Bcl-XL

Bcl-xL antagonist 2 is an effective and selective antagonist of Bcl-xL with an IC50 of 91 nM and a Ki of 65 nM. Bcl-xL antagonist 2 induces apoptosis in cancer cells and can be used in studies about chronic lymphocytic leukemia and non-Hodgkin's lymphoma.

BCL-xLligand 2 is a ligand for BCL-xL. It can be conjugated with an E3 ligase ligand and a linker to form the Bcl-xL-targeting PROTAC degrader PZ671.

PROTACBcl-xL degrader-4 (Compound 2-38-III) is a Bcl-xL PROTAC degrader with significant antitumor activity against HepG2 and HUVEC cells. It induces apoptosis by reducing mitochondrial membrane potential and activating the MAPK signaling pathway. PROTACBcl-xL degrader-4 markedly inhibits tumor growth in xenograft mouse models.

PROTAC Bcl-xL degrader-1 is a potent PROTAC composed of a Bcl-xL (Bcl-2 family member) ligand-binding group, a linker, and an IAP E3 ligases binding group, demonstrating effectiveness as a Bcl-xL degrader. It exhibits toxicity towards human platelets and MyLa 1929 cells, with IC50 values of 62 nM and 8.5 μM, respectively [1].

PROTAC Bcl-xL degrader-3 is a potent ROTAC Bcl-xL degrader.

PROTAC Bcl-xL ligand-1 serves as a ligand targeting Bcl-xL, essential in synthesizing PROTACs [1].

PROTAC Bcl-xL degrader-2, based on von Hippel-Lindau ligand, is a potent degrader of Bcl-xL (a Bcl-2 family member), demonstrating an IC 50 of 0.6 nM.

TAT-BH4 (Bcl-xL), primarily localized at the mitochondria, inhibits apoptotic cell death. This compound comprises an N-terminal eosin-labeled cysteine and the protein transduction domain of the HIV TAT protein (amino acids 49 to 57), fused to the Bcl-xL BH4 peptide. It serves as a tool for research into diseases characterized by accelerated apoptosis [1].

"TAT-BH4 (Bcl-xL) TFA, primarily localized at the mitochondria, inhibits apoptotic cell death. This compound comprises an eosin-labeled cysteine at the N-terminal and the protein transduction domain from the HIV TAT protein (amino acids 49 to 57), fused to the Bcl-xL BH4 peptide. It is utilized in research concerning diseases associated with accelerated apoptosis [1]."

Compound 72-1, also known as BCL-xL/BCL-2 ligand 1, serves as a ligand for BCL-xL and BCL-2 proteins. It can be tethered to an E3 ligase via a linker, facilitating the formation of PROTACs [1] [2].

AZD4320 is an inhibitor of BH3-mimicking dual BCL2/BCLxL. For KPUM-MS3, KPUM-UH1, and STR-428 cells, the IC50s values are 26 nM, 17 nM, and 170 nM , respectively.

BCL-XL-IN-1 (Compound 11) is a selective inhibitor of BCL-XL, exhibiting a Ki of less than 0.01 nM against BCL-XLTR-FERT. It is primarily used in cancer research.

BCL-XL-IN-3 (Compound 11) is an inhibitor of BCL-XL, with a Ki of less than 0.01 nM. It suppresses cell viability in both normal Molt-4 cells and digitonin-permeabilized Molt-4 cells, with EC50 values of 77.8 nM and 0.07 nM, respectively. BCL-XL-IN-3 can be utilized as an ADC toxin for synthesizing Clezutoclax.

BCL-XL-IN-4 (compound 10) is a potent and selective BCL-XL inhibitor, exhibiting Ki values of 0.042 nM for BCL-XL and 170 nM for BCL-2. Additionally, BCL-XL-IN-4 demonstrates cytotoxic properties.

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.

Navitoclax-piperazine (ABT-263-piperazine) is a B-cell lymphoma extra large (BCL-XL) inhibitor.

CAY10404 (3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-T) is a potent and highly selective inhibitor of COX-2 and COX-1. It is also a potent inhibitor of PKB/Akt and MAPK signalling pathways and induces apoptosis in NSC-LC cells, with analgesic, anti-inflammatory and anti-cancer activities.

Lisaftoclax (Bcl-2/Bcl-xl inhibitor 1) is an oral dual inhibitor of Bcl-2 and Bcl-xl, with IC50 values of 2 nM and 5.9 nM for Bcl-2 and Bcl-xl, respectively. Lisaftoclax is used to treat chronic lymphocytic leukemia (CLL) by inhibiting the action of the BCL-2 protein, which promotes the death of leukemia cells.

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

PDK4-IN-1 hydrochloride, an anthraquinone derivative, is a potent and orally active inhibitor of pyruvate dehydrogenase kinase 4 (PDK4) with an IC50 value of 84 nM.

S55746 hydrochloride is a potent, orally active and selective inhibitor of BCL-2(Ki of 1.3 nM and a Kd of 3.9 nM),with antitumor activity with low toxicity.

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

WEHI-539 hydrochloride is a selective Bcl-XL inhibitor with an IC50 of 1.1 nM.