Apoptosis

Topo I/II-IN-2 (Compound 3g) is an inhibitor of both Topo I and Topo II. It exhibits inhibitory activity against NCI-H446 and NCI-H1048 cells with IC50 values of 1.30 μM and 1.42 μM, respectively. Topo I/II-IN-2 induces mitochondrial apoptosis, disrupts mitochondrial function, and stimulates activity generation. Additionally, it inhibits the PI3K/Akt/mTOR pathway, effectively preventing the proliferation, invasion, and migration of small cell lung cancer (SCLC) cells in vitro.

PKM2 modulator 1 (compound C998) is an effective PKM2 inhibitor with antiproliferative activity. It induces apoptosis and holds potential for research in glioblastoma studies.

USP1-IN-11 (compound 38-P2) is a selective, reversible, and non-competitive inhibitor of USP1 (Ubiquitin-specific protease 1). It activates the DDR (DNA damage repair) pathway, leading to cell cycle arrest and apoptosis, thereby inhibiting cell survival. USP1-IN-11 increases sensitivity to Olaparib in drug-resistant cells and works synergistically with Andrographolide in cancer cells with functional BRCA. In the MDA-MB-436 xenograft model, USP1-IN-11 demonstrates significant dose-dependent antitumor activity.

Thalidomide-PEG3-NH2: a cereblon-based E3 ligase ligand-linker for PROTAC tech.

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.

Hydrocinchonine is an Alkaloid from Olea europaea and is found in fruits.

DC 81: Streptomyces-derived antitumor antibiotic, potent nucleic acid synthesis inhibitor, binds DNA sequences, forms covalent adducts.

Sodium 2,4-dichlorophenoxyacetate: selective herbicide, controls broadleaf weeds by disrupting growth and protein/DNA synthesis.

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

TrxR-IN-7 (14f) is a potent inhibitor of thioredoxin reductase (TrxR), with an IC50 value of 3.5 µM. It exhibits antiproliferative activity and can induce apoptosis and the production of reactive oxygen species (ROS).

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.

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)

WKYMVM is a N-formyl peptide receptor (FPR1) agonist.

PTP1B-IN-30 (Compound 3j) is an inhibitor of PTP1B with an IC50 of 0.51 µM. It suppresses the proliferation of T47D cancer cells with an IC50 of 21.21 µM, induces cell cycle arrest at the S phase, and triggers apoptosis in T47D cells.

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.

FMP is a platinum (IV) complex. It significantly upregulates the expression of γ-H2AX and p53, enhances ROS production, and markedly increases the expression of apoptosis (Apoptosis) related proteins (DR5, Fas, caspase-8, Cyt-c, caspase-3, cleaved-PARP1, Bax). FMP exhibits antiproliferative activity against breast cancer.

TS-IN-6 (Compound 10) is a thymidylate synthase (TS) inhibitor with an IC50 value of 0.54 μM, showing significant antiproliferative activity. It can induce G1 phase cell cycle arrest and apoptosis (with notable increases in early and late apoptosis rates) and is useful for research in cancers such as colon, breast, and liver cancer.

NSC243928 mesylate binds to human lymphocyte antigen 6 (LY6), a cell growth inhibitor with anticancer activity.

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.

TS-IN-5 (Compound 15) is an inhibitor of thymidylate synthase (TS). It induces apoptosis by modulating the proteins Bax, BCL-2, PI3K, and STAT1. TS-IN-5 exhibits antitumor activity against liver cancer, breast cancer, and colon cancer.

BKM1644 is an effective inhibition of the proliferation of metastatic, castration-resistant PCa (mCRPC) cells.

Cuprichydroxide exhibits inhibitory activity against Ralstonia solanacearum and A549 cells and has acute pulmonary toxicity.

RTX-002 is a human monoclonal antibody (mAb) targeting PDCD1/PD-1/CD279. This compound is applicable in the research of autoimmune diseases such as systemic lupus erythematosus and multiple sclerosis.

Thalidomide-NH-(CH2)2-NH2 TFA is an alkyl-modified derivative of Thalidomide serving as a Cereblon ligand to recruit CRBN proteins and a pivotal intermediate in

Bim BH3 is a bioactive peptide that belongs to the pro-apoptotic Bcl-2 family of proteins.

Pep19-2.5: Synthetic antitoxin peptide inhibits LP/LPS signals via PRRs, preventing inflammation and pyroptosis.

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.

Siomycin A: thiopeptide antibiotic, selectively inhibits FOXM1, anti-tumor, induces apoptosis.

GR-1405 is a human monoclonal antibody (mAb) that targets B7-H1/PD-L1/CD274. It enhances the antitumor immune response mediated by cytotoxic T lymphocytes (CTL) against tumor cells expressing PD-L1. GR-1405 is applicable in research related to lymphomas and solid tumors.

PROTACKSP-IN-1 (Compound 21) is a spindle protein (KSP) degrader as a PROTAC, effectively degrading KSP in HCT-116 cells with a DC50 value of 114.8 nM. It inhibits the proliferation of HCT-116 with an IC50 of 10 nM, causes G2/M phase cell cycle arrest, and induces apoptosis in HCT-116. Additionally, PROTACKSP-IN-1 demonstrates antitumor activity in mouse models.

Carubicin, an anthracycline antibiotic from Actinomadura carminata, disrupts DNA replication and repair by intercalating DNA and inhibiting topoisomerase II.

Fisetin quarterhydrate, a natural flavonol present in numerous fruits and vegetables, exhibits benefits including antioxidant, anticancer, and neuroprotective

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.

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

TMX1 is a molecular glue degrader targeting BRD4, selectively recruiting the ubiquitin ligase CUL4-DCAF16 complex to BRD4 (BD2.

c-MYC/BCL2 ligand 1 iodide is a dual-target ligand that specifically interacts with the G-quadruplex (G4) regions of the c-MYC and Bcl-2 promoters, exhibiting Kd values of 0.90 μM for c-MYCG4 and 0.56 μM for Bcl-2G4. It works by binding to these G4-forming sequences to inhibit transcription of the c-MYC and Bcl-2 genes, leading to reduced protein expression. This compound effectively suppresses MCF-7 cell proliferation and migration, induces G1 phase cell cycle arrest, and triggers apoptosis. Additionally, it significantly hampers tumor growth in the 4T1 homogenous model with negligible toxicity. c-MYC/BCL2 ligand 1 iodide is applicable in breast cancer research.

Nrf2 activator-11 (compound M11) is a Nrf2 activator that possesses blood-brain barrier permeability and offers anti-oxidation, anti-inflammation, anti-ferroptosis, and anti-apoptosis properties. It is applicable for use in studying cerebral ischemia-reperfusion (CI/R) injury models.

Bleomycin A5, or Pingyangmycin, is an oral glycopeptide antibiotic and acts as an antineoplastic and apoptosis inducer.

PROTACBRD4 Degrader-33 is an enzyme-activated, click-responsive BRD4 PROTAC degrader designed with effective tumor microenvironment responsiveness. This compound exhibits exceptional penetration into tumor tissues and effectively inhibits PD-L1 protein expression. In the 4T1 tumor mouse model, PROTACBRD4 Degrader-33 demonstrates potent antitumor immunomodulatory activity.

Tubulin polymerization-IN-45, a tubulin-targeting agent, acts as a tubulin polymerization inhibitor by binding to the tubulin's colchicine site.

S9-CMC1 TFA is a covalent peptide lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 value of 2.53 μM. It selectively targets the active site Cys360 of the enzyme. By inhibiting LSD1 activity, S9-CMC1 TFA elevates H3K4me1 and H3K4me2 levels, inducing G1 cell cycle arrest and apoptosis, thereby suppressing cell proliferation. In addition, S9-CMC1 TFA markedly inhibits tumor growth in A549 xenograft animal models.

Thalidomide derivative for CRBN protein recruitment, used in PROTACs production for protein degradation.

Monactin is a Marcrotetrolide antibiotic produced by cycloheximide producing species of Streptomyces. It is a homolog of nonactin from the same species.

FLT3-IN-29 (Compound MY-10) is an FLT3 inhibitor with IC50 values of 6.5 nM and 10.3 nM for FLT3-ITD and FLT3-D835Y mutants, respectively. It induces cell cycle arrest at the G0/G1 phase and effectively triggers apoptosis (Apoptosis). Additionally, FLT3-IN-29 reduces reactive oxygen species (ROS) and mitochondrial membrane potential (MMP), displaying anti-leukemic properties.

TOFA-Plasmalogen (compound 1), a derivative of glyceraldehyde, exhibits ferroptosis-inducing properties. This compound promotes lipid peroxidation in cell membranes, leading to cytotoxic effects with an inhibition concentration (IC 50 = 32.87 μM).

YJ1206 is a highly potent and selective CDK12/13 PROTAC degrader oral, DNA damage and cell-cycle arrest,and inhibits the proliferation of prostate cancer cells.

KB02-SLF, a molecular glue, degrades nuclear FKBP12 by modifying E3 ligase DCAF16 and extends protein degradation.

VEGFR-2-IN-50 (Compound 10f) is a VEGFR-2 inhibitor and apoptosis inducer with an IC50 of 0.33 μM. It exhibits growth inhibitory activity against the MCF-7 and MDA-MB-231 breast cancer cell lines, with IC50 values of 19.86 μM and 10.88 μM, respectively, making it a promising agent for breast cancer research.

MST3-IN-1 is a selective and orally active MST3 inhibitor with an IC50 of 122.4 nM. It exhibits antiproliferative activity in HepG2 cells, effectively induces apoptosis, and causes cell cycle arrest at the G2/M phase. In HepG2 xenograft mouse models, MST3-IN-1 significantly suppresses tumor growth, making it useful for liver cancer research.

Rat form of the beta-Amyloid (1-40) peptide

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

Odoroside A, from Nerium oleander leaves, induces cancer cell death via ROS/p53, causing apoptosis and cell cycle arrest.

Thymocartin (RGH 0206) is a fragment 32-35 of the naturally occurring thymic factor (thymopoietin).Thymocartin is used in the study of immunodeficiency diseases

RIPK1-IN-17 is a dual inhibitor of RIPK1 and RIPK3 inhibits necrosis by inhibiting phosphorylation of RIPK1, RIPK3 and MLKL,in a tnf-induced inflammation model.

XmAb-2513 is a humanized monoclonal antibody inhibitor targeting CD30. It demonstrates significant anti-proliferative activity along with excellent antibody-dependent cellular cytotoxicity (ADCC) and antibody-dependent cellular phagocytosis (ADCP). XmAb-2513 is applicable in research on hematological malignancies such as Hodgkin lymphoma (HL) and anaplastic large cell lymphoma (ALCL).

PIYLGGVFQ is a TNF-α peptide inhibitor. It can suppress TNF-α-mediated apoptosis, nuclear translocation, and activation of NF-κB. In a CIA mouse model, PIYLGGVFQ has demonstrated anti-arthritic activity.

MK-1248 is a human IgG4 monoclonal antibody (mAb) targeting TNFSF18. It enhances the proliferative response of tumor-infiltrating lymphocytes to anti-CD3 stimulation and promotes the production of anti-tumor associated regulatory cytokines. MK-1248 is utilized in research on solid tumors.

TQB2916 is a humanized IgG2 monoclonal antibody agonist that targets CD40. It exhibits significant antitumor activity by occupying CD40 and activating immune function. TQB2916 is applicable for research in advanced solid tumors and lymphomas.

IBI356 is a humanized monoclonal antibody inhibitor that targets OX40L/CD134L/CD252. It can be utilized in the study of chronic inflammatory skin diseases, such as atopic dermatitis.

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

Placulumab (ART621), an anti-TNF α monoclonal antibody, targets inflammation, potentially aiding arthritis treatment.

Echitamine chloride, an alkaloid in Alstonia scholaris, has anti-cancer properties and inhibits pancreatic lipase (IC50: 10.92 µM).

Baminercept (BG 9924) is a lymphotoxin-β receptor-immunoglobulin fusion protein that blocks the lymphotoxin-letter/LIGHT axis.

Dazodalibep (MEDI 4920; VIB 4920) is a monoclonal antibody that specifically targets CD40LG/TNFSF5 and is fused to human serum albumin (ALB/HSA) [1].

Thalidomide-O-amido-C3-COOH is a cereblon ligand-linker for PROTACs, melding Thalidomide with a standard linker.

Lodapolimab (LY3300054) is an IgGλ anti- PD-1 monoclonal antibody [1] .

Sym029 is a human IgG monoclonal antibody (mAb) that targets TNFRSF5/CD40. It is applicable for cancer research. The suggested isotype control is Human IgG1 kappa, Isotype Control.

Tubulin/AKT1-IN-1 (Compound D1-1) serves as an inhibitor of both tubulin polymerization and AKT pathway activation, effectively suppressing proliferation and

ACBI3 is a pan-KRAS degrader with anticancer activity, degrading oncogenic KRAS.

Sotigalimab (APX 005) is a monoclonal antibody targeting CD40 with anticancer activity for the study of metastatic pancreatic cancer.

SZUH280 is a potent, selective PROTAC (proteolysis targeting chimera) HDAC8 (histone deacetylase 8) degrader, demonstrating a DC50 of 0.58 μM in A549 cells.

F1324 TFA is a potent, high affinity peptidic inhibitor of B cell lymphoma 6 (BCL6), with an IC50 of 1 nM.

Anti-PD-L1/B7-H1 Antibody (29E.2A3) represents a chimeric antibody of mouse IgG2b, κ type, specifically targeting human PD-L1/B7-H1. The recommended isotype control for this antibody is Mouse IgG2b kappa, Isotype Control.

MI-1061 TFA: potent MDM2 inhibitor, orally bioavailable, stable (IC50=4.4 nM, Ki=0.16 nM), activates p53, induces apoptosis in mice tumors.

CYP51/PD-L1-IN-1 (compound L11), a quinazoline with antifungal properties, simultaneously inhibits CYP51 (IC50: 0.884 μM) and PD-L1 (IC50: 0.083 μM).

Anti-Mouse PD-L1/B7-H1 (LALA-PG) Antibody (10F.9G2) is an IgG2a, κ antibody inhibitor derived from mice, specifically targeting and inhibiting mouse PD-L1/B7-H1.

DEDN6526A (RG-7636) is a humanized ADC compound targeting endothelin B receptor (ETBR), which can be used to study melanoma.

Tanfanercept (HL036337) is an anti-TNF-α antibody, improving corneal erosions in dry eye mice.

Retifanlimab (MGA-012) is a monoclonal antibody targeting programmed cell death protein 1 (PD-1). Retifanlimab is used in studies of Merkel cell carcinoma.

BK50164: CD73 inhibitor, IC50=13.089µM; binds CD99, KD=1.5µM; anticancer, induces apoptosis, arrests sub-G1.

Tibulizumab (LY 3090106) is a bispecific antibody for BAFF & IL-17A; Kds: 60 & 14 pM; for autoimmune research.

hMAO-B-IN-11 (Compound 12) is a selective and reversible inhibitor of human monoamine oxidase B (hMAO-B) with an IC50 value of 0.11 µM. It operates by competitively binding to the active site of hMAO-B, thereby preventing the oxidative deamination of monoamines and reducing hydrogen peroxide production. Additionally, hMAO-B-IN-11 inhibits pro-inflammatory mediators (NO, TNF-α, IL-1β) in activated microglia. This compound holds potential for research in neurodegenerative diseases such as Parkinson's and Alzheimer's.

Ropeginterferon alfa-2b (Ropeginterferon alfa-2b-njft), a monopegylated interferon-alpha (IFN-α), is utilized in the study of myeloproliferative neoplasms [1].

Tilogotamab (GEN-1029) is an agonistic hexameric complex targeting two independent epitopes on DR5, used for studying multiple myeloma (MM).

Citatuzumab bogatox is a recombinant immunotoxin targeting EpCAM with the toxin bouganin, inducing apoptosis in EpCAM-positive tumors.

Thalidomide-4-C3-NH2 HCl is a cereblon ligand for CRBN recruitment, used to make PROTACs with a linker.

Efaprimermin alfa (OMP-336B11) is a human monoclonal antibody that targets TNFRSF18, and functions as a GITR ligand-Fc fusion protein [1].

Latikafusp (AMG 256) is a fusion protein that is a PD-1 blocker and IL-21R agonist with antitumor activity.

Lenercept (Ro 45-2081) is a recombinant fusion protein combining the soluble TNF-receptor (p55) with the Fc portion of human IgG1 [1].

Compound 24a, an FPR1 antagonist, demonstrates potent inhibition of the formyl peptide receptor 1 (FPR1) with an IC50 value of 25 nM.

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

Apoptosis Inducer 11 (compound 3u) promotes apoptosis via the mitochondrial pathway and elicits a G2/M block alongside a marked reduction in the S phase within

HL435 is a heterobifunctional molecule that degrades BRD4 by linking with JQ1, with DC50 values of 11.9 nM and 21.9 nM in MDA-MB-231 and MCF-7 cells, respectively. It inhibits the proliferation of MDA-MB-231, MCF-7, 22Rv1, and A549 cells, arrests the cell cycle, and induces apoptosis. Additionally, HL435 exhibits antitumor activity in mouse models.

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.

2'-Epi-2'-O-Acetylthevetin B (GHSC-74), a cardiac glycoside extractable from Cerbera manghas L.

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.

NAE-IN-1 (compound X-10) is a potent inhibitor of NAE1. It induces apoptosis and causes cell cycle arrest in the G2/M phase. Furthermore, NAE-IN-1 increases ROS levels and inhibits cell migration, demonstrating antiproliferative activity.

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.

Ru-Poma is an Ru(II)-based photosensitizer designed to enhance the efficacy of photodynamic therapy (PDT) against tumors resistant to Cisplatin. It targets Pomalidomide to partially degrade CRBN, inducing ferroptosis by increasing lipid peroxides and downregulating GPX4 and GAPDH expression. In A549 cells, Ru-Poma exhibits cytotoxicity with IC50 values of 18.46 μM in the dark and 0.37 μM under illumination.