Apoptosi

EGFR-IN-169 is an epidermal growth factor receptor (EGFR) inhibitor derived from ginsenoside, with an IC50 of 5.19 μM. It disrupts colorectal cancer cell migration and growth by inhibiting the EGFR-mediated RalA/EMT pathway. With an IC50 of 4.46 μM against HCT-116 cells and a selectivity index (SI) of 16.92, EGFR-IN-169 also inhibits CDKs, induces G0/G1 cell cycle arrest, and suppresses cell migration and invasion. Additionally, EGFR-IN-169 reduces mitochondrial membrane potential, induces apoptosis and reactive oxygen species (ROS) production. It is applicable in cancer research, particularly for colorectal cancer.

TNF-α/IL-1β-IN-1 (compound 11a) is an anti-inflammatory agent that effectively reduces the expression of TNF-α and IL-1β, inhibits oxidative stress and myocardial cell apoptosis, and demonstrates significant activity against septic myocardial injury. Additionally, it improves myocardial blood flow in vivo.

BRD9 Ligand-5 (Compound 172-11) serves as a ligand for the target protein in PROTAC applications. It is utilized in the synthesis of CFT8634.

1D09C3 is a fully humanized anti-HLA-DR monoclonal antibody. It induces cell apoptosis (apoptosis) and death through a cascade of reactions, including reactive oxygen species (ROS) production, JNK activation, mitochondrial membrane depolarization, and the release of AIF from mitochondria. In xenograft models with JVM-2 cells and GRANTA-519 cells in mice, 1D09C3 demonstrated significant antitumor activity, improving overall survival and median survival time. This compound is applicable in cancer research, including studies on chronic lymphocytic leukemia (CLL).

PROTACc-Met degrader-6 is a potent and orally active c-Met PROTAC degrader. It effectively promotes the degradation of c-Met protein, with DC50 values of 0.52 nM in EBC-1 cells and 0.45 nM in Hs746T cells. This compound almost completely abolishes the migration and invasion capabilities of tumor cells, significantly induces apoptosis (apoptosis), and arrests the cell cycle at the G0/G1 phase. PROTACc-Met degrader-6 is useful for studying various cancers, including non-small cell lung cancer and gastric cancer.

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).

Apoptosisinducer 31 (compound 19) triggers caspase-dependent apoptosis (cell death). It plays a crucial role in cancer research.

Antitumor agent-196 (Compound 6a (β, β, β)) is an artemisinin-based oligomer with anticancer properties, exhibiting an IC50 of 90 nM against MCF-7 breast cancer cells. This compound induces apoptosis by modulating the Bax-caspase 3 signaling pathway and triggers ferroptosis by regulating key signaling molecules (including GPX4). Antitumor agent-196 shows potential for cancer research applications.

(GalNAc)3-CPT is a glycan-conjugated prodrug that targets the asialoglycoprotein receptor (ASGR) overexpressed on liver cells. It demonstrates significant antitumor activity by activating the cGAS-STING pathway and promoting CD8+ T cell infiltration into tumor sites, leading to apoptosis of tumor cells. In HepG2 cells, it shows an IC50 value of 3.07 μM.

OBHSA（Oxabicycloheptane sulfonamide） is a novel selective estrogen receptor depressant (SERD) that can be used to study breast cancer.

GLPG4970 is a potent, selective, orally active dual inhibitor of salt-inducible kinases 2 and 3 (SIK2/SIK3), with IC50 values of 0.3 nM and 0.7 nM, respectively. It exhibits weak inhibition of the hERG channel, with an IC50 value of 29 μM. GLPG4970 reduces the release of tumor necrosis factor α (TNFα) and increases the release of interleukin 10 (IL-10). This compound is applicable for research in inflammation and immunology, such as studies on colitis.

dASK1 is a selective CRBN-based PROTAC degrader targeting apoptosis signal-regulating kinase 1 (ASK1). It forms a stable ternary complex with ASK1, facilitating its rapid and sustained degradation via the ubiquitin-proteasome pathway. dASK1 exhibits strong ASK1 degradation capabilities and is applicable for hepatitis research.

Thymocartin Acetate, a thymopoietin fragment (32-35), inhibits enzyme breakdown; potential for immunodeficiency treatment.

F3-PEG8-RiboTAC is a RiboTAC compound that specifically degrades the mRNA of the oncogene LGALS1. This compound can induce apoptosis (cell death) in tumor cells and inhibit their invasion. F3-PEG8-RiboTAC exhibits antitumor activity and is applicable in research on leukemia and triple-negative breast cancer. (RNase L ligand; RNA binder; Linker)

Ac-WEHD-AFC TFA: a fluorogenic substrate detecting caspase-1 activity, used in tumor and inflammation research.

VTX-0811 is a human IgG4 monoclonal antibody (mAb) that targets PSGL1/CD162. It modulates immune signaling pathways by enhancing TNF-α/NF-κB and chemokine-mediated signaling while reducing oxidative phosphorylation, fatty acid metabolism, and Myc signaling. VTX-0811 increases the proportion of CD8+ T cells among infiltrating T cells and exhibits antitumor activity in humanized mouse PDX models of melanoma.

DSTYSLSSTLTLSK TFA detects infliximab, a chimeric IgG1 antibody targeting TNF-α.

STEP-IN-1 (Compound 14b) is a potent and selective inhibitor of STEP, with an IC50 of 5.27 μM. It offers neuroprotective effects by safeguarding neuronal cells from glutamate-induced toxicity, reducing intracellular reactive oxygen species (ROS) accumulation, and inhibiting apoptosis. STEP-IN-1 is applicable in research related to neurodegenerative diseases.

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.

Y2641, a tetrahydro β-carboline derivative, is an orally active dual inhibitor of RANKL and TNF-α, with Kd values of 3.984 μM and 18.59 μM respectively. It suppresses RANKL-induced osteoclastogenesis and exhibits anti-inflammatory and cartilage-protective properties. Y2641 is applicable in osteoarthritis research.

CGP-74514,CDK1 inhibitor (IC50=25 nM). Induces G2/M arrest, apoptosis. Used in bladder cancer research.

PROTACPI3K/110β degrader-2 is a selective PI3K/p110β PROTAC degrader. It effectively degrades the 110β protein and inhibits the expression of P-glycoprotein. Additionally, it increases reactive oxygen species (ROS) levels. PROTACPI3K/110β degrader-2 exerts antitumor effects by activating the endoplasmic reticulum stress (ERS) mediated mitochondrial apoptosis pathway and inhibiting the AKT/Bcl-2 signaling pathway. This compound is applicable in cancer research.

YTHu78 is a KDM5B PROTAC-based degrader. It induces the degradation of KDM5B through the ubiquitin-proteasome system and triggers apoptosis in MV-4-11 and MM.1S cell lines. YTHu78 demonstrates significant antiproliferative activity against various hematologic tumor cell lines and is useful for studying hematological malignancies.

GJ19 is a PD-L1 inhibitor with an IC50 of 32.06 nM. It binds effectively to human and mouse PD-L1 proteins, exhibiting KD values of 171 nM and 290 nM, respectively. In a co-culture model of HepG2/hPD-L1 and Jurkat T/hPD-1 cells, GJ19 promotes HepG2 cell death in a concentration-dependent manner. In the B16-F10 melanoma mouse model, GJ19 demonstrates significant tumor growth inhibition. GJ19 is applicable in tumor immunotherapy research.

(+)-Mcl-1 inhibitor 21 (Example 1-37) is a chemical compound that acts as an Mcl-1 inhibitor with an IC50 value of 172 nM. It demonstrates pro-apoptotic and antiproliferative activities in SUDHL5 and SUDHL10 cell lines, making it useful for cancer research.

WH244 is a second-generation dual degrader (PROTAC) targeting BCL-2 and BCL-xL proteins. It effectively degrades these proteins with high specificity, exhibiting a DC50 of 0.6 nM for BCL-xL and 7.4 nM for BCL-2. By promoting ubiquitination and subsequent proteasomal degradation of these proteins, WH244 restores apoptotic pathways in cells. The compound shows strong antitumor activity.

PDE4-IN-28 (Compound G1) is an inhibitor of PDE4D, with an IC50 of 29 nM. It suppresses the production of TNF-α and NO, with IC50 values of 13.32 μM and 2.32 μM, respectively. In a rat pressure ulcer (PU) model, PDE4-IN-28 exhibits anti-inflammatory, antibacterial, and analgesic properties, while promoting HUVEC cell migration to enhance wound healing.

FTI 277, a FTI 276 prodrug, blocks farnesyltransferase (IC50 = 0.5 nM), H-Ras/K-Ras processing, and fights tumor cell growth.

DefNEtTrp is an iron bis-chelating ligand composed of Def and Trp groups. It demonstrates potent broad-spectrum antiproliferative and cytotoxic effects in cancer cell lines. DefNEtTrp induces apoptosis and ferroptosis, exhibiting cytotoxicity with an IC50 value of 0.77 μM.

CDK4/6/HDAC-IN-1 (Compound N14) is a dual-target inhibitor of CDK4/6 and HDAC, with IC50 values of 7.23 nM for CDK4, 13.20 nM for CDK6, 55.66 nM for HDAC1, and 48.38 nM for HDAC6. It induces apoptosis and G0/G1 phase arrest through the HDAC-p21-CDK signaling pathway and can inhibit hepatocellular carcinoma.

GSNOR-IN-1 is a prodrug of GSNOR-IN-2 and functions as an S-nitrosoglutathione reductase (GSNOR) inhibitor capable of crossing the blood-brain barrier. GSNOR-IN-1 offers significant protective effects against damage induced by oxygen-glucose deprivation/reoxygenation (OGD/R). It regulates calcium signaling and synaptic function through Clstn1 S-nitrosylation and inhibits neuronal apoptosis. Additionally, GSNOR-IN-1 markedly reduces infarct volume in rat models of ischemic stroke while enhancing neurological function. With its neuroprotective properties, GSNOR-IN-1 holds potential for ischemic stroke research.

Thujopsene, a sesquiterpene found in T. dolabrata, exhibits a wide range of biological activities. It inhibits Na+/K+-ATPase and cytochrome P450 (CYP) isoform CYP2B6 with IC50 values of 25.9 µg/ml and Ki of 0.8 µM, respectively. Additionally, thujopsene demonstrates antimicrobial efficacy against both Gram-positive and Gram-negative bacteria, such as S. aureus, M. luteus, and S. typhimurium, with MICs ranging from 25-50 µg/ml. It also suppresses antigen-induced β-hexosaminidase release in IgE-sensitized RBL-2H3 mast cells (IC50= 25.1 µM) and shows cytotoxicity against A549 non-small cell lung cancer cells with an LC50 of 35.27 µg/ml. Furthermore, thujopsene causes mortality in mites D. farinae and T. putrescentiae, with LC50s of 9.82 and 10.92 µg/cm2, respectively.

Insect repellent M 3535 is a bug repellant.

Fosimdesonide, a small molecule analog of adalimumab, serves as a potent immunomodulator with demonstrated anti-inflammatory activity [1].

Perfluorodecanoic acid is a biochemical.

Frangulin B (Compd 11g) exhibits anticancer properties and acts as an effective RecQ helicase inhibitor. It induces apoptosis in both HCT-116 and MDA-MB-231 cells and can arrest HCT-116 cells in the G2/M phase.

BAD (103-127) human peptide from BH3 domain, blocks Bcl-xL, 800x more binding than 16-mer.

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

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.

PROTACc-Met degrader-5 (Compound D19) is an orally active c-Met PROTAC degrader, with a DC50 of 0.42 nM in EBC-1 cells and 0.32 nM in Hs746T cells. It effectively induces apoptosis, causes G1 cell cycle arrest, and inhibits cell migration and invasion. This compound shows strong antiproliferative and degradative effects on c-Met-dependent cancer cells and those resistant to Tepotinib.

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.

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.

CH091138 is a potent and selective KRASG12D PROTAC degrader, exhibiting a DC50 value of 148.3 nM in HeLa cells and 469.8 nM in AsPC-1 cells. It selectively targets both exogenous and endogenous KRASG12D through the VHL-mediated ubiquitin-proteasome system, without affecting KRASWT or other KRAS mutants (G12C/G12S/G12V). CH091138 demonstrates significant antitumor activity by inducing apoptosis (apoptosis) in tumor cells and is applicable for research in pancreatic and colon cancers.

FLT3/IRAK4-IN-1 is a selective inhibitor of FLT3 and IRAK4, exhibiting significant activity against FLT3-WT (IC50= 1.95 nM), FLT3-D835Y (IC50= 3.22 nM), and IRAK4 (IC50= 53.72 nM). It demonstrates low cytotoxicity towards normal bone marrow cells, effectively promotes apoptosis, and has potential to overcome resistance. FLT3/IRAK4-IN-1 can be utilized in studies of acute myeloid leukemia (AML).

GDC-0152-acetamide is a pan-antagonist of apoptosis inhibiting proteins (IAPs). It induces the autoubiquitination and subsequent degradation of cIAP1/2, activates the non-canonical NF-κB pathway, and promotes the secretion of TNF-α, leading to apoptosis in tumor cells. GDC-0152-acetamide holds potential for research in ERα-positive breast cancer.

Bcl-2-IN-23 (compound 5) is a selective inhibitor targeting Bcl-2. It demonstrates an IC50 range of 25.7-33.7 μM in HTB-140, HeLa, and SW620 cells. Acting through non-covalent competitive binding to the Bcl-2 protein, Bcl-2-IN-23 significantly reduces Bcl-2 expression, inducing late-stage apoptosis and necroptosis in cancer cells. By disrupting the Bcl-2-mediated mitochondrial apoptotic inhibition pathway, it increases cancer cell susceptibility to apoptosis and reduces the release of the inflammatory factor IL-6. Bcl-2-IN-23 is applicable in anti-apoptosis research for malignant tumors such as melanoma, cervical cancer, and colorectal cancer.

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