2. PROTAC Epigenetics Apoptosis
  3. PROTACs Epigenetic Reader Domain c-Myc Apoptosis
  4. PROTAC BET Degrader-18

PROTAC BET Degrader-18 is a PROTAC targeting BET, with a DC50 of 0.676 nM in HEK293-BRD4-HiBiT-KI cells. PROTAC BET Degrader-18 mainly targets and degrades BRD4 (EC50 = 59.91 nM), and exhibits weak degradation activity against BRD2. PROTAC BET Degrader-18 inhibits the expression of downstream oncoprotein c-Myc, thereby inducing cell cycle arrest and apoptosis, while suppressing oncoprotein expression. PROTAC BET Degrader-18 shows antiproliferative activity against acute myeloid leukemia cells and triple-negative breast cancer cells. PROTAC BET Degrader-18 demonstrates antitumor efficacy in xenograft mouse models. PROTAC BET Degrader-18 can be used for the research of acute myeloid leukemia and triple-negative breast cancer.
(Pink: BRD4 ligand (HY-184339); Blue: Cereblon ligand (HY-W023573); Black: linker).

For research use only. We do not sell to patients.

PROTAC BET Degrader-18

PROTAC BET Degrader-18 Chemical Structure

CAS No. : 3097564-20-7

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PROTAC BET Degrader-18 Related Antibodies

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Brd BRPF1 BRPF2 BRPF3 BRD2 BRD3 BRD4 BRDT CECR2 BD1 BD2 BRD7 BRD9 BET BAZ

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Description

PROTAC BET Degrader-18 is a PROTAC targeting BET, with a DC50 of 0.676 nM in HEK293-BRD4-HiBiT-KI cells. PROTAC BET Degrader-18 mainly targets and degrades BRD4 (EC50 = 59.91 nM), and exhibits weak degradation activity against BRD2. PROTAC BET Degrader-18 inhibits the expression of downstream oncoprotein c-Myc, thereby inducing cell cycle arrest and apoptosis, while suppressing oncoprotein expression. PROTAC BET Degrader-18 shows antiproliferative activity against acute myeloid leukemia cells and triple-negative breast cancer cells. PROTAC BET Degrader-18 demonstrates antitumor efficacy in xenograft mouse models. PROTAC BET Degrader-18 can be used for the research of acute myeloid leukemia and triple-negative breast cancer[1]. (Pink: BRD4 ligand (HY-184339); Blue: Cereblon ligand (HY-W023573); Black: linker).

IC50 & Target[1]

BRD4

59.91 nM (EC50)

BRD2

 

In Vitro

PROTAC BET Degrader-18 (compound 36) (F364) (50 nM; 48.8 pM-12.8 μM) efficiently promotes the formation of the CRBN::BRD4 BD1 ternary complex, with an EC50 of 59.91 nM[1].
PROTAC BET Degrader-18 (10 μM; 24 h) potently degrades BRD4 in HEK293-BRD4-HiBiT-KI cells, with a Dmax of 93.96% and a DC50 of 0.676 nM[1].
PROTAC BET Degrader-18 (10 μM) potently inhibits the proliferation of MV4-11 wild-type acute myeloid leukemia cells and SHP099-resistant MV4-11 acute myeloid leukemia cells, with IC50 values of 4.99 nM and 1.62 nM, respectively[1].
PROTAC BET Degrader-18 (10 μM; 200 nM) inhibits the proliferation of MDA-MB-231 triple-negative breast cancer cells, with an IC50 of 127.87 nM and an inhibition rate of 54.50% at a concentration of 200 nM[1].
PROTAC BET Degrader-18 (10 nM-5 μM; 48 h) induces CRBN-mediated proteasomal degradation of BRD4 (maximum degradation rate of 88.52%) and downregulates c-Myc (maximum downregulation rate of 83.21%) in MV4-11 acute myeloid leukemia cells following 48 h of treatment[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

PROTAC BET Degrader-18 Related Antibodies

Western Blot Analysis[1]

Cell Line: MV4-11 acute myeloid leukemia cells
Concentration: 10 nM, 50 nM, 200 nM, 1 μM, 5 μM
Incubation Time: 48 h
Result: Induced CRBN-mediated proteasomal degradation of BRD4 (maximum degradation rate of 88.52%) and downregulates c-Myc (maximum downregulation rate of 83.21%).
In Vivo

PROTAC BET Degrader-18 (compound 36) (F364) (5-20 mg/kg; intravenous injection; once every other day; 3 weeks) achieves a tumor growth inhibition rate of 88.90% in the MV4-11 acute myeloid leukemia xenograft model, while BRD4 and c-Myc in tumor tissues are significantly downregulated, with no toxicity observed[1].
PROTAC BET Degrader-18 (5-20 mg/kg; intravenous injection; once every two days; 3 weeks) achieves a tumor growth inhibition rate of 66.83% in the MDA-MB-231 triple-negative breast cancer xenograft model, with no toxicity observed[1].
PROTAC BET Degrader-18 (20 mg/kg; intravenous injection; administered every other day for 2 consecutive weeks) is well tolerated in normal BALB/c mice, with no toxicity observed[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c nude mice were subcutaneously inoculated with MV4-11 cells (1×108 cells/mL, 0.1 mL per mouse) suspended in serum-free medium and Matrigel
[1]
Dosage: 5 mg/kg; 20 mg/kg
Administration: i.v.; every other day; 3 weeks
Result: Achieved a tumor growth inhibition (TGI) rate of 88.90%.
Reduced BRD4 protein levels in tumor tissues by 84.61%.
Reduced c-Myc expression to 91.40%.
Caused no notable body weight loss or overt clinical abnormalities.
Showed no treatment-related hematotoxicity via routine hematology.
Revealed no significant abnormalities in histopathological examination of major organs (heart, liver, spleen, lung, kidney).
Animal Model: BALB/c nude mice were subcutaneously inoculated with MDA-MB-231 cells (1×108 cells/mL, 0.1 mL per mouse) suspended in serum-free medium and Matrigel
[1]
Dosage: 5 mg/kg; 20 mg/kg
Administration: i.v.; every other day; 3 weeks
Result: Achieved a tumor growth inhibition (TGI) rate of 66.83%.
Caused no notable body weight loss or overt clinical abnormalities.
Showed no treatment-related hematotoxicity via routine hematology.
Revealed no significant abnormalities in histopathological examination of major organs (heart, liver, spleen, lung, kidney).
Molecular Weight

991.12

Formula

C51H58N8O11S
CAS No.
SMILES

CC(C1=C(NC(C(NC2=C(C=CC(S(=O)(N3CCOCC3)=O)=C2)OCCCC(N4CCN(CC4)CC5CCN(CC5)C6=CC=C7C(N(C(C7=C6)=O)C8CCC(NC8=O)=O)=O)=O)=O)=C1C9=CC=CC=C9)C)=O
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Purity & Documentation
References
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PROTAC BET Degrader-18 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PROTAC BET Degrader-183097564-20-7PROTAC BET Degrader18PROTAC BET Degrader 18PROTACsEpigenetic Reader Domainc-MycApoptosisMycBRD4acute myeloid leukemia cellstriple-negative breast cancer cellsubiquitin-proteasomal pathwayxenograft mouse modelscereblonCRBNHEK293-BRD4-HiBiT-KI cellsMV4-11 cellsInhibitorinhibitorinhibit

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