Apoptosi

<p>HDAC-IN-84 (compound 4a) is a potent HDAC inhibitor with IC50 values of 0.0045, 0.015, 0.013, 0.038, 5.8, and 26 μM for HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, and HDAC11, respectively. It effectively inhibits the proliferation of leukemia cells without causing toxicity.</p>

<p>LD4172 is a PROTAC degrader capable of degrading RIP kinase (RIPK1) with a DC50 in the nanomolar range. When used in combination with TNF-α, LD4172 can induce apoptosis in B16F10 cells. In mouse models, it demonstrates antitumor activity. (Pink: ligand for target protein; Black: linker; Blue: ligand for E3 ligase VHL)</p>

<p>HPCR exhibits antiproliferative activity against various cancer cells and is involved in apoptosis (apoptosis).</p>

<p>KT-253 is a p53 stabilizer and a PROTAC degrader of MDM2 (DC50=0.4 nM). It inhibits the proliferation of cancer cells RS4;11 with an IC50 of 0.3 nM, induces cell cycle arrest in the G2/M phase, and triggers apoptosis. In mouse models, KT-253 demonstrates antitumor activity. (Pink: ligand for target protein MDM2 ligand 4; Black: linker; Blue: ligand for E3 ligase cereblon)</p>

<p>TRF2-IN-1 (compound F2) is a potent inhibitor of telomere repeat-binding factor 2 (TRF2). It exhibits antiproliferative activity and induces apoptosis. TRF2-IN-1 binds directly to the TRF2TRFH domain, selectively inhibiting TRF2 protein expression and telomere localization. Additionally, TRF2-IN-1 possesses anticancer properties and shows potential for osteosarcoma research.</p>

<p>PROTAC LZK-IN-1 (Compound 21A) is a PROTAC molecule that targets the degradation of LZK (leucine zipper kinase, encoded by MAP3K13). At a concentration of 10 μM, PROTAC LZK-IN-1 facilitates the degradation of LZK and inhibits the expression of p53 and c-MYC, leading to reduced viability of global head and neck squamous cell carcinoma (HNSCC) cell lines. This compound is applicable in anticancer research.</p>

<p>Antioxidant agent-20 (Compound 3d) exhibits potent anti-inflammatory and antioxidant activities. It reduces reactive oxygen species (ROS) and apoptosis in a dose-dependent manner. Antioxidant agent-20 demonstrates photoprotective effects on UVB-exposed human skin keratinocytes (HaCaT) (IC50=5.13 µM) by activating Nrf2/HO-1 signaling and inhibiting the NF-κB pathway.</p>

<p>Mitochondria modulator-2 (Compound Ir1) induces depolarization of the mitochondrial membrane potential, generates reactive oxygen species (ROS), inhibits the migration of A549 cells, causes cell cycle arrest at the G2/M phase, and triggers apoptosis in A549 cells.</p>

<p>EGFR-IN-143 (Compound 5f) is a potent EGFR inhibitor with an IC50 value of 0.15 μM. It induces apoptosis by arresting the cell cycle at the G2/M phase and exhibits antitumor activity.</p>

<p>MDM2ligand 4 is a ligand of MDM2 and can be used in the synthesis of the PROTAC degrader [KT-253].</p>

<p>FLT3-IN-28 (Compound 12y) is an orally active FLT3 inhibitor with antitumor properties. It selectively targets cancer cells with FLT3 internal tandem duplication (ITD) mutations, demonstrating IC50 values of 85, 290, 130, 65, and 220 nM against BaF3-FLT3-ITD, BaF3-TEL-VEGFR2, MV4-11, MOLM-13, and MOLM-14 cell lines, respectively. These lines include acute myeloid leukemia (AML) cells harboring FLT3-ITD mutations such as MV4-11 and MOLM-13/14. The compound also reduces phosphorylation levels of FLT3 and STAT5 in MOLM-13 cells, leading to cell cycle arrest and apoptosis. With an oral bioavailability of 19.2% in SD rats, FLT3-IN-28 extends survival in a dose-dependent manner in MOLM-13 xenografted NSG mouse models. It holds promise for research in FLT3-ITD-related cancer studies.</p>

<p>Diethyl phthalate disrupts endocrine and induces apoptosis in PC12 cells; common in plastics, personal care items.</p>

<p>ARV-393 HCl is an orally active and potent PROTAC targeting BCL6 with antitumor activity for the study of non-Hodgkin's lymphoma.</p>

<p>Thiocolchicine inhibits tubulin polymerization (IC50: 2.5 µM, Ki: 0.7 µM), induces apoptosis, and serves as an ADC cytotoxin.</p>

<p>PLD-IN-1 (Compound 3r) is an orally effective inhibitor of phospholipase D (phospholipaseD) with an IC50 of 1.97 μM. It reduces the expression of CD24, CD47, and PD-L1 while enhancing the expression of calreticulin, thereby modulating the immune evasion mechanisms of lung cancer cells by promoting the phagocytosis of cancer cells by macrophages. PLD-IN-1 inhibits the viability of lung cancer cell lines A549, HCC44, H460, and HCC15 with IC50 values of 18.44, 22.31, 24.85, and 21.45 μM, respectively. It induces apoptosis (apoptosis) in A549 cells and inhibits cell migration. Additionally, PLD-IN-1 increases pro-inflammatory M1 macrophage levels and decreases anti-inflammatory M2 macrophage levels, exhibiting anti-tumor activity in mouse models.</p>

<p>Asaretoclax is an effective inhibitor of B-cell lymphoma 2 (Bcl-2), demonstrating potential for use in cancer research.</p>

<p>EGFR-IN-131 (compound 3a) is an efficacious EGFR inhibitor capable of crossing the blood-brain barrier, with an IC50 value of 272.9 nM. This compound exhibits anti-proliferative activity, induces cellular apoptosis (apoptosis), and causes cell cycle arrest in the G0/G1 phase. Additionally, EGFR-IN-131 reduces the protein expression of p-EGFR.</p>

<p>PRMT5-IN-45 (compound 36) is a potent and selective inhibitor of PRMT5, exhibiting an IC50 value of 3 nM. This compound effectively reduces the levels of symmetrical dimethylarginine (sDMA) and inhibits the proliferation of the MOLM-13 cell line by inducing apoptosis and causing cell cycle arrest.</p>

<p>SZU-B6, a PROTAC degrader, targets and degrades SIRT6 with DC50 values of 45 nM in SK-HEP-1 cells and 154 nM in Huh-7 cells. It inhibits the proliferation of SK-HEP-1 cells with an IC50 of 1.51 μM and suppresses colony formation in both SK-HEP-1 and Huh-7 cell lines. Additionally, SZU-B6 induces apoptosis in SK-HEP-1 cells and causes cell cycle arrest at the G2/M phase. It demonstrates anti-tumor activity in murine models.</p>

<p>STK17A/B-IN-1 hydrochloride is a potent, selective, orally active inhibitor of STK17A/B, displaying an IC50 value of 23 nM against STK17A. It is utilized in the research of tumors.</p>

<p>CQ-ER is a Coumarin-quinazolinone-based photosensitizer targeting the endoplasmic reticulum (ER). It induces ferroptosis, thereby enhancing photodynamic therapy (PDT).</p>

<p>LBM22, a CLK2 inhibitor, exhibits an IC50 value of 3.9 nM. It possesses anti-proliferative properties by inhibiting the phosphorylation of SR proteins. Additionally, LBM22 downregulates the expression of Wnt-related proteins and anti-apoptotic proteins, making it applicable in the study of non-small cell lung cancer.</p>

<p>Bfl-1-IN-5 (Compound (R,R,S)-26) is a selective inhibitor of Bfl-1, demonstrating an IC50 of 0.022 μM. This compound enhances the activity of caspase-3/7, with an EC50 of 0.37 μM, and also inhibits the viability of SU-DHL-1 cells, showing an EC50 of 1.3 μM.</p>

<p>PROTAC EZH2 Degrader-3 (compound ZJ-20) is a potent EZH2 degrader that exhibits strong inhibitory effects not only on EZH2 protein expression but also on the levels of other PRC2 subunits and H3k27me3 protein. Additionally, PROTAC EZH2 Degrader-3 demonstrates antiproliferative activity by blocking the cell cycle at the G0-G1 phase and inducing apoptosis (cell death). At a concentration of 5 μM and over a period of 24 hours, it effectively suppresses the expression of these critical proteins involved in cell regulation and growth.</p>

<p>DH-18 is an inhibitor of matrix metalloproteinase-2 (MMP-2), exhibiting IC50 values of 139.45 nM for MMP-2, 518.11 nM for MMP-9, and 833.34 nM for MMP-8. The compound promotes cell apoptosis and causes cell cycle arrest in the G0/G1 phase. DH-18 also inhibits cell growth, making it potential for research in chronic myeloid leukemia.</p>

<p>CDK-TCIP1 is a bivalent molecule that links the CDK9 inhibitor SNS-032 with the BCL6 ligand BI3812. It effectively and specifically kills cells overexpressing BCL6, with an EC50 of 7.7 nM for SUDHL5 cells.</p>

<p>TOPOI/PARP-1-IN-2 (compound 6c) serves as a dual inhibitor targeting both PARP-1 and topoisomerase 1 (TOPO-1), with IC50 values of 32.2 nM and 46.2 nM, respectively. This compound exhibits greater selectivity for PARP-1 over PARP-2. Additionally, TOPOI/PARP-1-IN-2 disrupts the S phase of the cell cycle and induces apoptosis in the NCI-60 cancer cell lines.</p>

<p>HSP90-IN-33 (compound 24e) is an effective Hsp90 inhibitor, demonstrating dissociation constants (Kd) of ≥200 µM for Hsp90α and 7.3 µM for Hsp90β. This compound induces cellular apoptosis (apoptosis) and arrests the cell cycle at the G0/G1 phase. Additionally, HSP90-IN-33 reduces the protein expression of ERα, CDK4, and Akt.</p>

<p>Barakol, a primary compound found in Cassia siamea, inhibits MMP-3 activity and enhances the anti-metastatic effects of doxorubicin. Additionally, Barakol induces apoptosis (Apoptosis), generates reactive oxygen species, increases the Bax/Bcl-2 expression ratio, and activates caspase-9. This compound also exhibits laxative, anti-anxiety, central nervous system depressant, antioxidant, and anticancer properties.</p>

<p>Salinomycin sodium salt (Sodium salinomycin), an antibiotic potassium ionophore, is an effective inhibitor of Wnt/β-catenin signaling.</p>

<p>AFMK (Formyl-N-acetyl-5-methoxykynurenamine) is an active metabolite of Melatonin with antioxidant and free radical scavenging activity.</p>

<p>1,2-Naphthoquinone inhibits urease, induces apoptosis in PBMC cells, inhibitory activity against hiCE, hCE1, hAChE, and hBChE.</p>

<p>Rasagiline (AGN1135) is an inhibitor of monamine oxidase used as adjunctive therapy in combination with levodopa and carbidopa in the management of Parkinsons</p>

<p>CAY10678 is an mPGES-1 inhibitor that inhibits PD-1.CAY10678 reduces collagen deposition and T-cell depletion, and may be used to study melanoma.CASHIPS</p>

<p>Cyanoacetamide has inhibitory activity against the myeloid leukaemia cell differentiation protein Mcl-1</p>

<p>(-)-Mcl-1 inhibitor 21 (Example 1-38) is an Mcl-1 inhibitor with an IC50 of 7.51 μM. It exhibits pro-apoptotic and anti-proliferative activity against SUDHL5 and SUDHL10 cell lines, making it useful for cancer research.</p>

<p>UM4118 (N-quinolin-8-ylpyridine-2-carboxamide) is a copper ion carrier used in the study of acute myeloid leukemia.</p>

<p>Flavopiridol (Alvocidib) blocks CDK1/2/4/6 by competing with ATP (IC50 ~40 nM); 7.5x selectivity over CDK7; also inhibits EGFR, PKA. In Phase 1/2 trials.</p>

<p>Macrophage-activating lipopeptide 2 TFA (MALP-2 TFA) is a diacylglycerol lipopeptide and TLR-2/TLR-6 agonist activates immune cell responses macrophages,</p>

<p>Dynorphin A is a endogenous opioid peptide and a κ-opioid receptor (KOR) agonist,a neurotransmitter and regulator in the central and peripheral nervous systems</p>

<p>Acetyl coenzyme A (Acetyl-CoA) is a pivotal molecule connecting multiple cellular metabolic pathways in the tricarboxylic acid cycle, fatty acid synthesis</p>

<p>IRF1-IN-1 (Compound I-2) is an IRF1 inhibitor , inhibiting the cleavage of Caspase 1, GSDMD, IL-1, and PARP1,protecting against skin inflammatory damage.</p>

<p>Kdo2-Lipid A ammonium (KLA) is a selective and potent TLR4 agonist, a lipopolysaccharide.Kdo2-Lipid A ammonium induces the release of TNF and PGE2.</p>

<p>SM-164 Hydrochloride: cell-permeable, binds to XIAP (BIR2/3 domains), IC50 of 1.39 nM, potent XIAP antagonist.</p>

<p>Gliotoxin, a mycotoxin, inhibits Wnt pathway, causing apoptosis in mutated colorectal cancer cells and blocks NF-κB by preserving IκB.</p>

<p>12-HETE ((±)12-HETE) is a regulator of PGE2, having both antithrombotic and prothrombotic effects.</p>

<p>BMH-7 HCl is a p53 activator, showing anti-cancer activity by activating the p53 pathway.</p>

<p>Daporinad hydrochloride (FK 866 hydrochloride) is a NAMPT inhibitor with antitumor and antiangiogenic activity that induces apoptosis in tumor cells.</p>

<p>Bcl-xL antagonist 2 is an effective and selective antagonist of Bcl-xL with an IC50 of 91 nM and a Ki of 65 nM.</p>

<p>MG-277 is a molecular glue compound transformed from PROTAC degradation agent, MG-277 potently inhibits tumor cell growth in a p53-independent manner.</p>

<p>TPP-resveratrol is a conjugate of Resveratrol and triphenylphosphine (TPP), noted for its anticancer activity. This compound enhances the efficacy of Resveratrol by facilitating its targeted delivery to mitochondria, thus inducing mitochondrial-mediated cell apoptosis (apoptosis).</p>

<p>CQ-Mito, a derivative of CQ, demonstrates excellent phototherapeutic efficacy with a PI value of 167. This compound induces cell death through mechanisms such as apoptosis and ferroptosis. It mediates mitochondrial dysfunction, characterized by alterations in mitochondrial morphology and loss of MMP. Additionally, CQ-Mito effectively inhibits tumor growth in 3D multicellular tumor spheroid models.</p>

<p>TRAP-1 (XJZ-06-462) is a p53 transcription activator that effectively activates mutant p53 and triggers the transcription of p53 target genes. In the p53Y220C pancreatic cell line, TRAP-1 rapidly upregulates p21 and other p53 target genes. TRAP-1 also inhibits cell proliferation, exhibiting IC50 values of 3.94 μM and 0.531 μM in BxPC-3 and A549 cell lines, respectively. Additionally, TRAP-1 modulates autophagy in lung cancer cells and provides protection against oxidative stress and apoptosis.</p>

<p>Prinaberel (ERB-041) is an effective and selective ERβ agonist and &gt;200-fold selective for ERβ.</p>

<p>TMI-1 (WAY-171318), a novel orally active inhibitor of ADAM17 (TACE) and MMP, induces tumor apoptosis in a breast cancer.</p>

<p>FTI-277, an FTase inhibitor, blocks H-Ras/K-Ras signaling and HDV infection; mimics Ras CAAX peptide.</p>

<p>Thalidomide-O-C6-NH2 TFA is a synthesized E3 ligase ligand-linker conjugate used in the PROTAC dTAG-13, a degrader of FKBP12F36V and BET[1].</p>

<p>PRDX1-IN-1 is a and PRDX1 inhibitor with potential anti-inflammatory and anti-cancer activity for the study of breast and esophageal cancer.</p>

<p>Pancratistatin, an isoquinoline from Hymenocallis littoralis, triggers apoptosis in melanoma and is studied for neuroblastoma, leukemia, and breast cancer.</p>

<p>Ancitabine is an antitumour drug that improves Hailey-Hailey disease-related phenotypes in yeast models. inhibits DNA synthesis, acute leukaemia.</p>

<p>Busulfan-d8 (Sulphabutin-d8) is the 2H-labeled Busulfan. Busulfan is an anticancer agent with immunosuppressive and myeloablative chemotherapy activities.</p>

<p>MCL-1/BCL-2-IN-2 is a selective Mcl-1 and Bcl-2 inhibitor with potential antitumor activity for tumor research.</p>

<p>Cl-amidine TFA: oral PAD inhibitor, induces cancer cell apoptosis, IC50s: PAD1 - 0.8μM, PAD3 - 6.2μM, PAD4 - 5.9μM.</p>

<p>CCW16 is a covalent E3 ubiquitin ligase RNF4 ligand, cysteine reactivity, inducing ferroptosis in AML cells by activating ROS signalling.</p>

<p>SU11652 is an effective and competitive receptor tyrosine kinase (RTK) inhibitor, including VEGFR, FGFR, PDGFR, and Kit.</p>

<p>Momelotinib sulfate is an ATP-competitive JAK1/JAK2 inhibitor (IC50: 11 nM/18 nM). It has 10-fold selectivity versus JAK3.</p>

<p>PERK-IN-2 is a potent inhibitor of PERK(IC50 of 0.2 nM).</p>

<p>(E/Z)-E64FC26 is a protein disulfide isomerase (PDI) family inhibitor with affinity for PDIA1, PDIA3, PDIA4, TXNDC5, and PDIA6.</p>

<p>5-(N,N-Hexamethylene)-amiloride (5-HMA) is an amiloride derivative that inhibits TRPA1-mediated calcium signaling (IC50: 35 μM). It functions as an inhibitor of the Na+/H+ exchanger (NHE) with Ki values ranging from 0.013 to 2.4 μM for various NHE isoforms. Additionally, 5-HMA blocks ASIC3 channels by 51% at 20 μM.</p>

<p>Necrostatin 2 S enantiomer is the S enantiomer of Necrostatin 2</p>

<p>KS100 inhibits ALDH1A1, ALDH2, ALDH3A1, boosts ROS, triggers apoptosis, and has anti-cancer properties.</p>

<p>SLC7A11-IN-1 is an SLC7A11 inhibitor with antiproliferative activity, inhibiting cell invasion and metastasis, useful for research on neurological diseases.</p>

<p>Methopterin shows the activation and bone resorption function of murine osteoclasts.</p>

<p>Thalidomide-O-amido-C4-NH2 is a thalidomide cereblon ligand-linker used for PROTAC synthesis as an E3 ligase.</p>

<p>MRT00033659 inhibits CK1 (IC50=0.9 μM), CHK1 (IC50=0.23 μM), activates p53, and destabilizes E2F-1; it's a pyrazolo-pyridine.</p>

<p>LNnT is a metabolite that reduces IL-8, has anti-inflammatory effects, and aids in wound healing.</p>

<p>4-Benzoyl-L-phenylalanine is an L-phenylalanine derivative and optically active amino acid.</p>

<p>Sodium catechol sulfate is a bioactive chemical.</p>

<p>Citrinin: a mycotoxin with antifungal, antibacterial, potential anticancer, and neuroprotective properties; contaminates food.</p>

<p>Propylparaben sodium, a plant-based preservative used in cosmetics, pharma, and food, hinders follicle growth and sperm health.</p>

<p>LG100268 is a selective, and oral RXR agonist，inducing transcriptional activation in adipocytes; inhibits keratin 17 increases PD-L1 expression.</p>

<p>Condurango glycoside A activates p53, induces ROS generation, up-regulates p53 expression, and triggers apoptosis as well as premature senescence associated</p>

<p>PI-103 Hydrochloride is a dual PI3K/Akt and mTOR inhibitor exhibiting nM-level inhibition of p110α, p110β, p110δ, p110γ, DNA-PK, mTORC1, and mTORC2.</p>

<p>Amoscanate is an antiparasitic agent. It is highly effective in animals against the four major species of schistosomes which infect humans.</p>

PETCM is a caspase-3 activator and acts as an cytochrome c (cyto c)-dependent manner.

<p>Diphenyl disulfide fights breast cancer by inducing cell death and stopping growth.</p>

<p>Forodesine hydrochloride blocks lymphocyte growth and induces leukemia cell death by inhibiting PNP, effective across species.</p>

<p>Ezatiostat (TER199(free base)) is a tripeptide analog of glutathione that can selectively inhibit GSTP1-1 catalytic activity.</p>

<p>Melatonin D5, a deuterium-labeled version of melatonin, is a hormone produced by the pineal gland, known for its role as a selective ATF-6 inhibitor that promotes apoptosis in human hepatoma cells via COX-2 downregulation. Additionally, it activates melatonin receptors and exhibits antioxidative and anti-inflammatory properties.</p>

<p>6-Azauridine is a purine analog with antitumor effects, inhibiting DNA synthesis and inducing apoptosis in lymphatic cancers.</p>

<p>4-Thiothymidine is a Nucleoside Derivative - Thio-nucleoside, 5-Modified pyrimidine nucleoside.</p>

<p>Casein Kinase inhibitor A86 is a highly effective and orally bioavailable inhibitor of casein kinase 1α (CK1α) and also inhibits CDK7 (TFIIH) and CDK9 (P-TEFb). It induces apoptosis in leukemia cells, exhibiting substantial anti-leukemic effects.</p>

<p>MC1742 inhibits class I/IIb HDACs, blocks sarcoma CSC growth, and reactivates latent HIV. IC50: HDAC1-3/8 (0.02-0.61 μM), HDAC6/10 (7-40 nM).</p>

<p>Hematoporphyrin monomethyl ether is a porphyrin photosensitizer that can be used in studies of port wine stains.</p>

<p>Acyclovir sodium is an antimetabolite. Acyclovir sodium inhibits HSV-specified DNA polymerases and prevents further viral DNA synthesis.</p>