Apoptosis

Declopramide (OXI-104) is a chemosensitizer with antitumor activity that can be used to study colorectal cancer and inflammatory bowel disease.

Siegeskaurolic acid reduces inflammation and pain by blocking iNOS and COX-2 in macrophages via NF-kappaB inactivation.

Applications 4-Benzyloxy-3-methoxybenzoic Acid is used in the synthesis of Hsp90 inhibitors as EGCG analogues. Also used in the preparation of vanillates exhibiting cytostatic properties towards cancel cells resistant to pro-apoptotic stimuli. References Khandelwal, A. et al.: J. Org. Chem., 78, 7859 (2013); Lamoral-Theys, D. et al.: Bioorg. Med. Chem., 18, 3823 (2010);

CPTH2 is a histone acetyltransferase inhibitor modulating Gcn5 network.

Stability Hygroscopic Applications α-Fructose L-Arginine is an analogue of Fructose-leucine, an amadori compound having the potential to alter cellular adhesion, inhibit cancer metastasis and induce apoptosis. References Slatter, D. et al.: Int. J. Biochem. Cell Biol., 40, 2253 (2008); Horiuchi, T., et al.: Agric. Biol. Chem., 55, 333 (1991), Glinsky, G., et al.: Cancer Res., 56, 5319 (1996); Srinivas, S. et al.: J. Agri Food Chem., 60, 1522 (2012);

MARK4 inhibitor 1 inhibits cancer cell proliferation, metastasis and induces apoptosis.

NUN82647 (CU-242) is an Inhibitor of cell cycle at G2 phase, and apoptosis inducer.

H3R antagonist 4 (compound 11l) serves as a dual inhibitor of cholinesterases and histamine H3 receptors (H3R), demonstrating IC50 values of 7.04 μM (eeAChE), 9.73 μM (hAChE)(reversible), and 1.09 nM (H3R). It effectively inhibits both self and Cu2+-induced Aβ1-42 aggregation at 95.48% and 88.63%, respectively, and degrades Aβ1-42 protofibrils with 80.16% and 89.30% efficiency under similar conditions. Additionally, H3R antagonist 4 possesses the chelating capability for biometals Cu2+, Zn2+, Al3+, and Fe2+. It significantly reduces tau protein hyperphosphorylation induced by Aβ1-42, inhibits RSL-3 induced apoptosis and ferroptosis in PC12 cells, and shows optimal blood-brain barrier permeability and intestinal absorption characteristics in hCMEC/D3 and hPepT1-MDCK cells, respectively. Moreover, the compound improves learning and memory impairments in an Alzheimer's mouse model induced with scopolamine.

Tyrphostin AG1296 (Tyrphostin AG 1296) is an inhibitor of PDGFR with IC50 of 0.3-0.5 μM, no activity to EGFR.

Inavolisib (GDC-0077) is an orally available selective PI3Kα inhibitor with an IC50 value of 0.038 nM.Cost-effective and quality-assured.

Applications A potent and specific inhibitor of the Jak-2 tyrosine kinase. In acute lymphoblastic leukemia (ALL) cells which abundantly express JAK-2, AG-490 dose-dependently inhibited DNA synthesis, blocked cell growth and induced apoptosis. AG-490 does not significantly inhibit other kinases such as Lck, Lyn, Btk, Syk and Src. AG-490 is cell permeable and is active in vivo. Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package References Stock, J., et al.: J. Biol. Chem., 267, 19753 (1992), Levitzki, A., et al.: Science, 267, 1782 (1995), Meydan., N., et al.: Nature, 379, 645 (1996), Lu, H., et al.: Drug Metab. Dispos., 31, 572 (2003),

Actein stimulates bone formation, counters osteoporosis and oxidative damage, and may treat lipid disorders and cancer, inhibiting breast cancer cell growth.

Applications (3α,5β,7α,12α)-3,7,12-Trihydroxy-cholest-24-en-26-oic Acid Ethyl Ester is an intermediate in the synthesis of (25R)-3β,7α,12α-Trihydroxy-5-cholestenoic Acid (T795130), which is an oxysterol, an oxidized derivatives of cholesterol (C432501), which may be important in many biological processes, including cholesterol homeostasis, atherosclerosis, sphingolipid metabolism, platelet aggregation, apoptosis, and protein prenylation,[1] though their roles are poorly understood. References Schroepfer, G., et al.: Physiol. Rev., 80, 361 (2000); Bjorkhem, I.: J. Clin. Invest., 6, 725(2002); Bjorkhem, I., et al.: Arterio. hromb. Vascul. Biol., 22, 734 (2002)

Boc-Asp(OMe)-FMK is a broad-spectrum caspase inhibitor that blocks Fas-mediated processes without affecting IL-8 chemotaxis.

Isoverticine exhibits significant antitussive, expectorant and anti-inflammatory activities, it also displays significant cytotoxicity.

ARS-853 is an inhibitor of K-RASG12C(IC50 : 2.5 μM), a mutant form of K-RAS that accumulates in the active GTP-bound state in certain cancer cells

(E/Z)-TG003 is a potent and ATP-competitive Cdc2-like kinase (Clk) inhibitor.

α-Lipoic Acid, a sulfur-containing octanoic acid derivative, is biosynthesized from linoleic acid and used in dietary supplements.

Anti-TNBC agent-2 (3j), a purine derivative, acts as an anti-triple negative breast cancer (TNBC) therapeutic.

Applications 1-Pyrrolidinecarbodithioic Acid induces apoptosis in rat smooth muscle cells and inhibits apoptosis in leukemia HL-60 cells. It also prevents induction of nitric oxide synthetase by inhibiting translation of NOS mRNA; References Cui, J., et al.: J. Biol. Chem., 285, 38951 (2010); Reid, P., et al.: Mol. Cancer, 8, 49 (2009)

GL392 is a senolytic agent that delivers the potent senescence-clearing compound Dasatinib specifically to senescent cells. By targeting the LBD domain, it binds lipofuscin in these cells and releases Dasatinib via an ester linkage, inducing apoptosis (Apoptosis) in senescent cells. Additionally, GL392 is encapsulated in PEO-b-PCL microcapsules to ensure efficient intracellular delivery while minimizing systemic toxicity. GL392 is applicable in cancer research.

Simvastatin (MK 733) is an HMG-CoA reductase inhibitor (Ki=0.2 nM) with oral activity.

TAT-NEP1-40 acetate, a potential therapeutic for axonal regeneration and functional recovery post-stroke, safeguards PC12 cells from oxygen and glucose

Amiloride hydrochloride (Amiloride HCl) 是上皮钠通道和尿激酶型纤溶酶原激活物受体的抑制剂,也是 polycystin-2通道阻断剂。

CV-4-26 (Compound 22) acts as a covalent inhibitor of TEAD. By inhibiting YAP/TEAD-driven transcription, it diminishes the expression of CTGF and CYR61. Furthermore, CV-4-26 impedes colony formation in Huh7 and HepG2 cells, inducing cell cycle arrest and apoptosis (apoptosis). This compound demonstrates anti-tumoral activity against hepatocellular carcinoma (HCC) and hepatoblastoma (HB).

Sclareol from clary sage inhibits growth and is cytotoxic to many human Y cell lines.

Barakol, a primary compound found in Cassia siamea, inhibits MMP-3 activity and enhances the anti-metastatic effects of doxorubicin. Additionally, Barakol induces apoptosis (Apoptosis), generates reactive oxygen species, increases the Bax/Bcl-2 expression ratio, and activates caspase-9. This compound also exhibits laxative, anti-anxiety, central nervous system depressant, antioxidant, and anticancer properties.

Busulfan-d8 (Sulphabutin-d8) is the 2H-labeled Busulfan. Busulfan is an anticancer agent with immunosuppressive and myeloablative chemotherapy activities.

Applications 20(R)-Ginsenoside Rg3 causes an inhibition of phosphatidylinositol 3-kinase/Akt activation that, in turn, results in modulations in Bcl-2 family proteins in such a way that the apoptosis of U87 cells are regulated. Elicits a significant inhibition of in vitro cell adhesion and invasion of U87 cells. in vitro stereoselective inhibition of ginsenosides toward UDP-glucuronosyltransferase isoforms and in vivo inhibition of tumor angiogenesis of lung cancer. References Liu, Y., et al.: Chengdu Yixueyuan Xuebao, 9, 4 (2014); Liu, Y., et al.: Linchuang Junyi Zazhi, 42, 1138 (2014), Kim, D., et al.: Toxicol. Lett., 259, 1 92016); Geng, L., et al.: Zhonghua Zhongyiyao Zazhi, 29, 601 (2014)

Rosmarinic acid (Labiatenic acid) is widely found in plants and has antioxidant, anti-inflammatory, and antibacterial activities.

BAY 11-7082 (BAY 11-7821) is an NF-κB inhibitor that inhibits TNFα-induced IκBα phosphorylation (IC50=10 μM).

Demethylzeylasteral (T-96), isolated from Tripterygium wilfordii, has anti-inflammatory, immunosuppressive and anti-tumor activities.

CCG-1423, a selective RhoA pathway inhibitor, suppresses SRF-mediated transcription.

Evo312 is an inhibitor of protein kinase C beta I (PKCβI) with an IC50 of 117.34 nM and exhibits dose-dependent characteristics. It acts by inhibiting the expression of the PKCβI protein, which leads to cell cycle arrest and apoptosis in PANC-GR (gemcitabine-resistant pancreatic cancer cells). Evo312 also demonstrates antiproliferative effects in pancreatic cancer cells PANC-1 and PANC-GR, with IC50 values of 0.08 μM and 0.07 μM respectively, while presenting an IC50 of 2.95 μM in normal human pancreatic ductal epithelial cells HPDE6-c7. Additionally, Evo312 has shown antitumor activity in a mouse xenograft model using PANC-GR cells.

The test principle applied in this kit is Sandwich enzyme immunoassay. The microtiter plate provided in this kit has been pre-coated with an antibody specific to Mouse PDCD1. Standards or samples are added to the appropriate microtiter plate wells then with a biotin-conjugated antibody specific to Mouse PDCD1. Next, Avidin conjugated to Horseradish Peroxidase (HRP) is added to each microplate well and incubated. After TMB substrate solution is added, only those wells that contain Mouse PDCD1, biotin-conjugated antibody and enzyme-conjugated Avidin will exhibit a change in color. The enzyme-substrate reaction is terminated by the addition of sulphuric acid solution and the color change is measured spectrophotometrically at a wavelength of 450nm ± 10nm. The concentration of Mouse PDCD1 in the samples is then determined by comparing the OD of the samples to the standard curve.

Cidofovir ((S)-HPMPC) 通过特异性抑制病毒 DNA 合成来抑制病毒复制。

The test principle applied in this kit is Sandwich enzyme immunoassay. The microtiter plate provided in this kit has been pre-coated with an antibody specific to Rat ASK1. Standards or samples are added to the appropriate microtiter plate wells then with a biotin-conjugated antibody specific to Rat ASK1. Next, Avidin conjugated to Horseradish Peroxidase (HRP) is added to each microplate well and incubated. After TMB substrate solution is added, only those wells that contain Rat ASK1, biotin-conjugated antibody and enzyme-conjugated Avidin will exhibit a change in color. The enzyme-substrate reaction is terminated by the addition of sulphuric acid solution and the color change is measured spectrophotometrically at a wavelength of 450nm ± 10nm. The concentration of Rat ASK1 in the samples is then determined by comparing the OD of the samples to the standard curve.

Applications KU-0058948 is a poly (ADP-ribose) polymerase (PARP) inhibitor. Studies show that KU-0058948 is a potent agonist that activates transfected extracellular signal-regulated kinase 8 (ERK8) in cells. KU-0058948 induces cell cycle arrest and apoptosis of primary myeloid leukemic cells and myeloid leukemic cell lines in vitro References Klevernic, I.V. et al.: FEBS Lett., 583, 680 (2009); Gaymes, T.J. et al.: Haematologica, 94, 638 (2009);

MIRA-1 (WRN Helicase Inhibitor) is a restorer of wild-type p53 conformation/cellular function and selectively inhibits Werner syndrome WRN helicase activity

Spliceostatin A is an anticancer agent and splicing inhibitor that induces apoptosis by inducing cell cycle arrest in the G1 and G2/M phases.

ISOGINKGETIN (4',4'''-Dimethylamentoflavone), a compound derived from the leaves of Ginkgo biloba, to up-regulate adiponectin secretion.

TAI-1 is a potent and specific Hec1 inhibitor, which disrupts Hec1-Nek2 protein interaction.

Ralimetinib dimesylate (LY2228820 dimesylate) is a orally available, p38 MAPK inhibitor with potential anti-inflammatory and antineoplastic activities.

PRLX-93936 HCL is an analog of erastin and demonstrated synergistic effects against non-small cell lung cancer (NSCLC) cells with cisplatin.

Cytarabine (Ara-C) is a nucleoside analog, an inhibitor of DNA synthesis (IC50=16 nM).

Quercetin Dihydrate (Sophoretin) is a flavonoid natural product that activates or inhibits the activity of many proteins. It activates SIRT1 and inhibits PI3K.

Pheniramine maleate (Trimetose), an alkylamine derivative with antihistaminic and vasodilatory properties, binds to histamine H1 receptors.

MMRi64 inhibits Mdm2-MdmX, boosts p53, triggers apoptosis, and is used in cancer research.

MN58b is a selective inhibitor of choline kinase α (CHKα).

Applications N-Acetylcysteine Amide is used for the treatment of acquired immune deficiency syndrome and HIV infection, an antidote for an acetaminophen toxicity. Also used as authentic imaging probe for accurate tracing of cells viability from beginning to end to distinguish apoptotic and necrotic cells, A thiol-based antioxidant and a precursor of glutathione (GSH), alleviates MTX-induced platelets apoptosis and oxidative damage. References (1) Paul, M., et al.: PLoS One, 10, e0127558/1 (2015) (2) Ferreira, L. F., et al.: Med. Sci. Sports Exerc 43, 1025 (2011) (3) Khayyat, A., et al.: Toxicol. Lett. 241, 133 (2016)

The test principle applied in this kit is Sandwich enzyme immunoassay. The microtiter plate provided in this kit has been pre-coated with an antibody specific to Mouse PYCARD. Standards or samples are added to the appropriate microtiter plate wells then with a biotin-conjugated antibody specific to Mouse PYCARD. Next, Avidin conjugated to Horseradish Peroxidase (HRP) is added to each microplate well and incubated. After TMB substrate solution is added, only those wells that contain Mouse PYCARD, biotin-conjugated antibody and enzyme-conjugated Avidin will exhibit a change in color. The enzyme-substrate reaction is terminated by the addition of sulphuric acid solution and the color change is measured spectrophotometrically at a wavelength of 450nm ± 10nm. The concentration of Mouse PYCARD in the samples is then determined by comparing the OD of the samples to the standard curve.

LDN-57444 is a reversible, competitive proteasome Uch-L1 inhibitor(IC50=0.88 μM) .

Ketorolac (Acuvail) is an NSAID that blocks prostaglandin synthesis, related to heterocyclic acetic acids.

Pravastatin sodium (CS-514 (sodium)), an HMG-CoA reductase inhibitor, inhibits sterol synthesis with IC50 of 5.6 μM.

Minocycline HCl: tetracycline antibiotic, treats bacterial infections and acne, may cause acute or chronic hepatitis.

Angophorol, a flavonoid from Pterocarpus indicus, exhibits anticancer properties by inhibiting growth and inducing apoptosis in K562 cells.

Adenosine (D-Adenosine) is a ribonucleoside. Adenosine has vasodilatory, antiarrhythmic and analgesic effects. Cost-effective and quality-assured.

L-Mimosine (Leucenol) is an antineoplastic alanine-substituted pyridine derivative isolated from Leucena glauca and acts as an iron chelator.

ROCK/HDAC-IN-2 (Compound C-9) is a dual inhibitor of ROCK/HDAC, characterized by IC50 values of 0.185 µM for HDAC6, 0.8 µM for ROCK1, and 0.7 µM for ROCK2. It effectively induces apoptosis and mitochondrial membrane potential alterations in cancer cells and demonstrates notable antitumor activity, making it useful for research in pancreatic ductal adenocarcinoma (PDAC) and triple-negative breast cancer (TNBC).

Sorafenib tosylate (Bay 43-9006) is a potent multikinase inhibitor (IC50s: 6/20/22 nM for Raf-1/VEGFR-3/B-Raf).

Etomoxir sodium salt ((R)-Etomoxir sodium salt) is a carnitine palmitoyltransferase 1a (CPT-1a) inhibitor that blocks fatty acid synthesis.

The test principle applied in this kit is Sandwich enzyme immunoassay. The microtiter plate provided in this kit has been pre-coated with an antibody specific to Mouse IRF5. Standards or samples are added to the appropriate microtiter plate wells then with a biotin-conjugated antibody specific to Mouse IRF5. Next, Avidin conjugated to Horseradish Peroxidase (HRP) is added to each microplate well and incubated. After TMB substrate solution is added, only those wells that contain Mouse IRF5, biotin-conjugated antibody and enzyme-conjugated Avidin will exhibit a change in color. The enzyme-substrate reaction is terminated by the addition of sulphuric acid solution and the color change is measured spectrophotometrically at a wavelength of 450nm ± 10nm. The concentration of Mouse IRF5 in the samples is then determined by comparing the OD of the samples to the standard curve.

Cirsiliol is a 5-LOX inhibitor that inhibits cell proliferation and promotes apoptosis in OS cells.

GSK2606414 is a cell-permeable and orally active protein kinase R-like endoplasmic reticulum kinase(PERK)inhibitor.Cost-effective and quality-assured.

Ibandronate sodium monohydrate (BM-210955) is a highly potent nitrogen-containing bisphosphonate used for the treatment of osteoporosis.

PS-47(PS 47) is an inactive E-isomer of PS48. PS48 is an activator of PDK1.

2-aminobenzo[d]thiazol-6-ol: antimicrobial, antioxidant, anticancer; may trigger cancer cell apoptosis.

Hydroxy-PP-Me is a CBR1 inhibitor that inhibits apoptosis induced by serum withdrawal.Hydroxy-PP-Me is used in the study of leukemia.

[Au(L4)(CyJohnPhos)]SbF6 is a gold-containing compound that exhibits inhibitory effects on cyclooxygenase-1/2 (COX-1/2), suppresses the proliferation of colon cancer cells Caco2-/TC7 with an IC50 of 0.98 μM, and induces cell apoptosis (apoptosis). Additionally, [Au(L4)(CyJohnPhos)]SbF6 acts as an inhibitor of thioredoxin reductase (TrxR) and demonstrates antioxidative activity by modulating ROS levels.

DCC-2036 (Rebastinib (DCC-2036)) is a conformational control Bcr-Abl inhibitor for Abl1(WT, IC50: 0.8 nM) and Abl1(T315I, IC50: 4 nM), also inhibits LYN, SRC,

PARP-2-IN-3 is used in the study of breast cancer as a PARP-2 inhibitor with antitumor activity that induces apoptosis (apoptosis) and necrosis in cancer cells.

Puromycin aminonucleoside (NSC-3056) increases podocyte permeability by modulating ZO-1 in an oxidative stress-dependent manner.

Selumetinib sulfate (AZD6244 sulfate) is a MEK1/2 inhibitor that inhibits MEK1/2 phosphorylation.

Sodium etidronate (Didronel), a bisphosphonate, resists degradation, inhibits osteoclasts, and may boost bone formation.

Mocetinostat (MG0103) is an orally available HDAC inhibitor with most potency for HDAC1 (IC50: 0.15 μM), 2- to 10- fold selectivity against HDAC2/3/11.