signaling pathway and promotes the production of reactive oxygen species (ROS), as well as induces autophagy and apoptosis. Additionally, NF-κB-IN-19 inhibits levels of VEGF and HIF-1α, exerting antiproliferative effects in tumor cells through the PI3K/AKT and STAT-3 pathways. It is also effective in overcoming cisplatin resistance and exhibits antitumor activity.</p>

<p>EGFR/COX-2-IN-1 is an EGFR/COX-2 inhibitor that effectively targets EGFRWT, EGFRT790M, COX-1, and COX-2 with IC50 values of 0.12, 0.076, 20.1, and 1.52 μM, respectively. It inhibits MCF-7, HT-29, and A-549 cells with IC50 values of 1.20, 5.14, and 14.81 μM, respectively. The compound induces apoptosis by upregulating Bax protein and downregulating Bcl-2 protein levels. Additionally, EGFR/COX-2-IN-1 significantly increases the proportion of cells in the G2/M phase in MCF-7 cells, demonstrating a broad-spectrum antitumor effect.</p>

Thalidomide-O-amido-C8-NH2 hydrochloride, a synthetic cereblon ligand-linker for PROTAC synthesis.

BM-1244 is a potent Bcl-xL/Bcl-2 inhibitor with Kis of 134 and 450 nM for Bcl- xL and Bcl-2, respectively.

<p>(R)-Q-VD-OPh is the less active enantiomer of Q-VD-OPha. Q-VD-OPha is an irreversible inhibitor of pan-caspase, with potent antiapoptotic properties.</p>

<p>EGFR/VEGFR2-IN-1 (Compound 10e) serves as an inhibitor for VEGFR-2 and EGFR, with respective IC50 values of 0.26 and 0.14 μM. It inhibits microtubule protein polymerization with an IC50 of 40.9 μM and induces cell apoptosis (Apoptosis). EGFR/VEGFR2-IN-1 is applicable in research related to anti-leukemia and anti-lymphoma treatments.</p>

<p>Thailanstatin D blocks AR-V7 splicing, disrupts U2AF65/SAP155 binding, and induces apoptosis in CRPC xenografts.</p>

<p>PROTAC 20S proteasome subunit β5 degrader 1 (compound 12f) serves as a targeted degrader of the 20S proteasome subunit β5, exhibiting a DC50 value of 0.11 μM in FaDu cells. This compound disrupts the cell cycle and promotes apoptosis (apoptosis), while inhibiting cell proliferation and migration in both FaDu and KM3/BTZ cells. It is applicable for research into resistance to Bortezomib in pharyngeal carcinoma and multiple myeloma.</p>

<p>Cathepsin B, a cysteine protease located within the subcellular endosomes and lysosomal compartments, mediates apoptosis and can be used in cancer research.</p>

P53R3 is a potent reactivator of p53, effectively restoring sequence-specific DNA binding to several p53 hot spot mutants, namely p53 R175H, p53 R248W, and p53

<p>PCC0208017 is an inhibitor of MARK3 and MARK4 with IC50s of 1.8 and 2.01 nM. PCC0208017 disrupts microtubule dynamics and displays potent antitumor activity.</p>