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Art. -Nr.: HY-170900

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SJ44236

SJ44236 is a BET PROTAC degrader with activity against BRD2, BRD3 and BRD4 (DC₅₀ = 127 pM). SJ44236 induces ubiquitination and proteasomal degradation by forming a ternary complex with BET proteins and CRBN-DDB1. SJ44236 downregulates c-Myc, upregulates p53 and reduces cancer cell viability. SJ44236 can be used for the research of leukemia and medulloblastoma.
(Pink: BET ligand (HY-78695); Blue: Cereblon ligand (HY-W890189); Black: linker (HY-W012935)).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Formel: C₄₀H₄₅ClN₈O₃S
Molecular Weight:753.36

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (271 KB)

SJ44236 Chemical Structure

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

SJ44236 is a BET PROTAC degrader with activity against BRD2, BRD3 and BRD4 (DC₅₀ = 127 pM). SJ44236 induces ubiquitination and proteasomal degradation by forming a ternary complex with BET proteins and CRBN-DDB1. SJ44236 downregulates c-Myc, upregulates p53 and reduces cancer cell viability. SJ44236 can be used for the research of leukemia and medulloblastoma^[1]. (Pink: BET ligand (HY-78695); Blue: Cereblon ligand (HY-W890189); Black: linker (HY-W012935)).

IC₅₀ & Target^[1]

BRD4

127 pM (DC₅₀)

BRD2

BRD3

Cereblon

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle Epigenetic Reader Domain Isoform-spezifische Produkte anzeigen :

In Vitro

SJ44236 (1×10^-10 to 1×10² μM; 24 h) potently degrades BRD4 in HiBiT-BRD4 HEK293 LgBiT stable cells with a Dmax₅₀ of 0.19 nM, achieving 96.9% maximal degradation sustained for over 20 h with no impact on cell viability^[1].
SJ44236 (0.001-100 nM; 4 h) degrades endogenous BRD4 in MV4-11 cells with a DC₅₀ of 0.127 nM after 4 h of treatment, consistent with its potency in engineered HEK293 cells^[1].
SJ44236 (72 h) potently inhibits the proliferation of MV4-11 cells with an IC₅₀ of 0.12 nM and HD-MB03 cells with an IC₅₀ of 0.92 nM after 72 h of treatment^[1].
SJ44236 (100 nM; 4 h) induces over 90% degradation of BRD2, BRD3, and BRD4 in MV4-11 cells after 4 h of treatment at 100 nM, alongside expected downstream regulation of c-Myc (down) and p53 (up)^[1].

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

Parmacokinetics

Species	Dose	Route	C_max	T_max	Bioavailability	AUC_last	CL	T_1/2 (Elimination)	AUC	V_d
Mice^[1]	3 mg/kg	i.v.	/	/	/	/	8.85 mL/min/kg	3.4 h	5541 ng·h/mL	0.85 L/kg
Mice^[1]	10 mg/kg	p.o.	2436 ng/mL	0.5 h	45 %	8060 ng·h/mL	/	/	/	/

In Vivo

SJ44236 (3-10 mg/kg; i.v., p.o.; single dose) exhibits favorable in vivo pharmacokinetic properties in female CD1 mice, including 45% oral bioavailability, low clearance, and rapid oral absorption^[1].

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

Chemical Information

Molecular Weight 753.36
Formel C₄₀H₄₅ClN₈O₃S
SMILES

O=C(C[C@@H]1N=C(C2=C(N3C1=NN=C3C)SC(C)=C2C)C4=CC=C(Cl)C=C4)N5CCC(CC5)CN6CCN(C7=CC=C(C=C7)C8C(NC(CC8)=O)=O)CC6
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (271 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Actis M, et al. Evaluation of Cereblon-Directing Warheads for the Development of Orally Bioavailable PROTACs. J Med Chem. 2025;68(3):3591-3611. [Content Brief]

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

MOQ

Minimum order quantity

100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise

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Art. -Nr.:
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SJ44236

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle Epigenetic Reader Domain Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

SJ44236 Related Classifications

HY-170900 Related Classifications