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pan-BET

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By Targets:	Apoptosis (1) Epigenetic Reader Domain (7) ERK (1) Ligands for E3 Ligase (1)
By Research Areas:	Cancer (8) Inflammation/Immunology (2)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-136570

GSK778 1 Publications Verification iBET-BD1	Epigenetic Reader Domain Apoptosis	Inflammation/Immunology Cancer
GSK778 (iBET-BD1), a chemical probe, is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC₅₀s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. GSK778 phenocopies the effects of pan-BET inhibitors in cancer models .

HY-13032B

Molibresib besylate 20+ Cited Publications GSK 525762C; I-BET 762 besylate	Epigenetic Reader Domain ERK	Cancer
Molibresib besylate (GSK 525762C; I-BET 762 besylate) is an orally active pan-BET inhibitor that targets and binds to BRD2, BRD3, BRD4 and BRDT. By competitively occupying acetylated lysine binding sites, Molibresib besylate disrupts the interaction between BET proteins and chromatin, thereby effectively inhibiting MYC expression and target gene transcription. Molibresib besylate exhibits broad antiproliferative activity, which not only inhibits cancer cell growth and induces growth arrest, but also downregulates mitosis-related genes and upregulates the level of p-ERK1/2. When combined with MEK inhibitors, Molibresib besylate shows a significant synergistic effect, reduces tumor burden in mouse models of leukemia, modulates the immune microenvironment and prolongs survival. Molibresib besylate is widely applicable to research related to acute myeloid leukemia, multiple myeloma, triple-negative breast cancer, small-cell lung cancer and various advanced refractory solid tumors .

HY-142520

I-BET567	Epigenetic Reader Domain	Inflammation/Immunology Cancer
I-BET567 is a potent and orally active inhibitor of *pan-BET* candidate with pIC₅₀s of 6.9 and 7.2 for BRD4 BD1 and BD2, respectively. I-BET567 has been demonstrated efficacy in mouse models of oncology and inflammation .

HY-100696

PNZ5	Epigenetic Reader Domain	Cancer
PNZ5 is a potent and isoxazole-based *pan-BET* inhibitor with high selectivity and potency similar to the well-established (+)-JQ1, with a K_D of 5.43 nM for BRD4(1) .

HY-111823

VH032 thiol VHL ligand 6	Ligands for E3 Ligase	Cancer
VH032 thiol (VHL ligand 6) is a VHL ligand, which binds to pan-BET inhibitor JQ1 via a linker to form PROTAC .

HY-153226

BET-IN-14	Epigenetic Reader Domain	Cancer
BET-IN-14 is an orally active pan BET inhibitor (IC₅₀: 5.35 nM). BET-IN-14 has anti-cancer activity .

HY-173315

pan-BET/BD2-IN-1	Epigenetic Reader Domain	Cancer
pan-BET/BD2-IN-1 (compound 6b) is a selective extra-terminal (BET) protein inhibitor (BRDT-1 K_i = 1.05 μM and BRD4-1 K_i = 0.68 μM). pan-BET/BD2-IN-1 inhibits MM.1S cancer cell growth with an IC₅₀ of 2.6 μM .

HY-155891

BET-IN-18	Epigenetic Reader Domain	Cancer
BET-IN-18 (Compound 3) is a pan-BET bromodomain small-molecule inhibitor, with K_i values of 0.69 μM and 0.37 μM, and K_d values of 1.6 μM and 8.4 μM against BrdT (1) and Brd4 (1) bromodomains, respectively. BET-IN-18 potently and competitively inhibits the binding of the known BET inhibitor (+)-JQ1 (HY-13030) to Brd4 (1) and BrdT (1), with IC₅₀ values of 1.0 μM and 2.3 μM, respectively. BET-IN-18 also competitively inhibits the binding of acetylated histone substrates to Brd4 (1) (IC₅₀ = 0.90 μM). BET-IN-18 can be used in the research of multiple myeloma .

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BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.

BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

MedchemExpress Validation 03

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred

MedchemExpress Validation 04

MedchemExpress Validation

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pan-BET

Inhibitors & Agonists