bcl-2

ABT-737 is a BH3 mimetic and an inhibitor of Bcl-2, Bcl-xL, and Bcl-w (EC50=30.3 nM 78.7 nM 197.8 nM). ABT-737 exhibits antitumor activity and anti-aging activity.

Navitoclax (ABT-263) is a potent oral Bcl-2 inhibitor that binds to Bcl-xL, Bcl-2, and Bcl-w proteins (Ki<1 nM), demonstrating antitumor activity and inducing apoptosis.

Venetoclax (ABT-199) is a Bcl-2 inhibitor (Ki<0.01 nM) with potent, selective, and orally active properties. Venetoclax has a 3-order-of-magnitude lower affinity for Bcl-xL and Bcl-W (Kis=48 245 nM). Venetoclax induces autophagy and apoptosis.

Docetaxel trihydrate (RP-56976 Trihydrate) is an antineoplastic agent that has a unique mechanism of action as an inhibitor of cellular mitosis and that currently plays a central role in the therapy of many solid tumor including breast and lung cancer. Therapy with docetaxel has been associated with a low rate of serum enzyme elevations and rarely to instances of acute hepatic necrosis generally due to severe hypersensitivity reactions or sepsis.

(S)-(+)-Ibuprofen (Dexibuprofen) , is a non-steroidal anti-inflammatory drug (NSAID), inhibiting cyclooxygenase (COX).

Allethrin induces oxidative stress, apoptosis and calcium release. Allethrin, a pyrethroid insecticide is a major mosquito repellent agent.

Thymoquinone (NSC 2228) is a compound be found in herbs and spices with anti-inflammatory and anti-oxidant effects.

A-1155463, a highly potent and selective BCL-XL inhibitor, shows picomolar binding affinity to BCL-XL, and >1000-fold weaker binding to BCL-2 and related proteins BCL-W(Ki=19 nM) and MCL-1(Ki>440 nM).

S55746 (BLC201) is an effective and selective BCL-2 inhibitor (Ki: 1.3 nM and a Kd of 3.9 nM).

Thevetiaflavone (2-Genistein-5-methyl ether) is a natural flavonoid from Wikstroemia indica that inhibits the leakage of lactate dehydrogenase from the cytoplasm and increases cell viability.

(S)-Gossypol acetic acid ((S)-(+)-Gossypol acetic acid) is a conformational isomer of Gossypol that acts as a BH3 mimic capable of binding Bcl-xL and Bcl-2 proteins, with the potential to induce apoptosis and inhibit cell growth.

Alpinetin ((-)-alpinetin) has antibacterial activity.Alpinetin has anti-inflammatory activity.Alpinetin can enhance the sensitivity of HepG2 hepatoma cells to the chemotherapeutic agent CDDP. Alpinetin has strong anti-hepatoma and pancreatic cancer cells effects, by inhibiting proliferation , regulating of the Bcl-2 family and XIAP expression, releasing of cytochrome c and activating caspases.

Hinokiflavone, a novel modulator of pre-mRNA splicing activity both in vitro and in cellulo, inhibits the assembly of the spliceosome, particularly blocking the formation of the B complex. Additionally, it acts as a SUMO protease inhibitor by impeding the activity of sentrin-specific protease 1 (SENP1). Hinokiflavone also demonstrates significant cytotoxicity, including the inhibition of MMP-9.

Zibotentan (ZD4054) (ZD4054) is a specific Endothelin (ET)A antagonist with IC50 of 21 nM, exhibiting no activity at ETB. Phase 3.

Obatoclax Mesylate (GX15-070) is a Bcl-2 antagonist (Ki: 0.22 μM) and can induce apoptosis with up-regulation of Bim, induced cytochrome c release, and activation of caspase-3.

Sulforaphene is a natural product isolated from radish seeds, exhibits an ED50 against velvetleaf seedlings approximately 2 x 10 -4 M. Sulforaphene promotes cancer cells apoptosis and inhibits migration via inhibiting EGFR, p-ERK1 2, NF‐κB and other signa

δ-Tocotrienol (Delta-Tocotrienol) is a potential angiogenic inhibitor. δ-Tocotrienol is also a nontoxic activator of mir-34a which can inhibit nonsmall cell lung cancer cells (NSC-LC) cell proliferation, induce apoptosis and inhibit invasion, and thus offering a potential starting point for the design of novel anticancer agents.

Ginsenoside Rg6 can inhibit JK cell proliferation in human lymphocytoma and induce its apoptosis, the mechanism may through mitochondrial dysfunction and an increase of Bax expression and decrease of Bcl-2 expression.

17-Hydroxy sprengerinin C is a glycoside compound isolated from rhizomes of Polygonatum sibiricum with stronger anticancer activities. 17-Hydroxy sprengerinin C reduces the expression of Blc-2 and pro-caspase3 and increases the production of Bax.

Dihydrokaempferol (Aromadendrin) is a natural product. It induces apoptosis and inhibits Bcl-2 and Bcl-xL expression, possesses anti-inflammatory, antioxidant, and anti-diabetic properties, it exhibits anti-inflammatory activity

Ergosta-4,6,8(14),22-tetraen-3-one exhibits cytotoxic activity against human gastric cancer cells and can induce G2 M cell cycle arrest and apoptosis in human hepatocellular carcinoma (HepG2) cells. These findings could facilitate the further use of various medicinal fungi in cancer treatment.

Liriodenine is a potent inhibitor of topoisomerase II (EC 5.99.1.3) both in vivo and in vitro, it has antitumor, antibacterial and antifungal activities, it can suppress ventricular arrhythmias induced by myocardial ischaemia reperfusion, through inhibiti

Lupiwighteone has anti-angiogenesis potential, it also has anticancer and cancer preventive effects on SH-SY5Y cells.

N-Methylnicotinamide is one of the endogenous metabolites that ameliorates endothelial dysfunction.