bcl-6

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.

BI-3812 is an inhibitor of BCL6. Which inhibiting the BTB domain of BCL6 (IC50: 3 nM). BI-3812 also has antitumor activity.

CID5721353 (BCL6 inhibitor) is a B-Cell Lymphoma 6 Inhibitor (BCL6 inhibitor) that disrupts BCL6/corepressor complexes in vitro and in vivo, and was shown to bind the critical site within the BTB groove.

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

BCL6-IN-6 is an inhibitor of Bcl-6 and can be used in studies about diffuse large B-cell lymphoma. BCL6-IN-6 blocks the interaction of Bcl-6 with its corepressors and dose-dependently reactivates Bcl-6 target genes.

Bcl-2-IN-6 is a potent inhibitor of Bcl-2 (b-cell lymphoma-2) that downregulates Bcl-2 expression and increases the expression of p53, Bax, and caspase-7 mRNA. bcl-2-IN-7 induces cell cycle arrest and apoptosis in breast cancer MCF-7 cells. bcl-2-IN-7 acts on MCF-7 cells ( Bcl2-IN-7 showed good antitumor effects on MCF-7 cells (IC50: 20.91 μM), LoVo cells (IC50: 22.30 μM), HepG2 cells (IC50: 42.29 μM) and A549 cells (IC50: 48.00 μM).

ARV-393 HCl is an orally active and potent PROTAC targeting BCL6 with antitumor activity for the study of non-Hodgkin's lymphoma.

ARV-393 is a PROTAC degrader targeting BCL6 with the advantage of being highly potent and orally available.ARV-393 recruits BCL6 and E3 ligase cerebellum to rapidly degrade BCL6 through the cell's natural ubiquitin proteasome system for the treatment of diffuse large b-cell lymphoma (DLBCL) and non-Hodgkin's lymphoma (NHL).

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).

BI-3802, a highly potent BCL6 degrader, targets and inhibits the Bric-à-brac (BTB) domain of BCL6, exhibiting an IC50 value of ≤3 nM. It induces polymerization of BCL6 and facilitates its degradation in a manner dependent on the E3 ligase SIAH1, demonstrating notable antitumor activity[1][2].

BCL6-IN-7 (BCL6 inhibitor-7) is a BCL6 co-repressor interaction inhibitor with potential anticancer activity. It can be used for studying lymphomas.

EB-TCIP (BAK-04-212) is a bivalent molecule composed of AP1867 and BI-3812. It facilitates the reversible formation of a ternary complex between FKBPF36V and BCL6BTB, thereby recruiting FKBP12F36V-tagged EWS/FLI1 to DNA sites bound by the transcriptional regulator BCL6, rapidly inducing expression of BCL6 target genes such as SOCS2 and CXCL11. EWS/FLI1 is a fusion transcription factor found in Ewing sarcoma. EB-TCIP is applicable for studying transcriptional dysregulation in cancer.

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-8c is an orally active and potent inhibitor of B-cell lymphoma 6 (BCL6)-corepressor interaction(IC50 of 0.10 μM in cell-free enzyme-linked immunosorbent assay).

PBOX 6 is a pyrrolo-1,5-benzoxazepine (PBOX) compound exhibiting anticancer and antitumor activity by inhibiting breast cancer cell growth in vitro and selectively inducing apoptosis in leukemia cells through c-Jun NH2 terminal kinase-dependent phosphorylation and inactivation of Bcl-2 and Bcl-XL.

Bfl-1-IN-6 (Compound 20) is an orally active inhibitor of Bcl-2-related protein A1 (BFL1) with an IC50 of 19 nM. This compound can stabilize BFL1 protein, activate cleaved caspase 3, and demonstrates antitumor activity in mouse models.

BCL6-IN-4, a potent inhibitor of B-cell lymphoma 6 (BCL6), exhibits anti-tumor activities with an inhibitory concentration 50 (IC50) value of 97 nM[1].

3',6-Disinapoylsucrose (Disinapoyl sucrose) shows the neuroprotective effect and antidepressive activity in rats.

BCL6-IN-5 is a highly effective inhibitor of BCL6. It exhibits a pIC50 value of 5.82.

Mcl-1 inhibitor 6 is a potent, orally active chemical compound that selectively inhibits the myeloid cell leukemia 1 (Mcl-1) protein, with a high affinity (K d = 0.23 nM) and binding activity (K i = 0.02 μM). This compound exhibits exceptional selectivity over other members of the Bcl-2 family, including Bcl-2, Bcl2A1, Bcl-xL, and Bcl-w (K d >10 μM). Notably, Mcl-1 inhibitor 6 demonstrates strong antitumor activity.

Puerarin 6''-O-xyloside possesses significant anti-osteoporotic activity on ovariectomy mice, it has significant antitumour activities, the mechanisms are related to increased levels of caspase-3, caspase-7, caspase-9 and Bax, and reduced levels Bcl-2.

A-1331852 is a potent and selectiveBCL-XL inhibitor and may be useful in the treatment of cancer, immune and autoimmune diseases.

Atiprimod is an orally bioavailable small molecule belonging to the azaspirane class of cationic amphiphilic agents with anti-inflammatory, antineoplastic, and antiangiogenic properties. Atiprimod inhibits the phosphorylation of signal transducer and activator of transcription 3 (STAT3), blocking the signalling pathways of interleukin-6 and vascular endothelial growth factor (VEGF) and downregulating the anti-apoptotic proteins Bcl-2, Bcl-XL, and Mcl-1, thereby inhibiting cell proliferation, inducing cell cycle arrest, and inducing apoptosis.

Edratide (TV 4710), a 19-amino-acid synthetic peptide derived from the complementarity-determining region 1 (CDR1) of a human anti-DNA antibody that exhibits the 16 6 Id idiotype, has been found to lower apoptosis rates and regulate the expression of caspase-8 and caspase-3 downward, while increasing Bcl-xL expression. It shows promise for systemic lupus erythematosus (SLE) research [1] [2] [3].