Bcl-2 Family Activator

Bcl-2 Family Activators (27):

Cat. No.	Product Name	Effect	Purity

HY-100543

Zenidolol	Activator	99.60%
Zenidolol (ICI-118551) is a selective β2-adrenergic receptor antagonist with K_i values of Zenidolol for β2, β1 and β3 adrenergic receptors of 0.7, 49.5 and 611 nM, respectively. Zenidolol exerts antitumor effects via inducing apoptosis, inhibiting tumor sphere formation, and downregulating the HIF pathway by blocking β2-AR on tumor cells. Zenidolol exhibits a unique pulmonary vessel-specific vasodilatory effect in mouse models. Zenidolol can be used as an intraocular pressure-lowering agent in ophthalmic disease research.

HY-W105310A

Croconic acid disodium	Activator	99.98%
Croconic acid disodium (Nacr) is a lysine crotonylation (Kcr) activator and electroactive material. Croconic acid disodium reduces the expression of HDAC2, HDAC3, SIRT1, and SIRT3, and increases the expression of EP300, CITED1, ACSS2, DPF2, CDYL, MLLT3, and YEATS2. Croconic acid disodium elevates intracellular crotonyl-CoA content and global histone lysine crotonylation levels. Croconic acid disodium promotes the growth of bovine fibroblasts, regulates cell cycle progression, and inhibits bovine fibroblast apoptosis (apoptosis). Croconic acid disodium improves the blastocyst development efficiency of bovine somatic cell nuclear transfer embryos. Croconic acid disodium undergoes reversible lithium intercalation/deintercalation reactions via sodium-lithium ion exchange. Croconic acid disodium is applicable to research related to cell growth promotion.

HY-N1440

Koumine	Activator	99.97%
Koumine is an alkaloid separated from Gelsemium elegans, shows potent anti-tumor activity. Koumine up-regulates the Bax/Bcl-2 ratio and caspase-3 expression in human breast cancer cells. Koumine has anxiolytic, antistress, antipsoriatic, and analgesic activities, protects against the development of arthritis in Rheumatoid arthritis (RA) animal models.

HY-B0842

Thiophanate-Methyl	Activator	99.86%
Thiophanate-Methyl is a pesticide residue and fungicide. Thiophanate-Methyl induces hepatotoxicity via caspase-3-mediated apoptosis and oxidative stress, thereby causing metabolic imbalance in the liver of zebrafish. Thiophanate-Methyl impairs the rhizobacteria-mediated defense response of cucumber against fusarium wilt.

HY-N0863

Methyl protodioscin	Activator	99.67%
Methyl protodioscin (NSC-698790; Smilax saponin B) is a multi-target, selective, steroidal diglycoside inhibitor with antitumor activity that induces cell cycle arrest. The mechanism of action of Methyl protodioscin is complex, involving the induction of G2/M cell cycle arrest, regulation of the Bcl-2/Bax apoptotic pathway, inhibition of the Akt1/c-Myc axis and MAPK/ERK signaling, while simultaneously downregulating ADAM15 and inducing FOXO1 to reduce cholesterol synthesis. It also inhibits the JNK/c-Jun pathway, reducing the production of inflammatory factors (IL-6, TNF-α). Methyl protodioscin exhibits significant antitumor (inhibiting proliferation, migration, invasion, and inducing apoptosis), anti-inflammatory, and anti-restenosis activities. Methyl protodioscin can be used in research on lung cancer, prostate cancer, pancreatic cancer, and other tumors, as well as inflammatory diseases such as airway inflammation and enteritis.

HY-N0060BS

(E)-Ferulic acid-d₃	Activator	99.76%
(E)-Ferulic acid-d₃ is the deuterium labeled (E)-Ferulic acid. (E)-Ferulic acid is a isomer of Ferulic acid which is an aromatic compound, abundant in plant cell walls. (E)-Ferulic acid causes the phosphorylation of β-catenin, resulting in proteasomal degradation of β-catenin and increases the expression of pro-apoptotic factor Bax and decreases the expression of pro-survival factor survivin. (E)-Ferulic acid shows a potent ability to remove reactive oxygen species (ROS) and inhibits lipid peroxidation. (E)-Ferulic acid exerts both anti-proliferation and anti-migration effects in the human lung cancer cell line H1299.

HY-N6573

Bufarenogin	Activator	99.36%
Bufarenogin induces intrinsic apoptosis via Bax and ANT cooperation.

HY-121337

Flurochloridone	Activator	99.61%
Flurochloridone (R-40244) is a selective preemergence and persistent herbicide. Flurochloridone induces endoplasmic reticulum (ER) stress and activated unfolded protein response (UPR) signaling pathways. Flurochloridone impairs cell viability and induces cytotoxicity and apoptosis mediated by ER stress via activating eIF2α-ATF4/ATF6-CHOP-Bim/Bax signaling pathways in TM4 cells.

HY-158783

SACLAC	Activator	99.70%
SACLAC, a Ceramide analog, is a potent and covalent acid ceramidase (ASAH1; AC) inhibitor with a K_i of 97.1 nM. SACLAC effectively blocks AC activity and induces a decrease in sphingosine 1-phosphate (S1P) and total ceramide levels. SACLAC reduces the levels of splicing factor SF3B1 and alternative Mcl-1 mRNA splicing, increases pro-apoptotic Mcl-1S levels to induce apoptosis in acute myeloid leukemia (AML) cells. SACLAC reduces the leukemic burden in human AML xenograft mouse models.

HY-B1752

Quinpirole	Activator	98.95%
Quinpirole (LY 171555; (-)-LY 141865) is a D2/D3 dopamine receptor agonist and a CaV1.3 calcium channel modulator. Quinpirole normalizes dendritic spine density in dopamine-depleted striatum, upregulates the protein expression of BCL2 and GluR2, downregulates the protein expression of BAX, and delays the onset of seizures. Quinpirole enhances learning and memory, inhibits neuronal apoptosis (apoptosis), and induces anxiety-like, stereotyped, and compulsive behaviors. Quinpirole disrupts prepulse inhibition in rhesus monkeys, enhances the activity of paraventricular thalamic neurons to promote recovery from Isoflurane anesthesia, and alters the composition of the gut microbiota in rats. Quinpirole can be used in research related to dyskinesia, pain, epilepsy, and neurological disorders including anxiety disorder, obsessive-compulsive disorder, and schizophrenia.

HY-N13250

Hawthorn Extract	Activator
Hawthorn Extract is an orally active hawthorn extract. Hawthorn Extract decreases Bax expression and increases Bcl-2 expression in the aorta. Hawthorn Extract regulates the AMPK signaling pathway, induces apoptosis, enhances the hepatic antioxidant system, and ameliorates symptoms of liver injury, inflammation and cancer. Hawthorn Extract reduces plasma levels of pro-inflammatory factors, increases plasma levels of anti-inflammatory adiponectin, and alleviates atherosclerotic plaque lesions in the aorta. Hawthorn Extract improves symptoms associated with chronic heart failure. Hawthorn Extract inhibits FMLP-induced superoxide anion production, Elastase release, ILB₄ generation and calcium signaling in neutrophils, and also reduces LPS-induced cytokine production in neutrophils. Hawthorn Extract induces autophagy and inhibits the proliferation of intestinal stem cells. Hawthorn Extract can be used in research related to atherosclerosis, hepatitis, alcoholic liver disease, non-alcoholic fatty liver disease, hepatocellular carcinoma, chronic heart failure and hypotension.

HY-N5033

17-Hydroxy sprengerinin C	Activator	99.68%
17-Hydroxy sprengerinin C (compound 10) is a glycoside compound isolated from rhizomes of Polygonatum sibiricum. 17-Hydroxy sprengerinin C possesses stronger anticancer activities. 17-Hydroxy sprengerinin C reduces the expression of Blc-2 and pro-caspase3 and increases the production of Bax.

HY-117235R

Diallyl Trisulfide (Standard)	Activator
Diallyl Trisulfide (Standard) is the analytical standard of Diallyl Trisulfide. This product is intended for research and analytical applications. Diallyl Trisulfide is an orally active anticancer agent that can be isolated from garlic. Diallyl Trisulfide has the ability to induce apoptosis and exhibits anticancer, anti-inflammatory, antioxidant, and antibacterial activities. Diallyl Trisulfide can be used to study a variety of cancers, including liver, colon and prostate cancer[1][2][3][4].

HY-N1440R

Koumine (Standard)	Activator
Koumine (Standard) is the analytical standard of Koumine. This product is intended for research and analytical applications. Koumine is an alkaloid separated from Gelsemium elegans, shows potent anti-tumor activity. Koumine up-regulates the Bax/Bcl-2 ratio and caspase-3 expression in human breast cancer cells. Koumine has anxiolytic, antistress, antipsoriatic, and analgesic activities, protects against the development of arthritis in Rheumatoid arthritis (RA) animal models.

HY-182469

FuBIG	Activator
FuBIG is an iminoguanidine derivative with neuroprotective effects. FuBIGL inhibits L-LDH activation and reduces lactate production. FuBIGL exerts protective effects on inflammatory nerve cells, upregulates the expressions of AMPK, pAMPK and FOXO3, and activates the AMPK pathway in cells. FuBIG exerts anti-inflammatory effects by reducing pro-inflammatory cytokines (IL-6, IL-1β, TNF-α) and increasing the anti-inflammatory cytokine IL-10. FuBIG maintains mitochondrial membrane potential, alleviates mitochondrial dysfunction, reduces ROS production, and relieves oxidative stress. FuBIG upregulates Bcl-2, downregulates Bax and Caspase-3, and inhibits cell apoptosis (apoptosis). FuBIG improves metabolic disorders in diabetic mice, decreases the levels of LDL-C, ALT and AST, and increases HDL-C level simultaneously. FuBIG can be used in the research of diabetic neuroinflammation.

HY-N6801S

Nivalenol-¹³C₁₅	Activator
Nivalenol-¹³C₁₅ is the ¹³C labeled Nivalenol (HY-N6801). Nivalenol, a trichothecene mycotoxin that can be produced by Fusarium graminearum, is a fungal metabolite present in agricultural product. Nivalenol modulates apoptotic pathway, cell cycle regulation, Bax, ERK, caspase-3, and poly-ADP-ribose synthase activity in macrophages. Nivalenol inhibits ribosomal peptidyltransferase site, protein synthesis, DNA synthesis, and cell proliferation. Nivalenol induces late-stage apoptotic morphological changes, reduces cellular metabolism, and decreases cell proliferation in erythroleukemia cells. Nivalenol induces lymphocyte apoptosis in murine thymus, spleen, and Peyer's patches. Nivalenol can be used for the research of erythroleukemia.

HY-17495

Carteolol	Activator
Carteolol is a non-selective β-adrenoceptor antagonist. Carteolol induces apoptosis via a caspase activated and mitochondrial-dependent pathway. Carteolol can be used for glaucoma research.

HY-N0060BR

(E)-Ferulic acid (Standard)	Activator
(E)-Ferulic acid (Standard) is the analytical standard of (E)-Ferulic acid. This product is intended for research and analytical applications. (E)-Ferulic acid is an isomer of ferulic acid, an aromatic compound abundant in plant cell walls. (E)-Ferulic acid causes phosphorylation of β-catenin (β-catenin), leading to proteasome degradation, increasing the expression of pro-apoptotic factor Bax and reducing pro-apoptotic factor Expression of the survival factor survivin. (E)-Ferulic acid can effectively remove reactive oxygen species (ROS) and inhibit lipid peroxidation. (E)-Ferulic acid exerts antiproliferative and antimigratory effects in the human lung cancer cell line H1299.

HY-N6801R

Nivalenol (Standard)	Activator
Nivalenol (Standard) is the analytical standard of Nivalenol (HY-N6801). This product is intended for research and analytical applications. Nivalenol, a trichothecene mycotoxin that can be produced by Fusarium graminearum, is a fungal metabolite present in agricultural product. Nivalenol modulates apoptotic pathway, cell cycle regulation, Bax, ERK, caspase-3, and poly-ADP-ribose synthase activity in macrophages. Nivalenol inhibits ribosomal peptidyltransferase site, protein synthesis, DNA synthesis, and cell proliferation. Nivalenol induces late-stage apoptotic morphological changes, reduces cellular metabolism, and decreases cell proliferation in erythroleukemia cells. Nivalenol induces lymphocyte apoptosis in murine thymus, spleen, and Peyer's patches. Nivalenol can be used for the research of erythroleukemia.

HY-182349

Bax activator-2	Activator
Bax activator-2 (compound 27c) is a pro-apoptotic agent targeting BAX, with an IC₅₀ of 0.30 μmol/L against human BAX. Bax activator-2 binds to the trigger site of BAX and induces its conformational change. Bax activator-2 induces mitochondrial depolarization, cytochrome c release, caspase-3/9 cleavage and PARP cleavage, thereby initiating apoptosis. Bax activator-2 exhibits cytotoxicity against various cancer cell lines, shows reduced cytotoxicity in BAX-knockout A549 cells, and has low cytotoxicity against non-cancerous cell lines. Bax activator-2 can be used in studies related to acute myeloid leukemia and solid tumors.

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