Apoptosis Inhibitor

Phosphocreatine (disodium) is an organic compound found in vertebrate skeletal muscles. Phosphocreatine (disodium) enhances antioxidant activity, and activates the TAK1 pathway to protect the heart. Phosphocreatine (disodium) normalizing mitochondrial function and reducing oxidative stress via Akt mediated Nrf2/HO-1 pathway. Phosphocreatine (disodium) provides renal protection by suppressing Apoptosis and ROS (Reactive Oxygen Species) generation through ERK mediated mediated Nrf-2/HO-1 pathway..

BRD3308 is a highly selective HDAC3 inhibitor with an IC₅₀ of 54 nM. BRD3308 is 23-fold selectivity for HDAC3 over HDAC1 (IC₅₀ of 1.26 μM) or HDAC2 (IC₅₀ of 1.34 μM). BRD3308 suppresses pancreatic β-cell apoptosis induced by inflammatory cytokines or glucolipotoxic stress, and increases functional insulin release. BRD3308 activates HIV-1 transcription and disrupts HIV-1 latency.

WKYMVm is a selective formylpeptide receptor 2 (FPR2) agonist. WKYMVm has a powerful anti-inflammatory effect that can reduce lung injury and spinal cord injury. WKYMVm ameliorates obesity by regulating lipid metabolism and leptin signaling. WKYMVm is involved in the regulation of immune cells by activating FPRs. WKYMVm can promote the chemotactic migration of immune cells and inhibit the apoptosis of phagocytes. In addition, WKYMVm may play a favorable or unfavorable role in tumors, depending on the type of tumor.

Methazolamide (L584601) is a BBB-penetrable and orally active carbonic anhydrase inhibitor, with a K_i of 14 nM for human carbonic anhydrase II. Methazolamide can reduce intraocular pressure and has a neuroprotective effect, being able to inhibit neuronal apoptosis. Methazolamide can be used in the research of ophthalmic diseases such as glaucoma and cerebrovascular diseases such as subarachnoid hemorrhage.

Higenamine (Norcoclaurine), a β2-AR agonist with antioxidant capability, is a key component of the Chinese herb aconite root that prescribes for treating symptoms of heart failure in the oriental Asian countries. Higenamine is also a α1-adrenergic receptor antagonist with hypotensive effect. is a selective LSD1 inhibitor (IC₅₀=1.47 μM) that can be isolated from aconite. Higenamine hydrochloride has anti-inflammatory and antibacterial activity. Higenamine protects myocyte Apoptosis and ischemia/reperfusion (I/R) injury through selective activation of beta2-adrenergic receptor (β2-AR). Higenamine also reduces I/R-induced myocardial infarction in mice. Higenamine can attenuate IL-1β-induced Apoptosis through ROS-mediated PI3K/Akt signaling pathway. Higenamine protects brain cells from oxygen deprivation. Higenamine can promote bone formation in osteoporosis through the SMAD2/3 pathway. Higenamine can be used to study cancer, inflammation, cardiorenal syndrome and other diseases.

Elaidic acid is an orally active trans fatty acid. Elaidic acid enhances the stemness of colorectal cancer cells by activating the Wnt/ERK1/2 pathway, thereby promoting cell proliferation, invasion and metastasis, and inhibiting apoptosis. Elaidic acid also inhibits the growth of Lactobacillus and alters the cell surface hydrophobicity of Lactobacillus. Elaidic acid reduces basal 2-deoxyglucose uptake in muscle cells and adipocytes. Elaidic acid can be used in research on colorectal cancer, insulin and other related areas.

3-Hydroxyphenylacetic acid is an orally active flavonoid metabolite produced by intestinal flora, with blood pressure-lowering activity. 3-Hydroxyphenylacetic acid can also inhibit ferroptosis by upregulating the expression of GPX4, thereby improving spermatogenic dysfunction in aged mice. In addition, abnormal levels of 3-Hydroxyphenylacetic acid are closely related to certain diseases, such as autism spectrum disorders.

Camprenstat (GGTI-2418) is a highly potent, competitive, and selective geranylgeranyltransferase I (GGTase I) inhibitor. Camprenstat inhibits GGTase I and FTase activities with IC₅₀s of 9.5 nM and 53 μM, respectively. Camprenstat also increases p27(Kip1) and induces significant regression of breast tumors.

Azoramide is a potent, orally active small-molecule modulator of the unfolded protein response (UPR). Azoramide improves ER protein folding and elevates ER chaperone capacity, which together protects cells against ER stress. Azoramide alleviates PLA2G6 mutant-induced ER stress through modulating unfolded protein response, and enhances the CERB signaling to rescue mitochondrial function, thereby preventing apoptosis of DA neurons. Azoramide has antidiabetic activity.

Bilobalide, a sesquiterpene trilactone constituent of Ginkgo biloba, inhibits the NMDA-induced efflux of choline with an IC₅₀ value of 2.3 μM. Bilobalide prevents apoptosis through activation of the PI3K/Akt pathway in SH-SY5Y cells. Exerts protective and trophic effects on neurons.

DCP-LA (FR236924), a linoleic acid derivative, selectively and directly activates PKCε. DCP-LA activates Ca(²⁺)/calmodulin-dependent protein kinase II (CaMKII) and inhibits protein phosphatase-1 (PP-1) to stimulate AMPA receptor exocytosis. DCP-LA inhibits activation of caspase-3/-9 and protects neurons at least in part from oxidative stress-induced apoptosis.

Cetrorelix (SB-75) acetate is a competitive gonadotropin-releasing hormone receptor (GnRHR) antagonist with a K_d of 0.19 nM. Cetrorelix acetate inhibits the secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), thereby suppressing the secretion of downstream sex steroids. Cetrorelix acetate prevents ovulation, induces reversible reproductive shutdown and azoospermia, reduces ovarian fibrosis, improves superovulation outcomes, and inhibits chemotherapy-induced mitochondria-dependent apoptosis. Cetrorelix acetate is applicable for fertility assistance research.

Coenzyme Q9 (Ubiquinone Q9), the major form of ubiquinone in rodents, is an amphipathic molecular component of the electron transport chain that functions as an endogenous antioxidant. Coenzyme Q9 attenuates the diabetes-induced decreases in antioxidant defense mechanisms. Coenzyme Q9 improves left ventricular performance and reduces myocardial infarct size and cardiomyocyte apoptosis.

Ucf-101 is a selective and competitive inhibitor of pro-apoptotic protease Omi/HtrA2, with an IC₅₀ of 9.5 μM for His-Omi. Ucf-101 exhibits very little activity against various other serine proteases (IC₅₀>200 μM). Ucf-101 has a natural red fluorescence at 543 nm that is used to monitor its ability to enter mammalian cells. Ucf-101 has a significant cardioprotective effect against MI/R injury and also has certain neuroprotective effect.

Crocetin (Transcrocetin) is an aglycone of crocin. Crocetin is an orally active and brain-penetrant. Crocetin shows strong NMDA receptor affinity and channel opening activity. Crocetin can downregulate the proinflammatory cytokines and COX-2 exoression. Crocetin can inhibit apoptosis and activation of MAPK. Crocetin can delay delays brain and body aging. Crocetin can be used for the researches of cancer, neurological disease and inflammation, such as cervical cancer and ischemia.

Boc-D-FMK is a cell-permeable, irreversible and broad spectrum caspase inhibitor. Boc-D-FMK inhibits apoptosis stimulated by TNF-α with an IC₅₀ of 39 μM.

Zonisamide (AD 810) is an orally active carbonic anhydrase inhibitor, with K_is of 35.2 and 20.6 nM for hCA II and hCA V, respectively. Zonisamide exerts neuroprotective effects through anti-apoptosis and upregulating MnSOD levels. Zonisamide also increases the expression of Hrd1, thereby improving cardiac function in AAC rats. Zonisamide can be used in studies of seizure, parkinson’s disease and cardiac hypertrophy.

Thyrotropin (TSH, Pretiron) is a thyroid-stimulating hormone produced by thyrotrope cells in the anterior pituitary gland. Thyrotropin regulates the endocrine function of the thyroid. Thyrotropin induces transcriptional regulation of TH-gatekeeper genes in tanycytes through the Tshr/Gαq/PKC pathway. Thyrotropin prevents Apoptosis. Thyrotropin has an association of low levels with increased bone remodeling, reduced bone mass and a high fracture risk in mice. Thyrotropin is promising for research of skeletal remodeling, hyperthyroidism.

DC260126 is a potent antagonist of GPR40 (FFAR1). DC260126 dose-dependently inhibits GPR40-mediated Ca²⁺ elevations stimulated by linoleic acid, oleic acid, palmitoleic acid and lauric acid (IC₅₀: 6.28, 5.96, 7.07, 4.58 μM, respectively). DC260126 could protect MIN6 β cells from palmitate-induced ER stress and apoptosis.

MSN-125 is a potent Bax and Bak oligomerization inhibitor. MSN-125 prevents mitochondrial outer membrane permeabilization (MOMP) with an IC₅₀ of 4 μM. MSN-125 potently inhibits Bax/Bak-mediated apoptosis in HCT-116, BMK Cells, and primary cortical neurons, protects primary neurons against glutamate excitotoxicity.