2. PROTAC Epigenetics
  3. PROTACs Epigenetic Reader Domain
  4. BD-9136

BD-9136 is a potent and highly selective BRD4 PROTAC depressant. BD-9136 has low-nanomolar degradation potencies against BRD4 , and its degradation selectivity for BRD4 is 1000 times that of BRD2 and BRD3 proteins. BD-9136 has antitumor activity.(Pink: Desmethyl-QCA276 (HY-44103); Black: 3-(2-(4-Methylpiperazin-1-yl)ethyl)azetidin-3-ol; Blue: Thalidomide-4-OH (HY-103596))

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

BD-9136 Chemical Structure

BD-9136 Chemical Structure

CAS No. : 3037514-38-5

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Based on 1 publication(s) in Google Scholar

BD-9136 Related Antibodies

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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Description

BD-9136 is a potent and highly selective BRD4 PROTAC depressant. BD-9136 has low-nanomolar degradation potencies against BRD4 , and its degradation selectivity for BRD4 is 1000 times that of BRD2 and BRD3 proteins. BD-9136 has antitumor activity[1].(Pink: Desmethyl-QCA276 (HY-44103); Black: 3-(2-(4-Methylpiperazin-1-yl)ethyl)azetidin-3-ol; Blue: Thalidomide-4-OH (HY-103596))

In Vitro

BD-9136 (0-1 μM; 4 h) induces BRD4 degradation in 8 cancer cell lines, DC50 is 0.1-4.7 nM, Dmax > 90%, and has no degradation effect on BRD2 and BRD3[1].

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

BD-9136 Related Antibodies

Western Blot Analysis[1]

Cell Line: MV4;11 and MDAMB-231 cells
Concentration: 0, 0.1, 0.3, 1, 3, 10, 30, 100, 300, 1000 nM
Incubation Time: 4 h
Result: Reduced the level of BRD4, but BRD2 and BRD3 did not change.
In Vivo

BD-9136 (20 mg/kg; Intraperitoneal injection; 5 times a week for 4 weeks) has anti-tumor effects in mouse models of tumor cell xenograft[1].

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

Animal Model: SCID mice bearing the MV4;11 xenograft tumors[1]
Dosage: 20 mg/kg
Administration: Intraperitoneal injection (i.p.); 5 days a week for 4 weeks
Result: Achieved 92% of tumor growth inhibition at the end of the treatment.
Caused no significant weight loss or other signs of toxicity in mice during the entire experiment.
Molecular Weight

824.95

Formula

C44H44N10O5S
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

CC1=NN=C2COCC(C(CC3=CC=CC=C3)=C(S4)C#CC5=CN(N=C5)C6(CCN7CCN(CC7)C)CN(C8=C(C9=CC=C8)C(N(C9=O)C%10CCC(NC%10=O)=O)=O)C6)=C4N21
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (121.22 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.2122 mL 6.0610 mL 12.1219 mL
5 mM 0.2424 mL 1.2122 mL 2.4244 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.2122 mL 6.0610 mL 12.1219 mL 30.3049 mL
5 mM 0.2424 mL 1.2122 mL 2.4244 mL 6.0610 mL
10 mM 0.1212 mL 0.6061 mL 1.2122 mL 3.0305 mL
15 mM 0.0808 mL 0.4041 mL 0.8081 mL 2.0203 mL
20 mM 0.0606 mL 0.3030 mL 0.6061 mL 1.5152 mL
25 mM 0.0485 mL 0.2424 mL 0.4849 mL 1.2122 mL
30 mM 0.0404 mL 0.2020 mL 0.4041 mL 1.0102 mL
40 mM 0.0303 mL 0.1515 mL 0.3030 mL 0.7576 mL
50 mM 0.0242 mL 0.1212 mL 0.2424 mL 0.6061 mL
60 mM 0.0202 mL 0.1010 mL 0.2020 mL 0.5051 mL
80 mM 0.0152 mL 0.0758 mL 0.1515 mL 0.3788 mL
100 mM 0.0121 mL 0.0606 mL 0.1212 mL 0.3030 mL
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BD-9136 Related Classifications

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:

BD-91363037514-38-5BD9136BD 9136PROTACsEpigenetic Reader DomainMV4;11 cellsMDAMB-231 cellsInhibitorinhibitorinhibit

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