Caspase Activator

Cucurbitacin IIa (Hemslecin A) (Standard) is the analytical standard for Cucurbitacin IIa (HY-N1988). This product is used for research and analytical applications. Cucurbitacin IIa is an orally active, blood-brain barrier-penetrating EGFR inhibitor with an IC₅₀ of 1.455 nM for human EGFR. Cucurbitacin IIa induces caspase-3 dependent cell apoptosis, downregulates survivin expression, enhances autophagy levels, disrupts the actin cytoskeleton through actin aggregation, blocks the cell cycle at the G2/M phase, and inhibits the EGFR-MAPK signaling pathway to exert anti-inflammatory activity. Cucurbitacin IIa can be used in research on inflammatory-related diseases, depression, and non-small cell lung cancer and other cancers.

Pan-PDK degrader-1 is a pan-PDK class PROTAC degrader that degrades PDK2, PDK3 and PDK4 with DC₅₀ values of 9.2 nM, 9.9 nM and 11.5 nM, respectively. Pan-PDK degrader-1 recruits the mitochondrial protease HsClpP and induces selective pan-PDK degradation via HsClpP-mediated proteolysis. Pan-PDK degrader-1 reprograms mitochondrial metabolism toward oxidative phosphorylation, promoting ROS accumulation, mitochondrial permeability transition pore opening, endogenous mitochondrial apoptosis, calreticulin exposure and HMGB1 release. Pan-PDK degrader-1 upregulates cleaved Caspase-9, Caspase-3 and PARP. Pan-PDK degrader-1 inhibits primary and distal tumor growth via selective degradation of PDK in tumor tissues. Pan-PDK degrader-1 can be used for the research of breast cancer.

Bcl-2-IN-6 (compound 10) is a potent Bcl-2 (B-cell lymphoma-2) inhibitor. Bcl-2-IN-7 down-regulates the expression of Bcl-2, and increases the expression of p53, Bax, and caspase-7 mRNA. Bcl-2-IN-7 induces cell cycle arrest and apoptosis in breast cancer MCF-7 cells. Bcl-2-IN-7 shows good anticancer activity, with IC₅₀ values of 20.91, 22.30, 42.29, and 48.00 μM against MCF-7, LoVo, HepG2, and A549 cell lines, respectively.

Dynorphin A TFA is an endogenous opioid peptide involved in inhibitory neurotransmission in the central nervous system (CNS). Dynorphin A TFA is a highy potent kappa opioid receptor (KOR) agonist, and is also an agonist for other opioid receptors, such as mu (MOR) and delta (DOR). Dynorphin A TFA can induce neuronal death, and can be used in the research of neurological disease.

Topoisomerase I-IN-20 is a Topoisomerase I inhibitor. Topoisomerase I-IN-20 disrupts DNA synthesis and transcription, thereby inhibiting the proliferation and migration of cancer cells. Topoisomerase I-IN-20 induces S-phase cell cycle arrest and mitochondria-mediated Apoptosis in cancer cells, which is characterized by upregulated expression of p53, Bax, caspase-3 and caspase-9, along with downregulated expression of Bcl-2. Topoisomerase I-IN-20 increases intracellular ROS levels. Topoisomerase I-IN-20 is applicable to lung cancer-related research.

Vernodalin is an orally active, cytotoxic sesquiterpene lactone with a K_d value of 9.55 μM for p38 MAPK. Vernodalin downregulates the expression of phosphorylated ERK, JNK, AKT, PI3K, mTOR, p38MAPK, FAK, MMP-2, MMP-9, and uPA, while upregulates the expression of TIMP-1 and TIMP-2. Vernodalin increases ROS production, upregulates the expression of Bax and caspase 3, downregulates the expression of Bcl-2, and induces apoptosis (apoptosis), oxidative stress response and cell cycle arrest. Vernodalin inhibits the proliferation, adhesion and metastasis of cancer cells. Vernodalin enhances the activity of VEGF-B, AMPK and eNOS signaling pathways. Vernodalin alleviates myocardial injury and restores hemodynamic parameters. Vernodalin inhibits the growth of Trypanosoma brucei rhodesiense. Vernodalin can be used in research related to various cancers including gastric cancer, colorectal cancer and lung cancer, as well as African human trypanosomiasis and myocardial infarction.

AKN-028 TFA, a novel tyrosine kinase (TK) inhibitor, is a potent, orally active FMS-like receptor tyrosine kinase 3 (FLT3) inhibitor with an IC₅₀ value of 6 nM. AKN-028 TFA inhibits FLT3 autophosphorylation. AKN-028 TFA induces dose-dependent cytotoxic response (mean IC₅₀=1 μM). AKN-028 TFA induces apoptosisby activation of caspase 3. AKN-028 TFA can be used in research of acute myeloid leukemia (AML).

VEGFR/PD-L1-IN-1 is a VEGFR2 and PD-L1 inhibitor, with IC₅₀ values of 0.383 μM and 134.407 pg/mL against VEGFR2 and PD-L1, respectively. VEGFR/PD-L1-IN-1 enhances the secretion of INF-γ, induces G0/G1 cell cycle arrest in cancer cells, and triggers cancer cell apoptosis. VEGFR/PD-L1-IN-1 upregulates the expression of BAX and Caspase-3, and downregulates the expression of Bcl-2. VEGFR/PD-L1-IN-1 can be used in research related to hepatocellular carcinoma, prostate cancer, and colorectal cancer.

Lb54 is a caspase-3 and caspase-7 activator with an EC₅₀ of 660.9 nM for human procaspase-3. Lb54 activates caspase-3/7, which cleaves Gasdermin D (GSDMD) at aspartic acid residue 87 to generate a p10 fragment, preventing formation of the pore-forming p30 fragment of GSDMD. Lb54 suppresses GSDMD-mediated pyroptosis through caspase-3/7 activation, thereby attenuating inflammatory responses and conferring protection against sepsis. Lb54 alleviates acute lung injury, and inhibited systemic inflammation by restraining the maturation of monocyte-derived dendritic cells. Lb54 can be used for the research of sepsis.

EGFR/HER2-IN-17 (Compound 7h) is a dual inhibitor of epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2). EGFR/HER2-IN-17 inhibits cancer cell proliferation. EGFR/HER2-IN-17 interacts with the binding pockets of EGFR and HER2, activating caspase-3 and caspase-8, and decreases the expression of Bcl-2, thereby inducing apoptosis. EGFR/HER2-IN-17 is promising for research of cancers.

NSC745887 (compound 25) is an inhibitor that targets DNA topoisomerase cleavage, activates the caspase-8/9-caspase-3-poly (ADP-ribose) polymerase cascade, and induces apoptosis in cancer cells. NSC745887 enhances γH2AX expression and causes DNA fragmentation leading to DNA damage.

IHMT-BMX-068 is a BMX PROTAC degrader with a DC₅₀ of 0.007 μM. IHMT-BMX-068 promotes ubiquitination and degradation of BMX. IHMT-BMX-068 increases the levels of cleaved PARP and cleaved Caspase-3, and induces Apoptosis. IHMT-BMX-068 exerts anti-cancer effects against prostate cancer. IHMT-BMX-068 can be used for the research of prostate cancer.

Mcl-1-IN-23 is a Mcl-1 inhibitor with a K_i value of 0.024 μM. Mcl-1-IN-23 binds directly to Mcl-1 and displaces the pro-apoptotic proteins Bak and Bim from Mcl-1 complexes. Mcl-1-IN-23 induces cell apoptosis, activates caspase-3, promotes PARP cleavage, and exerts antiproliferative activity against cancer cells. Mcl-1-IN-23 can be used for the research of leukemia.

Acetic acid lead is a carboxylic acid and short-chain fatty acid (SCFAs). Magnesium acetate tetrahydrate activates AMPK, increases ROS, cleaved caspase 9, PPARα, downregulates SREBP-1c, ChREBP expression. Acetic acid lead exhibits antifungal activity against Saccharomyces cerevisiae W303-1A. Acetic acid lead regulates energy metabolism. Acetic acid lead has anticancer activity against gastric cancer. Acetic acid lead induces writhing reaction and ulcerative colitis. Acetic acid lead can be used in the researches for gastric cancer, ulcerative colitis, hepatic steatosis, and pain.

2'-Deoxyadenosine monohydrate-1′-¹³C is the ¹³C labeled 2'-Deoxyadenosine monohydrate (HY-W011683). 2′-Deoxyadenosine monohydrate is an adenine nucleoside that inhibits glucose-stimulated insulin release. 2′-Deoxyadenosine monohydrate inhibits glucose-stimulated increases seen in islet cyclic AMP (cAMP) accumulation. 2'-Deoxyadenosine monohydrate activates caspase-3 and promotes apoptosis. 2'-Deoxyadenosine monohydrate inhibits the activity of S-adenosyl-L-homocysteine hydrolase (SAHH). 2'-Deoxyadenosine monohydrate inhibits the growth of various cells. 2'-Deoxyadenosine monohydrate has an anticancer effect on colon cancer.

Procaspase-3 activator 1 is a potent procaspase-3 activator. Procaspase-3 activator directly activates procaspase-3 through zinc chelation, thereby inducing apoptosis and inhibiting cancer cell proliferation. Procaspase-3 activator 1 can be used for the research of non-small cell lung cancer (NSCLC) and melanoma.

Ac-VEID-pNA is an artificially synthesized peptide. Ac-VEID-pNA is utilized as substrate for caspase 6, that cleaves the lamin A at the cleavage site of VEID.

YTHu78 is a KDM5B PROTAC degrader. YTHu78 induces KDM5B degradation via the ubiquitin-proteasome system and CRBN E3 ligase, and triggers lytic apoptosis in hematologic malignant cells. YTHu78 can be used in studies related to hematologic malignancies.

SC-60 is a derivative of Sorafenib (HY-10201). SC-60 exerts its anti-tumor effect by activating the phosphatase activity of SHP-1, thereby inhibiting the STAT3 signaling pathway. SC-60 exhibits strong proliferation inhibitory activity in various hepatocellular carcinoma (HCC) cell lines. SC-60 downregulates the expression of downstream anti-apoptotic proteins (such as Bcl-2, Cyclin D1, Survivin), ultimately inducing caspase-dependent apoptosis. SC-60 significantly inhibits tumor growth in xenograft tumor models. SC-60 can be used for the study of HCC.

HDAC1-IN-14 is an indole-based benzamide selective HDAC1 inhibitor with an IC₅₀ of 77 nM. HDAC1-IN-14 acts as an antiproliferative agent, with GI₅₀ values ranging from nanomolar to low micromolar levels in various cancer cells. HDAC1-IN-14 induces G0-G1 cell cycle arrest in colon cancer cells. HDAC1-IN-14 upregulates the expression of Caspase-3, Cyto-C and Bax, and downregulates the expression of AKT-1. HDAC1-IN-14 can be used in research related to leukemia, non-small cell lung cancer, colon cancer, central nervous system cancer, melanoma, ovarian cancer, renal cancer, prostate cancer and breast cancer.