Apoptose

<p>Anticancer Agent 118, an N‑acylated ciprofloxacin derivative, exhibits antibacterial efficacy against Gram-positive strains and antiproliferative effects on</p>

<p>Ponicidin, a diterpenoid from Rabdosia rubescens, has immunoregulatory, anti-inflammatory, anti-viral, and anti-cancer properties.</p>

<p>APE1-IN-2 (AP1), a Pt(IV) proagent, targets APE1 protein, induces DNA damage, and triggers apoptosis with anticancer effects.</p>

<p>(+)-Apogossypol is an antagonist of pan-BCL-2. (+)-Apogossypol binds to Mcl-1(Bcl-2 and Bcl-xL with EC50s of 2.6, 2.8 and 3.69 μM, respectively).</p>

<p>YS-363 is a potent, selective, and orally active inhibitor of the epidermal growth factor receptor (EGFR), exhibiting half-maximal inhibitory concentrations (</p>

<p>BHD, a reversible male contraceptive agent, effectively induces spermatogenic cell apoptosis and causes abnormalities in seminiferous tubules in vivo at doses</p>

<p>eIF4A3-IN-18, a silvestrol analogue with EC50s: 0.8/35/2 nM, inhibits eIF4F complex and is cytotoxic (LC50: 0.06 nM) for cancer research.</p>

<p>NSC 689534 forms a chelate with copper (Cu 2+), resulting in the NSC 689534/Cu 2+ complex, which is a potent inducer of oxidative stress and exhibits antitumor activity [1].</p>

<p>RMC-4998 is an orally available KRASG12C mutant inhibitor that targets the active or GTP-bound state of the KRASG12C mutant,inhibit ERK and apoptosis.</p>

<p>K145 hydrochloride is a selective sphk2 inhibitor with substrate competitiveness and oral activity, with IC50 of 4.3 µM and Ki of 6.4 µM.</p>

<p>RET-IN-5 is a potent inhibitor of RET (IC50: 4.57 nM).</p>

<p>Immuno modulator-1 (compound 22) effectively suppresses the secretion of TNFα and IL-2 in human peripheral blood mononuclear cells (hPBMC) with IC50 values of 4</p>

<p>HDAC-IN-46 inhibits HDAC1 &amp; HDAC6, affects p-p38, Bcl-xL &amp; cyclin D1, blocks G2 phase &amp; induces apoptosis in TNBC research.</p>

<p>AGN194204 (IRX4204), an oral RXR agonist, inactive against RAR, has Kd 0.4-3.8 nM &amp; EC50 0.08-0.8 nM, with anti-inflammatory and anticarcinogenic properties.</p>

<p>LSD1-IN-25: potent, selective oral LSD1 inhibitor; IC50=46 nM, Ki=30.3 nM; induces cancer cell apoptosis.</p>

<p>FOXO1-IN-3 is a highly-selective, orally active inhibitor of FOXO1 that diminishes hepatic glucose production and enhances insulin sensitivity and glucose</p>

Docebenone is a selective and orally active inhibitor of 5-LO.

<p>SM-1295: IAP antagonist, Kd 3077 nM XIAP-BIR3, 3.2 nM c-IAP1-BIR3, 9.5 nM c-IAP2-BIR3.</p>

<p>GGTI2417 blocks Geranylgeranyltransferase I, targeting RalB for apoptosis and RalA to stop growth.</p>

<p>BTM-3566 triggers ISR via OMA1, induces apoptosis in cancer cells, and is used to research DLBCL.</p>

<p>Eeyarestatin I blocks ER protein degradation, hinders p97/atx3 processes, and induces anticancer proteins.</p>

(S)-Verapamil hydrochloride is an inhibitor of leukotriene C4 (LTC4) and calcein transport by MRP1,and leads to the death of potentially resistant tumor cells.

<p>c-Met/HDAC-IN-3: dual inhibitor; IC50: c-Met 12.5 nM, HDAC1 26.97 nM; induces apoptosis, G2/M arrest.</p>

<p>MTP, a PKM2 inhibitor, promotes apoptosis in cancer cells via caspase-3 activation while also inducing autophagy and enhancing ROS generation.</p>

<p>RET-IN-25 (compound 6b) is an anticancer RET kinase inhibitor that demonstrates efficacy against medullary thyroid carcinoma (MTC), exhibiting half-maximal</p>

<p>HM90822 is an IAP antagonist that inhibits XIAP and cIAP1/2 protein expression, induces IAP ubiquitination and promotes proteasome-dependent IAP degradation.</p>

<p>Ac-Val-Ala-Asp-CHO (Ac-VAD-CHO) serves as a pan-caspase inhibitor and preserves mitochondrial membrane potential (MMP) while preventing the release of</p>

<p>NHWD-870 selectively inhibits BET bromodomains BRD2-4, BRDT; potent anti-cancer effect by inducing apoptosis, halting cell growth.</p>

<p>WYE-125132: potent mTOR inhibitor, IC50 0.19 nM, selective over PI3Ks/hSMG1/ATR.</p>

<p>13h (hGGPPS-IN-3), a strong C2-ThP-BPs hGGPPS blocker, triggers MM cell apoptosis and shows in vivo anti-myeloma effects.</p>

<p>Protein kinase D (PKD), a serine/threonine protein kinase activated by diacylglycerol downstream of PKC signaling, has three human isoforms that modulate cell proliferation, survival, invasion, and protein transport. CRT0066101 acts as an inhibitor of these three PKD isoforms, with IC50 values of 1, 2.5, and 2 nM for PKD1, PKD2, and PKD3, respectively. It demonstrates selectivity for PKD over a range of more than 90 protein kinases, including PKCα, PKBα, MEK, ERK, c-Raf, c-Src, and c-Abl. This specificity allows CRT0066101 to inhibit cell proliferation, induce apoptosis, and notably reduce the viability of pancreatic cancer cells both in vitro and in vivo.</p>

<p>ST1074, a dual inhibitor of CerS2 and CerS4, promotes apoptosis and is applicable in cancer research [1].</p>

<p>IK-862 is a selective TACE inhibitor with potential anti-inflammatory and anticancer activity for the study of neuritis.</p>

<p>CDKI-83, a potent CDK9 inhibitor, inhibits tumor growth with GI50 &lt;1μM and triggers apoptosis in A2780 cells, showing promise as an anti-cancer agent.</p>

<p>MRT199665, a selective MARK/SIK/AMPK inhibitor, blocks SIK CRTC3 S370 phosphorylation and triggers apoptosis in AML cells.</p>

<p>Bcl-2-IN-11 (compound 6) is a potent and selective inhibitor of Bcl-2 activity, exhibiting an IC50 of 0.9 nM, and demonstrates minimal inhibition against Bcl-xl</p>

<p>Fasnall, a fatty acid synthase (FASN) inhibitor, exhibits an IC50 of 3.71 μM against the human recombinant enzyme. It halts tritiated acetate incorporation into lipids (IC50= 5.84 μM), boosts ceramide levels, and triggers lipid droplet formation in BT474 HER2+ breast cancer cells. Demonstrating antiproliferative effects on various breast cancer cell lines, including non-tumorigenic MCF-10A and tumorigenic MCF-7, MDA-MB-468, BT474, and SK-BR-3, its efficacy is directly linked to FASN expression in vitro. In murine models of HER2+ breast cancer, particularly the MMTV-Neu model, Fasnall significantly reduces tumor volume and extends survival. Furthermore, it enhances the efficacy of carboplatin in vivo, bolstering the objective response rate of stable disease from 25% with carboplatin alone to 88% when paired with Fasnall.</p>

<p>HDAC/JAK/BRD4-IN-1 (compound 25ap) is a potent triple inhibitor targeting HDAC, JAK, and BRD4.</p>

<p>SC 67655 is a peptidomimetic that specifically suppresses human leukocyte antigen DRB10401-restricted T cell proliferation.</p>

<p>15-Deoxy-Δ12,14-Prostaglandin A1, a deoxyanalog of prostaglandins, inhibits NF-κB signaling and induces apoptosis. It also prevents TNF-α-induced upregulation of inflammatory endothelial cell adhesion molecules (CAM) and reduces monocyte arrest [1].</p>

<p>Merodantoin induces apoptosis in KRAS-mutant cancer cells via ROS-autophagy and Akt pathway.</p>

<p>RIPK-IN-4 is an effective and selective inhibitor of RIPK2. It also has excellent oral bioavailability (IC50: 3 nM).</p>

<p>Agerafenib hydrochloride is a highly potent inhibitor of BRAFV600E (Kd: 14 nM).</p>

<p>Antitumor agent-60 inhibits growth by targeting RAS-RAF, binding CRAF (Kd: 721.3 nM), boosting p53/ROS, causing apoptosis, and arresting G2/M phase.</p>

<p>Compound 37b3, an anticancer, halts tumor growth, triggers cell death, and pairs with Trastuzumab to form T-PBA, an ADC with targeted delivery.</p>

<p>Ro 41-5253 is a RARα antagonist with antitumor activity that inhibits the proliferation of ZR-75.1 estrogen receptor-positive breast cancer cells.</p>

<p>SWS1, a d-(+)-biotin-conjugated PD-L1 inhibitor (IC50: 1.8 nM), displays anticancer activity by augmenting tumor-infiltrating lymphocytes and demonstrating anti</p>

<p>IM156, a Metformin derivative, activates AMPK, enhances cognition in aging animals, and inhibits OXPHOS in solid tumor research.</p>

<p>RIPK1-IN-10 is a potent inhibitor of RIPK1.</p>

<p>Met-F-AEA is a metabolically stable analogue of anandamine that exhibits antitumor activity by inhibiting cell growth through the activation of apoptosis [1].</p>