cleaved caspase 3

CAY10526 (BTH) is a selective mPGES-1 inhibitor that acts as an inhibitor of the NF-κB signaling pathway.

Polyphyllin D induces apoptosis via the mitochondrial apoptotic pathway as evidenced by decreased Bcl-2 expression levels, disruption of MMP and increased Bax, cytochrome C, and cleaved-caspase-3 levels. Polyphyllin D has an anti-angiogenic effect. Polyphyllin D has toxicity in human RBCs as well as its underlying mechanism for the hemolysis and eryptosis/erythroptosis. Polyphyllin D has strong anticancer activity, can overcome drug resistance in R-HepG2 cells and elicit programmed cell death via mitochondrial dysfunction.

CSRM617 hydrochloride is a selective small-molecule inhibitor of the transcription factor ONECUT2 (OC2, a master regulator of androgen receptor), with a Kd of 7.43 µM in SPR assays, directly binding to the OC2-HOX domain. CSRM617 hydrochloride induces apoptosis through the appearance of cleaved Caspase-3 and PARP and is well tolerated in the mouse model of prostate cancer [1].

Emamectin Benzoate (MK-244), by binding gamma-aminobutyric acid (GABA) receptor and glutamate-gated chloride channels disrupting nerve signals within arthropods, acts as a chloride channel activator.

D-Isofloridoside, a polysaccharide precursor, exhibits free radical scavenging activity and inhibits both ROS expression and the enzymes MMP-2 and MMP-9.

EV206 is a potent Hsp70 inhibitor, demonstrating significant anti-proliferative activity. This compound induces apoptosis and promotes increased protein expression of cleaved PARP and caspase-3, indicating its potential anti-tumor activity.

MAPK-IN-3 (Compound 4a) is an antiproliferative agent demonstrating significant inhibitory effects on KYSE 30, HCT 116, and HGC 27 cell lines, with IC50 values of 0.57 μM, 3.27 μM, and 2.28 μM, respectively. This compound arrests the cell cycle via a p53-dependent mechanism and induces apoptosis through a p53-independent pathway. It reduces the expression of cell cycle-related proteins, such as Cyclin D1 and Cyclin B1, while increasing pro-apoptotic proteins like cleaved PARP, cleaved caspase-7, and cleaved caspase-9. MAPK-IN-3 also decreases anti-apoptotic proteins such as Bcl-2, elevates ROS levels in KYSE 30 cells, and enhances the expression of ROS-related MAPK pathway members, including p-ERK, p-p38, and p-JNK.

TFGF-18 is a GSK-3β inhibitor with an IC50 of 0.59 μM. It suppresses microglial activation and the release of pro-inflammatory mediators induced by LPS by inhibiting GSK-3β and downstream p65/NF-κB signaling. TFGF-18 also prevents neuronal apoptosis and oxidative stress, reduces the expression of Bax, caspase-3, and cleaved-caspase-3, while increasing Bcl-2 expression. It offers neuroprotection by inhibiting neuroinflammation and alleviating cognitive impairment.

Bfl-1-IN-6 is a high-affinity Bfl-1/A1 inhibitor (IC50 = 19 nM). It neutralizes anti-apoptotic effects by binding to the hydrophobic groove of Bfl-1, sensitizing cancer cells to chemotherapy in hematological malignancy research.

Bfl-1-IN-6 trifluoroacetate is a trifluoroacetate form of selective Bfl-1 inhibitor, which can stabilize BFL-1 protein and activate cleaved caspase-3, and has potential application value in targeted anti-apoptotic protein-related tumor therapy.

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.

DNH28 is a potent NF-κB and MAPK inhibitor with an IC50 value of 0.93 μM in HepG2 cells. It induces apoptosis by downregulating Bcl-2 and upregulating BAX and Cleaved-caspase-3 expression. DNH28 can arrest the cell cycle and inhibit cell migration, and is applicable for research in hepatocellular carcinoma (HCC).

HDAC8-IN-14 is a curcumin derivative serving as a selective HDAC8 inhibitor with a Ki of 9 nM. It induces reactive oxygen species (ROS) production, disrupts mitochondrial membrane potential, and promotes apoptosis. Furthermore, HDAC8-IN-14 significantly triggers cell accumulation in the sub-G0/G1 phase, indicative of apoptosis or necroptosis. It upregulates cytochrome c, cleaved caspase-3, and pro-apoptotic protein Bak expression, while maintaining anti-apoptotic protein Bcl-2 levels unchanged, making it a valuable compound for leukemia research.

STING-IN-17 is an orally active inhibitor of STING (human STING IC50= 29 nM, murine STING IC50= 15 nM). It effectively suppresses the phosphorylation of STING, TBK1, and IRF3. The compound inhibits the expression of IP10, IFNB1, and ISG56 mRNA in a dose-dependent manner. Additionally, STING-IN-17 reduces ROS and inhibits the expression of cleaved-PARP/caspase-3. It shows potential for improving renal function and can be utilized in research on inflammatory diseases such as acute kidney injury.

MC3817 is a selective DNMT inhibitor, with IC50 values of 0.044 μM for DNMT1 and greater than 10 μM for DNMT3A/3L. It inhibits P53-dependent cancer cell proliferation, induces apoptosis and DNA damage, and elevates the levels of cleaved Caspase 3, P53, and γH2AX. MC3817 is applicable in research on non-small cell lung cancer, colon cancer, cervical cancer, triple-negative breast cancer, and histiocytic lymphoma.

NPT100-18A is an inhibitor of α-synuclein oligomerization. It can restore cleaved caspase-3 levels to normal. NPT100-18A reduces mitochondrial oxidative stress probe levels in a compartment-specific manner and, at high concentrations, can increase ATP signaling. NPT100-18A is useful for research in Parkinson's disease (PD).

dCDK9-202 is a potent CDK9-PROTAC degrader with a DC50 value of 3.5 nM. It exhibits broad-spectrum antitumor activity and significantly disrupts oncogenic transcriptomes. dCDK9-202 activates Caspase-3/7, increases levels of cleaved PARP, and directly induces tumor cell apoptosis (apoptosis). It effectively inhibits the growth of TC-71 tumors without any observed toxicity in mice. dCDK9-202 is applicable for researching EGFR-driven cancers, such as sarcomas.

MC3817 free base is a selective DNMT inhibitor with an IC50 value of 0.044 μM for DNMT1 and greater than 10 μM for DNMT3A/3L. It suppresses P53-dependent cancer cell proliferation, induces apoptosis and DNA damage, and increases the levels of cleaved Caspase 3, P53, and γH2AX. MC3817 free base is applicable in research related to non-small cell lung cancer, colon cancer, cervical cancer, triple-negative breast cancer, and histiocytic lymphoma.

CSN5-IN-3 (Compound 30) is a CSN5 inhibitor with an IC50 value of 0.58 μM. It inhibits the enzymatic activity of CSN5, leading to increased accumulation of NEDD8-Cul1 and promoting the degradation of PD-L1. CSN5-IN-3 downregulates Bcl-2, while upregulating P53 and Cleaved caspase-3, exhibiting anticancer properties against triple-negative breast cancer.

ICD inducer-2 is an inducer of immunogenic cell death that binds to the colchicine binding site on tubulin, thereby inhibiting tubulin polymerization. It demonstrates broad-spectrum antiproliferative activity across various cancer cell lines and inhibits cell migration while causing G2/M phase arrest and inducing apoptosis. Additionally, it promotes CD4+ and CD8+ T cell infiltration into the tumor microenvironment. ICD inducer-2 decreases Bcl-2, an anti-apoptotic protein, and increases pro-apoptotic proteins Bax and Bim-1, as well as cleaved forms of caspase 3, caspase 9, and PARP. It also overcomes paclitaxel resistance in xenograft models, leading to tumor growth inhibition, and is applicable in cancer-related research, such as lung cancer studies.

(E)-3,4-Dimethoxycinnamic acid is a less active isomer of 3,4-dimethoxycinnamic acid, a natural monomer from Securidaca inappendiculata Hassk. It exerts anti-apoptotic effects in L-02 cells via ROS-mediated signaling, showing potential in research related to inflammation and immunology.

Downregulate phosphorylation of STAT3, increase the expression of cleaved caspase-3, inhibit cell cycle progression and promote apoptosis in breast and pancreatic cancer cells with low micromolar to nanomolar IC50 values. Furthermore, HJC-0123 significantly suppressed estrogen receptor (ER)-negative breast cancer MDA-MB-231 xenograft tumor growth in vivo (p.o.), indicating its great potential as an efficacious and orally bioavailable drug candidate for human cancer therapy.

Lig4-4 is a TREK-1 current inhibitor (IC50 = 2.06 μM) that has demonstrated potential for use as a protective agent against cerebral ischemia. It has been postulated that the neuroprotective effects of Lig4-4 against cerebral ischemia may be attributed to the modulation of Bcl-2 and cleaved-caspase-3 expression, leading to the inhibition of neuronal apoptosis.

Anticancer agent 137 (8q), a potent PI3k inhibitor, exhibits broad-spectrum anticancer activity by inducing G2/M cell cycle arrest and apoptosis. It increases levels of cleaved PARP, and caspases 3 and 7, making it useful in cancer research [1].