Apoptosis

RIPK1-IN-13 (compound 28) is a selective inhibitor of receptor-interacting serine/threonine-protein kinase 1 (RIPK1), showing a pKi of 7.66 as measured by the ADP-Glo kinase assay. It exhibits inhibitory effects in human leukemia U937 cells with a pIC50 of 7.2.

155H1 (Compound 11) is a stapled peptide that covalently binds to hMcl1 (172-323) with an IC50 of 18 nM.

<p>WEE1-IN-7 (compound 12h) is a potent, orally active WEE1 inhibitor with an IC50 value of 2.1 nM. This compound induces apoptosis and causes cell cycle arrest in the S phase, demonstrating antitumor activity.</p>

<p>Enpp/Carbonic anhydrase-IN-2 is a potent dual inhibitor of Enpp and carbonic anhydrase, inhibiting NPP1, NPP2, NPP3, CA-IX, CA-XII, with IC50 values of 1.13, 1.</p>

CBI1 is a covalent BAX inhibitor. It selectively derivatizes BAX at C126 and inhibits BAX activation by triggering a ligand or through point mutations. CBI1 prevents the lipidation and oligomerization of BAX by t-2-hex. It also inhibits BAX activation induced by BH3 ligands, F116A mutation, or t-2-hex.

<p>Thalidomide-based E3 ligase ligand linked to a PROTAC piperazine-piperidine chain.</p>

<p>PAK4-IN-3 (compound 27e) is a PAK4 inhibitor exhibiting an IC50 of 10 nM and demonstrates antiproliferative effects on A549 cells with an IC50 of 0.61μM.</p>

<p>AZD1152 is a pro-drug of Barasertib (AZD1152)-hQPA. Which is a highly selective Aurora B inhibitor with IC50 of 0.37 nM in a cell-free assay.</p>

<p>CRA-026440 hydrochloride is a potent and broad-spectrum HDAC inhibitor.</p>

<p>Rozanolixizumab (RYSTIGGO) is a humanized IgG4 monoclonal antibody that targets FcRn in newborns for autoimmune research.</p>

<p>PZ703b TFA, a Bcl-xl PROTAC degradation agent, promotes apoptosis and halts bladder cancer cell proliferation, making it a pertinent investigative compound for</p>

<p>EGFR-PK/JNK-2-IN-1 (Compound 6c) is a dual inhibitor of EGFR-PK and JNK-2, with IC50 values of 2.7 and 3.0 μM, respectively. It can induce apoptosis and cause cell cycle arrest at various stages. This compound is applicable in cancer research.</p>

<p>YN14-H is a PROTAC degrader that targets KRASG12C. It effectively inhibits the growth of NCI-H358 and MIA PaCa-2 cells, with IC50 values of 0.042 μM and 0.021 μM, respectively, and DC50 values of 28.9 nM and 18.1 nM. YN14-H significantly induces apoptosis and suppresses cell migration. It demonstrates favorable pharmacokinetics and excellent in vivo antitumor activity.</p>

Sodium valproate is an anti-epileptic, boosting brain GABA levels and possibly affecting potassium channels for membrane stability.

<p>Feladilimab (GSK3359609) is an IgG4 monoclonal antibody that is an ICOS agonist.</p>

<p>Conophylline, an alkaloid from Ervatamia microphylla, induces pancreatic cell differentiation and apoptosis, and suppresses HSC.</p>

<p>CIGB-300 acetate (P15-Tat acetate) is a peptide that acts as an inhibitor of casein kinase 2 (CK2). It exhibits anticancer properties by disrupting the phosphorylation activity of CK2. CIGB-300 acetate induces apoptosis in various tumor cell lines and is applicable for cancer research.</p>

<p>8-hydroxy Efavirenz, a main efavirenz metabolite by CYP2B6, causes apoptosis in rat neurons at 0.01 μM.</p>

<p>YB-0158 ammonium (Wnt pathway inhibitor 2 ammonium) is a reverse-rotation peptidomimetic with translation-enhancing potential and anticancer activity.</p>

Mepacrine (Erion) is an acridine derivative formerly widely used as an antimalarial.

<p>icFSP1 is a mitochondria-associated apoptosis-inducing factor regulator with antitumor activity for the study and treatment of tumor diseases.</p>

<p>Apoptosisinducer 33 (compound H2) is a hydrazone derivative. It exhibits antioxidant and antimicrobial properties, capable of inhibiting the growth of Staphylococcus aureus, Escherichia coli, and Candida albicans. Additionally, Apoptosisinducer 33 can suppress tumor cell proliferation and induce apoptosis (apoptosis), making it useful for tumor research.</p>

PRMT5-IN-33 (compound A8) is a selective inhibitor of PRMT5 that competes with SAM, exhibiting an IC50 of 10.9 nM. It induces apoptosis and inhibits the proliferation of Z-138 and MOLM-13 cells, demonstrating antitumor activity.

<p>2,2-Dimethyl-2,3-dihydrobenzofuran-7-ol inhibits the proliferation of the THP-1 cell line and anti-infective Leishmania and Toxoplasma gondii RH.</p>

Thalidomide-O-PEG4-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

<p>Galloflavin Potassium is an inhibitor of lactate dehydrogenase.</p>

CLEFMA has anti-proliferative activity. CLEFMA inhibits tumor growth associated with NF-κB-regulated anti-inflammatory and anti-metastatic effects.

<p>MY-943, a potent inhibitor of tubulin polymerization and LSD1, exhibits anticancer properties by inducing G2/M phase arrest, promoting apoptosis, and</p>

<p>3-Hydroxyterphenyllin from A. candidus is a fungal compound with antioxidant, anticancer, antibacterial, and antiviral effects.</p>

<p>ARI-1 is a receptor tyrosine kinase-like orphan receptor 1 (ROR1) inhibitor that binds to ROR1's extracellular Frizzled domain, effectively inhibiting aberrant</p>

<p>SSE1806, a podophyllotoxin derivative (a natural antimitotic agent), functions as a microtubule/tubulin inhibitor, exhibiting potent anticancer and</p>

<p>"Urelumab (BMS-66513), a humanized IgG4 mAb CD137 agonist, boosts T-cell/NK cell-mediated cytotoxicity and anti-tumor activity."</p>

<p>TNF-α-IN-11 (Compound 10) is a TNF-α inhibitor exhibiting a dissociation constant (K D) of 12.06 μM.</p>

<p>Petromurin C, a bis-indolyl benzenoid from P. muricatus, is cytotoxic to NS-1 cells (IC50=33μg/ml) and active against T. foetus (IC50=100μg/ml).</p>

<p>Anticancer agent 154 (Compound 8h) enhances reactive oxygen species production, causing mitochondrial damage, and promotes cell apoptosis and DNA damage.</p>

<p>Chloranil (tetrachloro-p-benzoquinone) induces inflammation and neurological dysfunction and can be used to model inflammation in mice.</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>

<p>NMC-001 is a human IgG1 monoclonal antibody (mAb) that targets MDM2. It is useful for pancreatic cancer research. The recommended isotype control is HumanIgG1kappa, Isotype Control.</p>

<p>PDE4-IN-1 is a PDE4 inhibitor characterized by high potency (IC50: 8.6 nM) and superior selectivity over other PDE subtypes. This compound inhibits the release of inflammatory cytokines and chemokines. Additionally, PDE4-IN-1 significantly restores the damaged cAMP-CREB signaling pathway, inhibits proliferation, and promotes differentiation to reverse psoriasis formation.</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>TRBP-IN-1 (Compound 13j) is an orally active inhibitor of TAR RNA-binding protein 2 (TRBP) with an IC50 of 12.72 μM. It exhibits significant anti-hepatocellular carcinoma (HCC) activity, effectively suppressing proliferation and metastasis of HCC cells [HCCLM3 cells (IC50: 18.96 μM) and SK-Hep-1 cells (IC50: 16.45 μM)]. TRBP-IN-1 modulates miRNA biosynthesis by targeting TRBP, inhibiting the expression of oncogenic miRNAs. It induces apoptosis and pyroptosis in HCC cells by decreasing miRNA levels. TRBP-IN-1 is suitable for research on targeted HCC therapy.</p>

<p>Platycoside G3 is a useful organic compound for research related to life sciences. The catalog number is T124100 and the CAS number is 849758-44-7.</p>

<p>4-N-Nonyloxyphenol, kaolinite nanotube photosensitizer, degrades phenolic pesticides, and disrupts endocrine.</p>

<p>TRP-601 is a caspase inhibitor.</p>

<p>2-deoxy-D-Glucose-13C6 is an internal standard for GC/LC-MS, a glycolysis inhibitor, and induces apoptosis in certain cells at 2 mg/ml.</p>

<p>Thalidomide-5-NH-PEG2-NH2 hydrochloride is a cereblon ligand based on Thalidomide, designed to recruit CRBN proteins. It has the capability to be linked with target protein ligands via a linker, facilitating the formation of PROTAC molecules, such as THAL-SNS-032.</p>

<p>This Bim peptide belongs to the pro-apoptotic group of the Bcl-2 family of proteins.</p>

<p>LZ-07 is an IRAK4 PROTAC degrader (DC50 = 1.14 nM), that, upon degradation of IRAK4, significantly inhibits the expression of cytokines such as IL-6, IL-1β, TNF-α, and IL-10. It is applicable in research related to autoimmune diseases.</p>

<p>PI3K/HDAC-IN-4 (Compound 31f) is a dual inhibitor targeting PI3K and HDAC, with an IC50 of 0.2μM. It demonstrates high selectivity for HDAC1-3, with IC50 values of 75.5 nM, 70.9 nM, and 1.9 nM, respectively. As a potent pan-PI3K inhibitor, PI3K/HDAC-IN-4 has IC50 values of 2.5 nM, 80.5 nM, 10.0 nM, and 57.2 nM for PI3Kα, β, δ, and γ, respectively. This compound effectively induces apoptosis in tumor cells by concurrently inhibiting the PI3K/AKT/mTOR signaling pathway and HDAC1-3. It shows significant antiproliferative activity across various tumor cell lines, such as MV4-11, Jeko-1, HL60, and MCF-7, with IC50 values of 0.2, 0.9, 0.8, and 1.5 μM, respectively. PI3K/HDAC-IN-4 is applicable in the study of lymphoma and leukemia.</p>

<p>FLT3/HDAC-IN-1 is a dual inhibitor targeting FLT3 and HDAC, with IC50 values of 30.4 nM for FLT3 and 52.4, 14.7 nM for HDAC1/3, respectively. It induces apoptosis in MV-4-11 cells and exhibits antiproliferative effects against BaF3 cells transformed by FLT3 mutations. FLT3/HDAC-IN-1 is useful for research on refractory solid tumors and hematological malignancies.</p>

<p>MEDI-7352 is a human bispecific antibody targeting NGF/bNGF and TNF. It can be utilized in research focused on osteoarthritis (OA) pain.</p>

<p>KRN 5500, a derivative of the nucleoside antibiotic spicamycin, has a wide range of antitumor activity against human cancer cell lines.</p>

CTP-347, a deuterated version of paroxetine, is potentially the best non-hormonal drug in its class for the treatment of hot flashes.

<p>VEGFR-2-IN-53 (Compound 15w) is an inhibitor of VEGFR-2 with an IC50 value of 4.34 μM. It induces cell apoptosis (Apoptosis) and inhibits angiogenesis by blocking VEGFR-2 activity and preventing cell migration. Additionally, it shows an IC50 of 3.87 μM in inhibiting the growth of MCF-7 cells, making it pertinent for research in cancer therapeutics.</p>

<p>MRIA9 inhibits SIK1/2/3 &amp; PAK2/3 with IC50: SIK1 (516 nM), SIK2 (180 nM), SIK3 (127 nM); ATP-competitive.</p>

<p>VPC-70063 (Thiourea, N-[3,5-bis(trifluoromethyl)phenyl]-N'-(phenylmethyl)-) is an inhibitor of c-Myc-MAX.</p>

<p>Methyl-4-oxoretinoate is a synthetic retinoid with anticancer properties, used for skin conditions and potential ocular treatments.</p>

<p>UZH1, a mix of active METTL3 inhibitor UZH1a (IC50 280 nM) and inactive UZH1b (IC50 28 μM), modifies epitranscriptomics and has antitumor properties.</p>

<p>Thalidomide-O-C7-NH2 is a cereblon ligand-linked E3 ligase for PROTAC use.</p>

<p>Lorigerlimab (MGD019) is a bispecific IgG4 DART that blocks PD-1/CTLA-4, enhancing T-cells for mCRPC research.</p>

Bornyl acetate (Isobornyl acetate) has an anti-inflammatory effect. It is the volatile ingredient in some Chinese traditional herbs and numerous conifer oils.

<p>PD-1/PD-L1-IN-39 (X 14) is an orally active PD-1/PD-L1 inhibitor with an IC50 value of 15.73 nM. It exhibits strong binding affinity to human and mouse PD-L1, with KD values of 14.62 and 392 nM, respectively. PD-1/PD-L1-IN-39 also demonstrates antitumor activity.</p>

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

<p>Anti-inflammatory agent 95 (Compound 2e) is a compound with potent anti-inflammatory properties, showing significant inhibition of NO production in LPS-induced RAW 264.7 mouse macrophages, with an IC50 of 8.8 μM. It also effectively suppresses the secretion of TNF-α and IL-1β, achieving inhibition rates of 60% and greater than 90% at 100 μM, respectively. Anti-inflammatory agent 95 holds promise for research into inflammatory diseases.</p>

<p>Anti-Mouse TNF alpha Antibody is a rat-derived IgG inhibitor targeting mouse TNF alpha.</p>

<p>Thalidomide-O-C8-NH2 is a synthetic cereblon ligand &amp; PROTAC linker, serving as an E3 ligase ligand-linker.</p>

<p>EGFR-IN-83 (Compound 9), an EGFR inhibitor with an IC50 of 2.53 nM, exhibits antiproliferative effects on MCF-7 and MDA-MB-231 cell lines, with respective IC50</p>

<p>GDCNF-11, an HSP90-based HIM-PROTACGPX4 degrader, facilitates the ubiquitination and degradation of GPX4 through the HSP90 chaperone complex. This reduction in endogenous GPX4 induces ferroptosis in HT-1080 cells, with a DC50 value of 0.08 μM.</p>

<p>Thalidomide-O-C5-acid, a synthesized E3 ligase linker, merges cereblon and PROTAC tech.</p>

<p>Ferroptosisinducer 6 (6d) is an inducer of ferroptosis (ferroptosis) that exhibits potent potential for Type I/II photodynamic therapy by inducing ROS production, oxidative stress, and mitochondrial damage. Additionally, it demonstrates antitumor activity.</p>

<p>CS4 is a selective HDAC inhibitor, with IC50 values for HDAC1, HDAC6, HDAC8, HDAC4, and HDAC11 reported as 38 nM, 12 nM, 5.8 μM, 19 μM, and 61 μM, respectively. It enhances the acetylation of α-tubulin and histone 3 (histone 3). Additionally, CS4 activates PPARγ and blocks glycolysis (glycolysis). It induces cell cycle arrest at the G2 phase and triggers apoptosis (apoptosis), exhibiting anticancer effects both in vitro and in vivo.</p>

<p>Z-Asp-CH2-DCB is an irreversible inhibitor of broad spectrum caspase.</p>

<p>PROTACSMARCA2/4 degrader-38 is a SMARCA2/4 PROTAC degrader with DC50 values of 3.0 nM and 4.0 nM, respectively. It facilitates the ubiquitination and degradation of SMARCA2/4 and can block the G0/G1 phase of the cell cycle, leading to the induction of apoptosis. PROTACSMARCA2/4 degrader-38 is applicable in acute myeloid leukemia (AML) research.</p>

VTP50469 fumarate is a highly selective and orally active inhibitor of Menin-MLL interaction (Ki: 104 pM), and has potently anti-leukemia activity.

TopoII/tubulin-IN-1 (Compound 1B8) is an inhibitor of TopoII/tubulin. It effectively suppresses the proliferation of tumor cells and reduces ROS levels, while inducing apoptosis and cell cycle arrest, without showing significant cytotoxicity to normal cells. TopoII/tubulin-IN-1 exhibits antitumor activity.

<p>Anticanceragent 267 (Compound 5q) serves as an activator of RIPK3 and MLKL. It effectively inhibits the proliferation of several cancer cell lines, with IC50 values of 9.79, 10.77, and 5.94 μM for MDA-MB-231, MDA-MB-486, and MCF-7, respectively. The compound induces cell cycle arrest at the subG1 phase and triggers necroptosis in MDA-MB-231 cells. Additionally, Anticanceragent 267 demonstrates antitumor activity in mouse xenograft models.</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>

WR-S-462 is a STAT3 inhibitor. It effectively blocks the phosphorylation and biological functions of STAT3 in vitro. The IC50 of WR-S-462 for inhibiting MDA-MB-231 cells is 0.03 μM, and it exhibits a strong binding affinity for STAT3 protein with a Kd of 58 nM. WR-S-462 prevents the nuclear translocation of p-STAT3 and selectively inhibits the expression of p-STAT3Tyr705 in MDA-MB-231 cells, as well as the expression of downstream target genes regulated by STAT3, such as Cyclin D1, Bcl-2, and Bcl-xl. This compound inhibits the growth and metastasis of triple-negative breast cancer (TNBC).

<p>Mcl1-IN-26 is an effective and selective myeloid cell leukemia 1 inhibitor.</p>

<p>Uvarigrin induces tumor multidrug resistance cell apoptosis and triggers Caspase-9 activation. Uvarigrin is isolated from the roots of Uvaria calamistrata.</p>

<p>PROTAC Mcl1 degrader-1 is a Cereblon ligand-based targeted chimeric protein degrader (PROTAC) and an Mcl-1 inhibitor, useful in cancer research.</p>

<p>EGFR-IN-151 (Compound 10) inhibits EGFR and its downstream signaling pathways ERK/STAT3. It effectively suppresses the proliferation of various lung cancer cells, with IC50 values of 11.7, 5.19, 7.32, and 1.53 μM for NCI-H1781, HCC827, NCI-H3255, and NCI-H1975, respectively. Additionally, EGFR-IN-151 hinders colony formation and cell migration in H1975, induces G1 phase cell cycle arrest, and triggers apoptosis in H1975 cells.</p>

<p>ERK-IN-6, a potent agent, inhibits ESCC growth and induces apoptosis through the ERK pathway.</p>

<p>Ac-Pro-Gly-Pro-OH can be used as a CXCR2 agonist with bactericidal and anti-inflammatory activity for the study of sepsis and lung inflammation.</p>

<p>HDAC6-IN-16 (compound 5c), a quinazolin-4(3H)-one-based inhibitor of histone deacetylase 6 (HDAC6), demonstrates an anticancer effect by inhibiting colony</p>

<p>PROTAC XPO1 degrader-1 (Compound 2c) is an XPO1 degrader. It exhibits anti-proliferative effects, induces apoptosis, inhibits NF-κB activity, and causes cell cycle arrest at the G1 phase. PROTAC XPO1 degrader-1 is applicable to research on hematological malignancies.</p>

<p>Thalidomide-based E3 ligase ligand for PROTAC degrader MI-389 synthesis, linked to cereblon and Boc.</p>

<p>Thalidomide derivative for CRBN protein recruitment, used in PROTACs production for protein degradation.</p>

<p>Vonlerizumab (Anti-TNFRSF4/OX40/CD134 Antibody) is a humanized monoclonal antibody targeting OX40, used in tumor research.</p>

F1324: potent BCL6 inhibitor, IC50=1nM, binding t1/2=441s, strongly inhibits BCL6 PPI.

<p>Milademetan tosylate hydrate, an oral MDM2 inhibitor targeting AML and solid tumors, induces G1 arrest and apoptosis.</p>

<p>eIF4E-IN-3: potent eIF4e inhibitor with promise for cancer study.</p>

<p>OICR12694 (JNJ-65234637) TFA, an orally active B cell lymphoma 6 (BCL6) inhibitor [1], demonstrates effectiveness in targeting BCL6 pathways.</p>

<p>Chloranthalactone B, a sesquiterpenoid from Sarcandra glabra, inhibits inflammation via AP-1 &amp; p38 MAPK.</p>

<p>MS1943 is a orally bioavailable EZH2 selective degrader(IC50 of 120 nM).</p>

<p>p53 and MDM2 proteins-interaction-inhibitor dihydrochloride is a interaction inhibitor between p53 and MDM2 proteins.</p>

<p>A011, a potent and selective ataxia-telangiectasia mutated (ATM) inhibitor, exhibits an IC50 of 1.0 nM and triggers apoptosis as well as G2/M phase cell cycle</p>

<p>CDK-IN-14 (B34) is a CDK2 inhibitor (IC50=0.097 μM) that exhibits anti-hepatocellular carcinoma activity. It inhibits the cell cycle in HepG-2 cancer cells and induces apoptosis (apoptosis) through a caspase-mediated mechanism.</p>

<p>CDK/HDAC-IN-4 is a highly selective dual inhibitor of cyclin-dependent kinase (CDK) and histone deacetylase (HDAC), with IC50 values of 88.4 nM and 168.9 nM, respectively. This compound exhibits antiproliferative effects in both hematologic and solid tumor cells. Additionally, CDK/HDAC-IN-4 induces apoptosis and S-phase cell cycle arrest in MV-4-11 cells. It has also demonstrated significant antitumor efficacy in an MV-4-11 xenograft model.</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>