2. PROTAC Epigenetics Apoptosis
  3. PROTACs Epigenetic Reader Domain Apoptosis
  4. PROTAC BRD9 Degrader-8

PROTAC BRD9 Degrader-8 is a selective, orally active BRD9 PROTAC degrader with a DC50 of 16 pM.\nPROTAC BRD9 Degrader-8 induces cell cycle arrest at the G1 phase and promotes apoptosis. PROTAC BRD9 Degrader-8 can be used for research on acute myeloid leukemia and diffuse large B-cell lymphoma.
(Pink: BRD9 ligand (HY-175915); Blue: Cereblon ligand (HY-W585171); Black: linker).

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

PROTAC BRD9 Degrader-8

PROTAC BRD9 Degrader-8 Chemical Structure

CAS No. : 3081180-48-2

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PROTAC BRD9 Degrader-8 Related Antibodies

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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Description

PROTAC BRD9 Degrader-8 is a selective, orally active BRD9 PROTAC degrader with a DC50 of 16 pM.\nPROTAC BRD9 Degrader-8 induces cell cycle arrest at the G1 phase and promotes apoptosis. PROTAC BRD9 Degrader-8 can be used for research on acute myeloid leukemia and diffuse large B-cell lymphoma[1]. (Pink: BRD9 ligand (HY-175915); Blue: Cereblon ligand (HY-W585171); Black: linker).

IC50 & Target[1]

BRD9

16 pM (DC50)

In Vitro

PROTAC BRD9 Degrader-8 (Compound E5) (7 days) potently inhibits proliferation of MV4-11, MOLM13, Kasumi-1, and OCI-LY10 hematological tumor cells with IC50 values ranging from 0.27 nM to 1.13 nM, with activity dependent on CRBN expression, and exhibits weaker activity in SU-DHL-2, SU-DHL-6, and U937 cells[1].
PROTAC BRD9 Degrader-8 (compound E5) (24 h) induces G1 phase cell cycle arrest in MV4-11 cells after 24 h of treatment[1].
PROTAC BRD9 Degrader-8 (compound E5) (0.01-10 nM; 48 h) dose-dependently induces apoptosis in MV4-11 cells after 48 h of treatment, with significant apoptosis observed at concentrations as low as 0.01 nM[1].

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

PROTAC BRD9 Degrader-8 Related Antibodies

Cell Cycle Analysis[1]

Cell Line: MV4-11 acute myeloid leukemia cells
Concentration: 0.01, 0.1, 1 and 10 nM
Incubation Time: 24 h
Result: Induced cell cycle arrest at the G1 phas

Apoptosis Analysis[1]

Cell Line: MV4-11 acute myeloid leukemia cells
Concentration: 0.01, 0.1, 1 and 10 nM
Incubation Time: 48 h
Result: Induced cell apoptosis.
In Vivo

PROTAC BRD9 Degrader-8 (Compound E5) (20 mg/kg; i.p.; once daily; for 19 consecutive days) achieves a tumor growth inhibition rate of 30.92% in a nude mouse MV4-11 acute myeloid leukemia xenograft model, while inducing complete degradation of BRD9 in tumor tissues with no observed toxicity[1].
PROTAC BRD9 Degrader-8 (30 mg/kg; p.o.; once daily; for 18 consecutive days) inhibits tumor growth of OCI-LY10 diffuse large B-cell lymphoma xenografts in mice to 40% of that in the vehicle control group, with no observed toxicity[1].

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

Animal Model: Nude mice[1]
Dosage: 20 mg/kg
Administration: i.p.; daily; 19 days
Result: Completely degraded BRD9 protein in tumor tissue relative to vehicle controls.
Achieved 30.92% tumor growth inhibition (TGI).
Reduced mean tumor volume to 766 mm3 vs 1187 mm3 in vehicle group.
Reduced mean relative tumor volume to 4.99 vs 7.85 in vehicle group.
Reduced mean tumor weight to 0.90 g vs 1.30 g in vehicle group.
Caused no significant weight loss or behavioral abnormalities in treated mice.
Animal Model: Balb/c mice[1]
Dosage: 30 mg/kg
Administration: p.o.; daily; 18 days
Result: Reduced mean tumor volume to 309 mm3 vs 561 mm3 in vehicle group.
Reduced mean relative tumor volume to 4.00 vs 9.07 in vehicle group.
Achieved a tumor growth ratio (T/C%) of approximately 40%.
Reduced mean tumor weight to 0.56 g vs 1.12 g in vehicle group.
Caused no significant weight fluctuation or mortality in treated mice.
Molecular Weight

767.91

Formula

C46H49N5O6
CAS No.
SMILES

O=C1C2=C(C(C3=CC(OC)=C(C(OC)=C3)CN4CCC(CN5CCC(CC5)C6=C7C(C8=CC=C7)=C(C=C6)N(C9C(NC(CC9)=O)=O)C8=O)CC4)=CN1C)C=CC=C2
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PROTAC BRD9 Degrader-8 Related Classifications

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Help & FAQs
  • 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 BRD9 Degrader-83081180-48-2PROTACsEpigenetic Reader DomainApoptosishematological tumor cellsubiquitin-proteasome systemMV4-11 cellsBRD7BRD9xenograft tumor modelsCRBNacute myeloid leukemiadiffuse large b-cell lymphomaBRD4Inhibitorinhibitorinhibit

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