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BRD4 levels

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Akt (3) Apoptosis (9) Autophagy (1) Bcl-2 Family (1) c-Myc (8) Casein Kinase (1) Caspase (2) CDK (2) DNA/RNA Synthesis (1) Epigenetic Reader Domain (21) ERK (1) FGFR (1) FKBP (2) FLT3 (1) JAK (1) MDM-2/p53 (1) PARP (1) PDGFR (1) PI3K (1) PROTACs (12) Reactive Oxygen Species (ROS) (1) Reference Standards (1) RET (1) ROS Kinase (1) STAT (1) Survivin (1)
By Research Areas:	Cancer (23) Neurological Disease (1)
Click Chemistry:	Alkynes (2)

Inhibitors & Agonists

Peptides

Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-103633

PROTAC BET Degrader-1 2 Publications Verification	PROTACs Epigenetic Reader Domain	Cancer
PROTAC BET Degrader-1 is a PROTAC connected by ligands for Cereblon and BET, decreasing BRD2, BRD3, and BRD4 protein levels at low concentration.

HY-132941

CFT-2718	PROTACs Epigenetic Reader Domain c-Myc Apoptosis	Cancer
CFT-2718 is a selective CRBN-dependent BRD4 PROTAC degrader. CFT-2718 mediates rapid, selective BRD4 degradation, reduces total and phosphorylated Ser2 RPB1 levels, and reduces MYC protein levels. CFT-2718 can inhibit cancer cells proliferation and induce apoptosis. CFT-2718 reduces growth of lung cancer and pancreatic patient-derived xenograft models. CFT-2718 can be used for the research of cancer, such as small-cell lung cancer and pancreatic cancer .

HY-151593

dBRD4-BD1	PROTACs Epigenetic Reader Domain	Cancer
dBRD4-BD1 is a selective and durable *BRD4* degrader with an DC₅₀ value of 280 nM (D_max=77%). dBRD4-BD1 upregulates BRD2/3 protein level and shows low cytotoxicity than iBRD4-BD1 .

HY-P10446

TAT-PiET-PROTAC	Epigenetic Reader Domain PROTACs	Cancer
TAT-PiET-PROTAC is a proteolysis-targeting chimera (PROTAC)-modified TAT-PiET (HY-P10445), which is a cell-penetrating peptide targeting the extra-terminal (ET) domain of *BRD4. TAT-PiET-PROTAC can reduce BRD4* and JMJD6 levels and inhibit cell proliferation. TAT-PiET-PROTAC also resists the endocrine resistance of ERα-positive breast cancer cells. TAT-PiET-PROTAC can be used for the research of cancer, such as breast cancer .

HY-168936

DP-15	PROTACs Epigenetic Reader Domain Apoptosis	Cancer
DP-15 is the degrader for GSPT1 and *BRD4* with DC₅₀s of 5.25 nM and 0.48 nM. DP-15 exhibits anti-proliferative activity of AML cells and NHL cells with an IC₅₀ of nanomolar levels, arrests the cell cycle at G1 phase, and induces apoptosis in MOLM13. DP-15 exhibits anti-leukemia activity in MOLM-13 xenograft mouse models . (Pink: ligand for target protein JQ-1 carboxylic acid (HY-78695); Black: linker (HY-W262798); Blue: ligand for E3 ligase Cereblon Thalidomide-5-OH (HY-23095))

HY-168635

SJ46420	PROTACs Epigenetic Reader Domain	Cancer
SJ46420, a SJ46421 (HY-168634) pro-drug variant, is a potent and selective BRD3 PROTAC degrader. SJ46420 degrads BRD3 in a KLHDC2-dependent manner, thereby partially reducing the levels of BRD2 or BRD4 (Pink: ligand for target protein (HY-13030); Black: linker (HY-20797); Blue: E3 ligase ligand (HY-159973)) .

HY-176502

FKBP12 ligand-3	FKBP	Cancer
FKBP12 ligand-3 (compound dj) is a high-affinity ligand targeting FKBP12. FKBP12 ligand-3 can be used to selectively enhance the binding of heterobifunctional molecules to BRD4, enriching the drug intracellularly through the "CellTrap" effect to form a ternary complex of FKBP12-ligand-BRD4. This ternary complex has inhibitory activity against BRD4, thereby inhibiting the expression of BRD4 target genes (such as MYC) and inducing tumor cell death. FKBP12 ligand-3 can be used for selective cancer research based on differences in intracellular presenter protein levels .

HY-143235

BRD4 Inhibitor-15	Epigenetic Reader Domain Apoptosis Bcl-2 Family Caspase c-Myc	Cancer
BRD4 Inhibitor-15 (compound 13) is a potent *BRD4* inhibitor, with an IC₅₀ of 18 nM. BRD4 Inhibitor-15 induces apoptosis of 22RV1 cells by regulating Bcl-2/Bax proteins and activating caspase-3 signaling pathway. BRD4 Inhibitor-15 down-regulates the c-Myc level in 22RV1 cells. BRD4 Inhibitor-15 can be used for prostate cancer research .

HY-176035

MS479	PROTACs Epigenetic Reader Domain	Cancer
MS479 is a BRD4 PROTAC degrader. MS479 binds BRD4-BD2 and GLP with high affinities (BRD4-BD2: K_d = 200 nM; GLP: K_d = 306 nM). MS479 can reduce the protein level of BRD4 short isoform. MS479 recruits the E3 ligase SPOP by directly binding its substrate GLP as a bridge protein. MS479 can be used to inhibit the proliferation of colorectal cancer cells. (Pink: BRD4 ligand (HY-78695); Blue: GLP ligand (HY-176036); Black: linker (HY-176037); GLP ligand+linker: HY-176038) .

HY-176501

FKBP12 ligand-2	FKBP	Cancer
FKBP12 ligand-2 (compound d) is a high affinity ligand targeting FKBP12. FKBP12 ligand-2 can be used to selectively enhance the binding of heterobifunctional molecules to BRD4, enriching the drug intracellularly through the "CellTrap" effect to form a ternary complex of FKBP12-ligand-BRD4. This ternary complex has inhibitory activity against BRD4, thereby inhibiting the expression of BRD4 target genes (such as MYC) and inducing tumor cell death. FKBP12 ligand-2 can be used for selective cancer research based on differences in intracellular presenter protein levels .

HY-146660

BRD4 Inhibitor-18	c-Myc Epigenetic Reader Domain Apoptosis	Cancer
BRD4 Inhibitor-18 is a highly potent *BRD4* inhibitor with an IC₅₀ value of 110 nM. BRD4 Inhibitor-18 has a hydrophobic acetylcyclopentanyl side chain. BRD4 Inhibitor-18 can significantly suppress the proliferation of MV-4-11 cells with high BRD4 level. BRD4 Inhibitor-18 has apoptosis-promoting and G0/G1 cycle-arresting activity .

HY-169994

BC13	CDK Epigenetic Reader Domain Apoptosis DNA/RNA Synthesis Reactive Oxygen Species (ROS)	Cancer
BC13 is a *CDK6/BRD4* inhibitor with the IC₅₀ values of 234 nM and 36 nM for CDK6 and BRD4, respectively. BC13 shows antiproliferative activity and induces cell apoptosis and DNA damage. BC13 increases in ROS levels .

HY-P10445

TAT-PiET	Epigenetic Reader Domain	Cancer
TAT-PiET is a cell-penetrating peptide targeting the extra-terminal (ET) domain of *BRD4. TAT-PiET can reduce BRD4* and JMJD6 levels and inhibit cell proliferation. TAT-PiET also resists the endocrine resistance of ERα-positive breast cancer cells. TAT-PiET can be used for the research of cancer, such as breast cancer .

HY-182801

PROTAC BRD4 Degrader-46	PROTACs Epigenetic Reader Domain c-Myc	Cancer
PROTAC BRD4 Degrader-46 is a heterobifunctional *BRD4* PROTAC degrader. PROTAC BRD4 Degrader-46 binds to both *BRD4* and CRBN, thereby triggering ubiquitination and proteasomal degradation of *BRD4. PROTAC BRD4* Degrader-46 downregulates the levels of downstream BRD2, BRD3 and MYC. PROTAC BRD4 Degrader-46 can be used in the research of cancers such as multiple myeloma .

HY-183273

BRD4/AKT-IN-1	Epigenetic Reader Domain Akt CDK Autophagy Apoptosis	Cancer
BRD4/AKT-IN-1 is a *BRD4/AKT* inhibitor with *BRD4* IC₅₀ 66.12 nM and AKT1 IC₅₀ 143.81 nM. BRD4/AKT-IN-1 blocks *BRD4*-mediated c-Myc transcriptional regulation, modulates AKT1 signaling, decouples AKT phosphorylation from pro-survival effectors. BRD4/AKT-IN-1 induces G0/G1 cell cycle arrest via downregulated phosphorylated RB, cyclin E1, CDK2. BRD4/AKT-IN-1 elevates LC3B levels to promote autophagy. BRD4/AKT-IN-1 promotes apoptosis in cancer cells. BRD4/AKT-IN-1 can be used for the research of metastatic castration-resistant prostate cancer .

HY-115541

BRD4-IN-41	Epigenetic Reader Domain JAK FLT3 RET ROS Kinase PDGFR FGFR c-Myc STAT Apoptosis PARP	Cancer
BRD4-IN-41 is a *BRD4* inhibitor with an IC₅₀ of 34 nM. BRD4-IN-41 also inhibits JAK2, FLT3, RET, ROS1, NTRK3, PDGFRb, and FGFR1 kinases with IC₅₀ values ranging from 0.9 nM to 43 nM. BRD4-IN-41 inhibits acetyl-lysine binding site of BRD4, downregulates c-MYC, reduces phosphorylated STAT3 levels, induces G1 cell cycle arrest and apoptosis, thereby inhibiting cancer cells growth. BRD4-IN-41 can be used for the research of cancer, such as multiple myeloma and acute myeloid leukemia .

HY-179734

PROTAC BRD4 Degrader-41	PROTACs Epigenetic Reader Domain Apoptosis c-Myc	Cancer
PROTAC BRD4 Degrader-41 (Compound A5) is a BRD4 PROTAC degrader with a DC₅₀ of 0.97 nM. PROTAC BRD4 Degrader-41 exhibits potent anti-proliferative activity against various types of cancer cells such as AML, lymphoma, breast cancer, ovarian cancer, and non-small cell lung cancer. PROTAC BRD4 Degrader-41 can induce G0/G1 phase arrest and apoptosis in MV4-11 cells. PROTAC BRD4 Degrader-41 downregulates the transcriptional level of c-Myc .

HY-157561

K2-B4-3e	PROTACs Epigenetic Reader Domain	Cancer
K2-B4-3e is a potent BRD4 PROTAC. K2-B4-3e induces BRD4 degradation with a DC₅₀ value of 66 nM .

HY-183770

LCI40	Akt PI3K Epigenetic Reader Domain c-Myc	Cancer
LCI40 is an orally active dual *PI3K/BRD4* inhibitor (PI3Kα IC₅₀ = 0.071 μM, PI3Kβ IC_{50 =}0.17 μM, PI3Kγ IC₅₀ = 0.66 μM, PI3Kδ IC₅₀ = 0.072 μM, *BRD4* BD1 IC₅₀ = 0.19 μM, and *BRD4* BD2 IC₅₀ = 1.88 μM. LCI40 inhibits phosphorylation of pAKT (S473) and suppresses c-MYC levels in mantle cell lymphoma cells. LCI40 displays immunomodulatory capacity with minimal toxicity to normal mouse immune cells. LCI40 can be used for the research of mantle cell lymphoma .

HY-103633R

PROTAC BET Degrader-1 (Standard)	Reference Standards PROTACs Epigenetic Reader Domain	Cancer
PROTAC BET Degrader-1 (Standard) is the analytical standard of PROTAC BET Degrader-1 (HY-103633). This product is intended for research and analytical applications. PROTAC BET Degrader-1 is a PROTAC connected by ligands for Cereblon and BET, decreasing BRD2, BRD3, and BRD4 protein levels at low concentration.

HY-179588

PROTAC BET Degrader-14	PROTACs Epigenetic Reader Domain c-Myc	Cancer
PROTAC BET Degrader-14 is a highly efficient PROTAC targeting BET (bromodomain and extra-terminal domain). PROTAC BET Degrader-14 can degrade all BET (BRD2, BRD3, BRD4) family proteins. PROTAC BET Degrader-14 potently degrades BET proteins in U2OS osteosarcoma cell lines (BRD4 DC₅₀ = 130 nM) and KYSE180 esophageal squamous cell carcinoma cell lines (DC₅₀ = 40 nM). PROTAC BET Degrader-14’s dependence on the ubiquitin-proteasome system. PROTAC BET Degrader-14 decreases levels of BET-regulated gene products c-Myc, RUNX2, and KRT14. PROTAC BET Degrader-14 can be used for the study of osteosarcoma .

HY-181442

CK2-TN03	Casein Kinase Survivin Epigenetic Reader Domain Akt Apoptosis Caspase MDM-2/p53	Neurological Disease Cancer
CK2-TN03 is an ATP-competitive casein kinase 2 (CK2) inhibitor, with an IC₅₀ of 165 nM and a K_i of 20 nM. CK2-TN03 inhibits CK2-mediated survivin activation and reduces CK2-dependent phosphorylation levels of *BRD4/MYCN* and AKT1. CK2-TN03 exerts anti-neuroblastoma effects by inhibiting survivin, leading to mitotic catastrophe and apoptosis of cancer cells. CK2-TN03 can be used in studies related to neuroblastoma .

Cat. No.	Product Name	Target	Research Area

HY-P10446

TAT-PiET-PROTAC	Epigenetic Reader Domain PROTACs	Cancer
TAT-PiET-PROTAC is a proteolysis-targeting chimera (PROTAC)-modified TAT-PiET (HY-P10445), which is a cell-penetrating peptide targeting the extra-terminal (ET) domain of *BRD4. TAT-PiET-PROTAC can reduce BRD4* and JMJD6 levels and inhibit cell proliferation. TAT-PiET-PROTAC also resists the endocrine resistance of ERα-positive breast cancer cells. TAT-PiET-PROTAC can be used for the research of cancer, such as breast cancer .

HY-P10445

TAT-PiET	Epigenetic Reader Domain	Cancer
TAT-PiET is a cell-penetrating peptide targeting the extra-terminal (ET) domain of *BRD4. TAT-PiET can reduce BRD4* and JMJD6 levels and inhibit cell proliferation. TAT-PiET also resists the endocrine resistance of ERα-positive breast cancer cells. TAT-PiET can be used for the research of cancer, such as breast cancer .

Cat. No.	Product Name		Classification

HY-176502

FKBP12 ligand-3		Alkynes
FKBP12 ligand-3 (compound dj) is a high-affinity ligand targeting FKBP12. FKBP12 ligand-3 can be used to selectively enhance the binding of heterobifunctional molecules to BRD4, enriching the drug intracellularly through the "CellTrap" effect to form a ternary complex of FKBP12-ligand-BRD4. This ternary complex has inhibitory activity against BRD4, thereby inhibiting the expression of BRD4 target genes (such as MYC) and inducing tumor cell death. FKBP12 ligand-3 can be used for selective cancer research based on differences in intracellular presenter protein levels .

HY-176501

FKBP12 ligand-2		Alkynes
FKBP12 ligand-2 (compound d) is a high affinity ligand targeting FKBP12. FKBP12 ligand-2 can be used to selectively enhance the binding of heterobifunctional molecules to BRD4, enriching the drug intracellularly through the "CellTrap" effect to form a ternary complex of FKBP12-ligand-BRD4. This ternary complex has inhibitory activity against BRD4, thereby inhibiting the expression of BRD4 target genes (such as MYC) and inducing tumor cell death. FKBP12 ligand-2 can be used for selective cancer research based on differences in intracellular presenter protein levels .

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