BCL

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

S63845 is a selective MCL-1 inhibitor(Kd: 0.19 nM)

UMI-77, a specific Mcl-1 inhibitor (Ki: 490 nM), has selectivity over other members of Bcl-2 family.

Kurarinone, a flavanoid derived from shrub Sophora flavescens,Kurarinone exhibits anti-tumor, estrogenic, and anti-inflammatory activities, it also shows strong inhibitory effect on immune responses. Kurarinone may ameliorate chronic inflammatory skin diseases through the suppression of pathogenic CD4(+) T-cell differentiation and the overall immune response.

Gossypol (BL 193) Acetate is a polyphenolic aldehyde that permeates cells and acts as an inhibitor for several dehydrogenase enzymes.

Triacetylresveratrol (Acetyl-trans-resveratrol) has anti-cancer activity,it inhibits the phosphorylation of STAT3 and NFκB, down-regulates Mcl-1, and up-regulates Bim and Puma in pancreatic cancer cells.

TV 3279 is a novel ChE-MAI inhibitor , and the neuroprotective properties depend on their ability to induce the anti-apoptotic proteins PKC, Bcl-2, Bcl-x, and SOD, and to block the nuclear translocation of the pro-apoptotic enzyme glyceraldehyde phosphate dehydrogenase in PC-12 and neuroblastoma cells.

1-[2,4-Dihydroxy-6-methoxy-3-(3-methyl-2-buten-1-yl)phenyl]-3-(4-hydroxyphenyl)-2-propen-1-one (Xanthohumol) , prenylchacone flavonoid, is a natural product with multi-biofunctions purified from Hops Humulus lupulus,is effective against HIV-1 and might serve as an interesting lead compound. It may represent a novel chemotherapeutic agent for HIV-1 infection.

BCL6-IN-3 is a potent BCL6 inhibitor with GI50 of 70 nM in SU-DHL4 cells. BCL6-in-3 regulates cell activation, differentiation, DNA damage and apoptosis, and has antitumor activity.

A09-003 is a novel cell cycle protein-dependent kinase-9 CDK-9 inhibitor.A09-003 inhibits the proliferation of a variety of leukemia cell lines and inhibits the increase of leukemia sequence-1 protein in myeloid cells.A09-003 also induces apoptosis, decreases RNA polymerase II activity, and decreases Mcl-1 expression.

PUMA BH3 acetate (PUMA BH3 Free base) is a p53 positive regulator of apoptosis (PUMA) BH3 domain polypeptide that acts as a direct activator of Bak with a Kd of 26 nM.

Epieriocalyxin A can suppress Caco-2 colon cancer cell growth. It could be a potential drug for colon cancer therapy in the future.

MIK665 (S-64315) (S-64315) has an inhibitory effect on myeloid leukemia.

Sonrotoclax (BGB 11417) is a selective inhibitor targeting the WT and G101V mutants of Bcl-2 with potential antitumor activity for the study of lymphoma and leukemia.

A-1210477 is an effective and specific MCL-1 and Bcl-2 inhibitor (Ki IC50: 0.454 26.2 nM).

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).

FX1 is an effective and selective BCL6 inhibitor (IC50: 35 μM).

ABT-737 is a BH3 mimetic inhibitor of Bcl-xL, Bcl-2 and Bcl-w (EC50s: 78.7 30.3 197.8 nM).

Chelerythrine Chloride is a cell-permeable inhibitor of protein kinase C, competitive with respect to the phosphate acceptor and non-competitive with respect to ATP.

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.

Gambogic Acid (Guttic Acid) ( EC50=0.78-1.64 uM) activates caspases. Gambogic Acid competitively suppresses Bcl-XL, Bcl-2, Bcl-W, Bcl-B, Bfl-1 and Mcl-1. The IC50s of Gambogic Acid for Bcl-XL, Bcl-2, Bcl-W, Bcl-B, Bfl-1 and Mcl-1 are 1.47, 1.21, 2.02, 0.66, 1.06 and 0.79 uM, respectively.

Bax inhibitor peptide V5 (BIP-V5) is a Bax-mediated apoptosis inhibitor with anticancer activity.

Gossypol acetic acid (AT101), a polyphenolic compound isolated from cottonseeds, binds with Bcl-2, Bcl-xL, Mcl-1, and does not inhibit BIR3 domain and BID.

1. Chelerythrine (Broussonpapyrine) may have antimanic effect . 2. Chelerythrine can inhibit telomerase activity. 3. Chelerythrine is a well-known protein kinase C inhibitor . 4. Chelerythrine has potential antiproliferative and antitumor effects.

Ergosta-4,6,8(14),22-tetraen-3-one has cytotoxic activity against human gastric cancer cell, it can induce G2/M cell cycle arrest and apoptosis in human hepatocellular carcinoma HepG2 cells, these results would be useful for the further utilization of man

Cimidahurinine can attenuate Doxorubicin (DOX)-induced cardiotoxicity in a dose-dependent manner with EC50 values of 45.79 uM; it protects against cardiotoxicity by decreasing reactive oxygen species (ROS) accumulation and downregulating apoptosis-related Bax/Bcl-2 proteins.

Ginsenoside F4 has inhibitory effect on human lymphocytoma JK cell by inducing its apoptosis, the mechanism is related to the mitochondrial dysfunction and the increase of Bax expression and decrease of Bcl-2 expression.

Bakkenolide IIIa has antioxidant, and neuroprotective effects, it protects against cerebral damage by inhibiting AKT and ERK1/2 activation and inactivated NF-κB signaling.

IMB-XH1 (Mcl1-IN-2) is a myeloid cell factor 1 (Mcl-1) inhibitor.

Reynosin has hepatoprotective, and anti-inflammatory effects, it has protective effect against dopamine-induced neuronal cell death, which may be due to the reciprocal up-regulation of E6-associated protein and down-regulation of α±-synuclein protein expr

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

WEHI-9625 is a tricyclic sulfone small molecule apoptosis inhibitor (EC50: 69 nM).

Pteropodine acts as a positive modulator of muscarinic M(1) and 5-HT(2) receptors. Pteropodine shows antigenotoxic, antioxidant and lymphocyte induction effects, it also shows strong apoptotic effect on acute leukaemic lymphoblasts.

TL4-12 is a specific MAP4K2/GCK inhibitor that inhibits IKZF1 and BCL-6.TL4-12 inhibits MM cell proliferation and induces apoptosis, and can be used in the study of multiple myeloma (MM).

Co-treatment with Tanshinone IIB (TSB) significantly inhibits the DNA laddering, cytotoxicity and apoptosis of rat cortical neurons induced by staurosporine in a concentration-dependent manner; TSB also suppresses the elevated Bax protein and decreased bc

VHD-valtrate has anticancer effects against human ovarian cancer cells in vitro and in vivo, it is a potential therapeutic agent for ovarian cancer, providing a basis for development of the compound as a novel chemotherapeutic agent.

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.

Wilfortrine can induce liver cancer cell HepG2 apoptosis, but with no effect on the cell cycle, mainly by promoting Bax expression and inhibiting anti-apoptotic protein Bcl-2 expression.

Panaxynol is the most potent antiplatelet agent in ginseng and its mechanism of action is chiefly due to the inhibition of thromboxane formation.

BM 957 is an effective Bcl-2 and Bcl-xL inhibitor (Kis: 1.2 and <1 nM; IC50s: 5.4 and 6.0 nM).

Myricanol can elicit growth inhibitory and cytotoxic effects on lung cancer cells, it can significantly decelerate tumor growth in vivo by inducing apoptosis.

2-Methoxystypandrone displays an immunomodulatory effect in a cellular model, it blocks inflammatory responses by impairing NF-κB signaling to limit the inflammation and oxidative stress for preservation of BBB integrity. 2-Methoxystypandrone concomitant

Cearoin has anti-inflammatory, and antiallergic activities, it can markedly inhibit inflammatory responses including LPS-induced NO production by suppressing the expression of iNOS mRNA and LPS-induced mRNA expression of TNFα and CCL2. Cearoin induces aut

Crenulatin has dual- direction effects on apoptosis of cerebral microvascular endothelial cells, inhibitive effect in 25 mg/L and stimulative effect in 100 mg/L group, respectively; the mechanism is related to the alterations of Fas/Bcl-2 expression and caspase-3 activity.

Scutebarbatine A shows significant antitumor effects on A549 cells in vivo and in vitro via mitochondria-mediated apoptosis by up-regulating expressions of caspase-3 and 9, and down-regulating Bcl-2. Scutebarbatine A and barbatine A show a significant ability to protect cells against H2O2 with ED50 values of 5.0 and 16.8 μM, respectively.

PROTAC Mcl1 degrader-1 induces the ubiquitination and proteasomal degradation of Mcl-1 by introducing the E3 ligase cereblon (CRBN)-binding ligand pomalidomide to Mcl-1 inhibitor S1-6 with μM-range affinity. PROTAC Mcl1 degrader-1, a proteolysis targeting chimera (PROTAC), is a potently and selectively Mcl-1 inhibitor with an IC50 of 0.78 μM.

Desmorpholinyl Navitoclax-NH-Me (Desmorpholinyl ABT-263-NH-Me) is a Bcl-xL inhibitor, which can be employed alongside a CRBN ligand to synthesize XZ739, a PROTAC BCL-XL degrader [1] [2].

Physalin A exerts anti-tumor activity in non-small cell lung cancer cell lines by suppressing JAK/STAT3 signaling, it inhibits androgen-independent prostate cancer cell growth through activation of cell apoptosis and downregulation of androgen receptor ex

Dehydrocavidine (Dehydrocorydaline) has antitumor activity, it inhibits MCF-7 cell proliferation by inducing apoptosis mediated by regulating Bax Bcl-2, activating caspases as well as cleaving PARP.