caspase-3-in-1

Caspase-3-IN-1 is a potent inhibitor of Caspase-3 (IC50: 14.5 nM).

1. Ginkgetin has anti-influenza virus and anti-fungal activities. 2. Ginkgetin has anti-inflammatory activity, can down-regulates COX-2 induction in vivo against skin inflammatory responses. 3. Ginkgetin is a good STAT3 inhibitor and may be a useful lead

1. Dehydrocorydaline (13-Methylpalmatine) exerts anti-metastatic potential via suppression of MMPs and Bcl-2 signaling in NSC-LC cells. 2. Dehydrocorydaline stimulates p38 MAPK activation, which can enhance heterodimerization of MyoD and E proteins, thus resulting in MyoD activation and myoblast differentiation. 3. Dehydrocorydaline shows antiplatelet effects, it inhibits thrombin-induced platelet aggregation in a low dose ( IC50= 34.914 ug/mL). 4. Dehydrocorydaline has anti-inflammatory and antinociceptive effects. 5. Dehydrocorydaline inhibits MCF-7 cell proliferation by inducing apoptosis mediated by regulating Bax/Bcl-2, activating caspases as well as cleaving PARP.

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].

ALPHA-PINENE ((-)-Alpha-Pinene) is a bicyclic monoterpene found in pine trees and other plants, including Cannabis with diverse biological activities [1]. It reduces the growth of a panel of seven Gram-positive bacteria, seven Gram-negative bacteria, and eight yeast strains with MIC values of 0.75-1.29, 1.05-1.59, and 0.7-1.17%, respectively [2]. It has insecticidal activity against C. molestus larvae with LC50 values ranging from 47 to 49 mg/L.3 ALPHA-PINENE (100 μg/ml) induces apoptosis, increases anion superoxide production and DNA fragmentation, and activates caspase-3 in B16/F10 melanoma cells [4]. In a B16/F10 mouse xenograft model, ALPHA-PINENE(100 ml of a 10 mg/ml solution) reduces the number of metastatic lung nodules by approximately 7-fold. ALPHA-PINENE(8.6 mg/L, aerosol) also increases the time spent in the open arms of the elevated plus maze by approximately 2-fold in mice, indicating anxiolytic-like activity [5].

VU0285655-1(BML-280) is a potent and selective phospholipase D2 (PLD2) inhibitor that inhibits the proliferation of PLD2-deficient cells.VU0285655-1 has an inhibitory effect on high glucose-induced caspase-3 cleavage and reduction of cell viability.VU0285655-1 is used in the study of diabetic retinopathy.

PDK4-IN-1 hydrochloride, an anthraquinone derivative, is a potent and orally active inhibitor of pyruvate dehydrogenase kinase 4 (PDK4) with an IC50 value of 84 nM.

15-Acetoxyscirpenol, a member of the acetoxyscirpenol moiety mycotoxins (ASMs), potently induces apoptosis and inhibits the growth of Jurkat T cells in a dose-dependent manner. This effect is mediated through the activation of caspases independent of caspase-3[1].

Nigericin is a polyether antibiotic with potent antimicrobial, antimalarial, anticoronaviral and anticancer activities. It is capable of promoting cellular potassium efflux, inducing Caspase-1/GSDMD and Caspase-3-mediated cellular pyroptosis and apoptosis in triple-negative breast cancer, and inducing apoptosis in PEL (primary exudative lymphoma) cells through mitochondrial dysfunction and Wnt/β-catenin signaling downregulation.

Tubulin polymerization-IN-68 (compound 32) serves as a tubulin inhibitor, disrupting cellular microtubule networks by hindering tubulin polymerization. It also upregulates PARP-1 and caspase-3 expression, thereby inducing apoptosis and exhibiting anticancer properties. Notably, Tubulin polymerization-IN-68 effectively suppresses HepG2 cells with an IC50 of 93 nM and markedly reduces the growth of HepG2 xenograft tumors in nude mice through oral administration.

PARP1-IN-31 (compound 11f) is a PARP1 inhibitor with an IC₅₀ of 97 nM. It induces apoptosis and inhibits proliferation in lung cancer cell lines (e.g., A549), while upregulating caspase-3 and caspase-9, making it suitable for lung adenocarcinoma research.

Bfl-1-IN-5 (Compound (R,R,S)-26) is a selective inhibitor of Bfl-1, demonstrating an IC50 of 0.022 μM. This compound enhances the activity of caspase-3/7, with an EC50 of 0.37 μM, and also inhibits the viability of SU-DHL-1 cells, showing an EC50 of 1.3 μM.

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.

Aβ aggregation-IN-1 (Compound 1b) is an inhibitor of amyloid-beta precursor protein. It suppresses the aggregation and disaggregation of amyloid-beta fibrils with IC50 values of 3.92 and 7.19 M, respectively. Additionally, Aβ aggregation-IN-1 reduces malondialdehyde formation in neuronal cells, increases intracellular levels of reduced glutathione (GSH), and inhibits caspase 3.

HTR2A antagonist 1 (Compound 15f) is an HTR2A antagonist with an IC50 of 42.79 nM. It induces sub-G1 cell cycle arrest and apoptosis in colorectal cancer cells by activating the p53/p21/caspase 3 signaling pathway. HTR2A antagonist 1 exhibits good liver microsomal stability and is useful for colorectal cancer research.

TCF4/β-catenin-IN-1 (Compound 8b) is an inhibitor of TCF4/β-catenin that induces apoptosis. This compound enhances the expression of p53, caspase-3, caspase-8, caspase-9, and Bax proteins, while reducing Bcl-2 protein levels. TCF4/β-catenin-IN-1 also inhibits CYP3A4, CYP1A2, and CYP2C19, demonstrating significant cytotoxic activity in cancer cells.

CDK9degrader-1 is a selective CDK9 degrader (DC50: 0.4073 µM). It recruits ATG101 to initiate the autophagy-lysosome pathway and forms autophagosomes by recruiting LC3, which then fuse with lysosomes to degrade CDK9 and its partner protein, Cyclin T1 (DC50: 1.215 µM). CDK9degrader-1 induces caspase 3-mediated apoptosis and exhibits antitumor activity in a mouse HCT116 xenograft model.

PeS-9 is an androgen receptor (AR) degrader that induces the degradation of androgen receptors. It enhances the production of cytotoxic reactive oxygen species (ROS), leading to mitochondrial and endoplasmic reticulum stress, which results in the release of mitochondrial cytochrome C and AIF. PeS-9 activates caspase-9 and caspase-3, causing DNA fragmentation and apoptosis. It exhibits anti-prostate cancer activity and demonstrates antitumor and antimetastatic effects in vivo with minimal side effects. PeS-9 is applicable for targeted therapy research in GLUT-1 overexpressing tumors.

COX-2-IN-55 (compound 1) is an orally active Celecoxib analogue with broad-spectrum anticancer properties and relatively weak COX-2 inhibition. It specifically inhibits SERCA2, leading to increased caspase-3 cleavage and DR5 levels, which activates GRP78 and suppresses the progression of triple-negative breast cancer (TNBC). Additionally, COX-2-IN-55 downregulates the angiogenesis markers VEGF-α and IL-8, thereby inhibiting microvessel formation.

XIAP-CASP7 PPI-IN-1 is a reversible inhibitor of the XIAP:CASP7 interaction, effectively disrupting the connection between XIAP and CASP7. It selectively induces apoptosis in MCF-7 and caspase-3 low-expression (CASP3/DR) triple-negative breast cancer cells. The compound overcomes chemoresistance by down-regulating β-catenin and associated ABC transporters in paclitaxel-resistant MCF-7 cells. XIAP-CASP7 PPI-IN-1 is useful for breast cancer research.

TopoisomeraseI/II-IN-1 is a dual inhibitor of Topoisomerase I and II. It induces G2/M cell cycle arrest and apoptosis (apoptosis) in cancer cells by increasing the levels of p53, p21, Bax mRNA, and caspase-3 proteins, as well as the Bax/Bcl-2 ratio, while decreasing Bcl-2 levels. This compound is useful for research on various cancers such as melanoma, renal cancer, colorectal cancer, and breast cancer.

p-nitro-Pifithrin-α is a cell-permeable analog of pifithrin-α, a potent p53 inhibitor. It suppresses p53-mediated TGF-β1 expression in HK-2 cells and inhibits the activation of caspase-3 by Zika virus (ZIKV) strains. Moreover, p-nitro-Pifithrin-α attenuates steatosis and liver injury in mice subjected to a high-fat diet, mitigating the effects of non-alcoholic fatty liver disease [1] [2] [3] [4].

NLRP3-IN-9 (INF-4E) is an inhibitor of NLRP3 ATPase and caspase-1. NLRP3-IN-9 acts by irreversibly trapping thiol nucleophiles, which prevents both ATP- and nigericin-triggered pyroptosis of human THP-1 cells in a time- and concentration-dependent manner.

1. Dehydrocorydaline(DHC) not only inhibits antibody-mediated allergic reactions but also influences cell-mediated allergic reactions, and the inhibitory effect of Corydalis Tuber on allergic reactions may be partially attributed to DHC. 2. Dehydrocorydal