Apoptosis

Tralokinumab: human IgG4 monoclonal antibody, blocks IL-13, may treat atopic dermatitis.

5α-dihydro Levonorgestrel is a metabolite of the synthetic progestin levonorgestrel .

RBN013209 is a potent CD38 inhibitor. RBN013209 is useful in the treatment of cancer.

Epoprostenol sodium (Prostaglandin I2 sodium salt) is a vasodilator and a synthetic prostacyclin that can be used to study pulmonary hypertension.

Ecdysone is a major steroid hormone in insects and herbs.

HPOB is an effective and specific HDAC6 inhibitor (IC50: 56 nM), >30-fold selectivity over other HDACs.

Pim-1 kinase inhibitor 4 is a potent Pim-1 kinase inhibitor with an IC50 value of 17.01 nM.Pim-1 kinase inhibitor 4 also possesses antioxidant activity and

GPI-1485 (GM1485) (GM1485) is a nonimmunosuppressive immunophilin ligand, promoting neurofunctional improvement and neural regeneration following stroke.

Diethylnorspermine HCl (N1,N11-Diethylnorspermine tetrahydrochloride) potently induces SSAT (spermidine/spermine N1-acetyltransferase) mRNA and effectively

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.

E3 ligase Ligand 36 is an E3 ligase ligand that can be utilized for synthesizing PROTACs, such as PROTAC BRM/BRG1 degrader-1.

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.

Obestatin (human) is an endogenous ligand for G-protein eurythmic entity 39 formed by shearing of preproghrelin and can be used to study obesity.

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.

BC13 is a CDK6/BRD4 inhibitor with IC50 values of 234 nM for CDK6 and 36 nM for BRD4. It exhibits antiproliferative properties, induces apoptosis (cell death) and DNA damage, and elevates ROS levels.

Tat-ASIC1a (1-20) (mouse, rat) is a competitive ASIC1a transmembrane peptide with significant neuroprotective effects. It alleviates acidotoxic neuronal damage by targeting the ASIC1a-RIPK1 pathway and an auto-inhibition mechanism. This compound effectively safeguards the brain in ischemic stroke mouse models against damage from ischemia and is applicable in research on neurodegenerative diseases, such as Huntington's disease and Parkinson’s disease.

(+)-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.

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.

ISB2001 is a human trispecific antibody targeting CD38, CD3, and BCMA. It is applicable for research on relapsed/refractory multiple myeloma (RRMM). The recommended isotype control is IgG1-kappa-IgG1-Fab.

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.

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.

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.

PK7088, a pyrazole-based peptide, selectively reactivates mutant p53 to a conformation with wild-type characteristics, demonstrating anticancer activity in

C8 D-threo Ceramide, a potent bioactive sphingolipid, is cytotoxic with IC50=17µM, enhances DNA fragmentation and pore formation, and activates CAPK.

CSN5-IN-1 (compound Ac-11) serves as an inhibitor of CSN5, exhibiting IC50 values of 12.56 μM in FP assay and 19 μM in fluorescence assay. Additionally, it influences cellular protein expression by downregulating PD-L1 and upregulating NEDD8-Cul1.

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.

N-methyl Paroxetine, a potent SSRI derivative with Ki=4.3 nM, blocks serotonin reuptake (IC50=22 nM) and is a precursor/impurity in paroxetine synthesis.

Biguanidinium-porphyrin free TFA is a mitochondrial-targeting photosensitiser exhibiting low dark toxicity towards human hepatocellular carcinoma HEp2 cells.

Thyrotropin (TSH), a thyroid-stimulating hormone, is synthesized by thyrotrope cells in the anterior pituitary gland and modulates the endocrine activity of the

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

PROTAC ATR degrader-2 (Compound 8i) serves as a PROTAC degrader targeting ATR, effectively degrading it in acute myeloid leukemia (AML) cell lines MV-4-11 and MOLM-13, with DC50 values of 22.9 and 34.5 nM, respectively. This compound induces apoptosis and inhibits the proliferation of AML cells. Additionally, PROTAC ATR degrader-2 demonstrates favorable pharmacokinetic properties and potent antitumor activity in a mouse model of AML.

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

XY077 (compound 14a) is a RORγ inverse agonist with an IC50 value of 0.004 μM. It induces cell apoptosis (cellapoptosis) and exhibits antiproliferative activity both in vitro and in vivo.

Dynorphin A TFA: endogenous peptide, potent KOR agonist, affects CNS, involved in neuron death research.

Bcl-2-IN-21 (compound C1), an iridium-based anticancer agent, effectively targets and inhibits Bcl-2, thereby impeding cancer cell colony formation and promoting increased levels of Bax and caspase 3.

PROTACFLT-3degrader 4 is an orally active CRBN-based FLT3-PROTAC degrader that efficiently induces the degradation of FLT3-ITD via the ubiquitin-proteasome system. It demonstrates high selectivity for FLT3-ITD mutant acute myeloid leukemia (AML) cells. [Blue: CRBN ligand, Black: linker; Pink: FLT3 inhibitor].

MD-265 is a PROTAC degrader that targets and degrades MDM2, leading to the activation of p53 in cancer cells with wild-type p53. MD-265 achieves complete tumor regression and enhances long-term survival in leukemic mice.

c-Fos-IN-1 (Compound P16) acts as a c-Jun inhibitor, effectively reducing the mRNA and protein levels of c-Fos. It also inhibits the phosphorylation activity of ERK and the transcriptional activity of AP-1. This compound demonstrates anticancer properties through the inhibition of the ERK/c-Fos/Jun pathway. c-Fos-IN-1 curbs the proliferation and migration of gastric cancer cells, with an IC50 of 2.31 μM for MGC-803 cells, causing cell cycle arrest at the G2/M phase and inducing apoptosis in cancer cells. Additionally, c-Fos-IN-1 hampers the growth of gastric cancer tumors.

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.

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.