bcl-1

Bcl-B inhibitor 1 is an antitumor compound that binds to and inactivates pro-apoptotic proteins in the BH3 structural domain.

MCL-1 BCL-2-IN-2 (Compound Nap-1) is a potent and selective dual inhibitor of Mcl-1 and Bcl-2, with IC50 values of 4.45 μM and 3.18 μM, respectively [1].

MCL-1 BCL-2-IN-2 is a potent and selective dual inhibitor of Bcl-2 and Mcl-1.

MCL-1 BCL-2-IN-3 is a selective and potent dual inhibitor of Mcl-1 and Bcl-2, with IC50 values of 5.95 and 4.78 μM, respectively.

MCL-1 BCL-2-IN-4 is a selective and potent dual inhibitor of Mcl-1 and Bcl-2.

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-2 Mcl-1-IN-1 is an inhibitor of Bcl-2 (Ki: 4.53 μM) and Mcl-1 (Ki: 1.19 μM), and can be used in cancer research.

Bcl-2 Mcl-1-IN-2 is an inhibitor of Bcl-2 [Ki: 4.70 μM] and Mcl-1 [Ki: 0.88 μM], suitable for use in cancer research.

Bcl-2 Mcl-1-IN-3 is a Bcl-2 Mcl-1 inhibitor, targeting Mcl-1 (Ki: 0.14 μM) and Bcl-2 (Ki: 0.23 μM), suitable for cancer research.

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

Beclin1-Bcl-2 Interaction Inhibitor 1 effectively disrupts the binding of Beclin 1 to Bcl-2, and is utilized in cancer and neurodegeneration research [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].

Bcl-2 Mcl-1-IN-4 (compound 20) acts as a dual inhibitor targeting Bcl-2 (Ki=0.49 μM) and Mcl-1 (Ki=0.51 μM). This compound effectively suppresses cancer cell proliferation and induces apoptosis in U937 cells. It is utilized in cancer research.

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.

1. Dehydrocorydaline (13-Methylpalmatine) exerts anti-metastatic potential via suppression of MMPs and Bcl-2 signaling in NSC-LC cells. 2. Dehydrocorydaline stimulates p38 MAPK activation, which can enhance heterodimerization of MyoD and E proteins, thus resulting in MyoD activation and myoblast differentiation. 3. Dehydrocorydaline shows antiplatelet effects, it inhibits thrombin-induced platelet aggregation in a low dose ( IC50= 34.914 ug mL). 4. Dehydrocorydaline has anti-inflammatory and antinociceptive effects. 5. Dehydrocorydaline inhibits MCF-7 cell proliferation by inducing apoptosis mediated by regulating Bax Bcl-2, activating caspases as well as cleaving PARP.

Sonrotoclax is a potent, orally active inhibitor of Bcl2, demonstrating effective cell-killing activity against a range of lymphoma and leukemia cell lines [1].

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).

Amantadine hydrochloride (CI-719) is an antiviral that is used in the prophylactic or symptomatic treatment of influenza A and Parkinson disease.

BT2, a BCKDC kinase (BDK) inhibitor, exhibits an IC50 of 3.19 μM and functions as a potent, selective Mcl-1 inhibitor with a Ki value of 59 μM. Its interaction with BDK induces helix movements in the N-terminal domain, leading to BDK's dissociation from the branched-chain α-ketoacid dehydrogenase complex (BCKDC).

Monoethyl pimelate is a PROTAC linker, which refers to the alkyl ether composition. Monoethyl pimelate can be used in the synthesis of (S,R,S)-AHPC-Me-C7 ester, a specific BCL-XL PROTAC degrader[1].