Art. -Nr.: HY-132199

SJ6986

Name: SJ6986
Brand: MedChemExpress
SKU: HY-132199
Price: 60.00 USD
Availability: InStock
Rating: 5 (1 reviews)

1 Cited Publications

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SJ6986 is an orally active GSPT1/2 molecular glue degrader, with a DC₅₀ of 9.7 nM at 4 h and 2.1 nM at 24 h for GSPT1 degradation in MV4-11 cells. SJ6986 recruits GSPT1/2 to the CRBN E3 ligase complex, inducing ubiquitination and proteasomal degradation of GSPT1/2. SJ6986 triggers activation of the integrated stress response pathway and apoptosis downstream of GSPT1 degradation. SJ6986 serves as a chemical probe for investigating the functions of GSPT1/GSPT2 in vitro and in vivo. SJ6986 can be used for research on acute leukemia and medulloblastoma.

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Reinheit: 98.35%
CAS. Nr.: 2765625-93-0
Formel: C₂₀H₁₄F₃N₃O₇S
Molecular Weight:497.40

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

SJ6986 Chemical Structure

CAS. Nr.: 2765625-93-0

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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
- Cellular Effect
- In Vitro
- Parmacokinetics
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

eRF3a/GSPT1

eRF3b/GSPT2

Alle Eukaryotic Release Factor (eRF) Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
MV4-11	EC50	1.5 nM	Antiproliferative activity against human MV4-11 (KMT2A-rearranged acute myeloid leukemia) cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent assay. Antiproliferative activity against human MV4-11 (KMT2A-rearranged acute myeloid leukemia) cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent assay.	34042448
MHH-CALL-4	EC50	0.4 nM	Antiproliferative activity against human MHH-CALL-4 (CRLF2-rearranged JAK2-mutated acute lymphoblastic leukemia) cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent assay. Antiproliferative activity against human MHH-CALL-4 (CRLF2-rearranged JAK2-mutated acute lymphoblastic leukemia) cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent assay.	34042448
MB002 cell	EC50	726 nM	Antiproliferative activity against human MB002 (TP53-mutated Group 3 medulloblastoma) cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent assay. Antiproliferative activity against human MB002 (TP53-mutated Group 3 medulloblastoma) cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent assay.	34042448
MB004 cell	EC50	336 nM	Antiproliferative activity against human MB004 (TP53-mutated Group 3 medulloblastoma) cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent assay. Antiproliferative activity against human MB004 (TP53-mutated Group 3 medulloblastoma) cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent assay.	34042448
HD-MB03	EC50	3583 nM	Antiproliferative activity against human HD-MB03 (TP53 wild-type Group 3 medulloblastoma) cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent assay. Antiproliferative activity against human HD-MB03 (TP53 wild-type Group 3 medulloblastoma) cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent assay.	34042448
MV4-11	DC₅₀	9.7 nM	Induction of GSPT1 protein degradation in human MV4-11 cells incubated for 4 hrs, measured by immunoblot analysis. Induction of GSPT1 protein degradation in human MV4-11 cells incubated for 4 hrs, measured by immunoblot analysis.	34042448
MV4-11	DC₅₀	2.1 nM	Induction of GSPT1 protein degradation in human MV4-11 cells incubated for 24 hrs, measured by immunoblot analysis. Induction of GSPT1 protein degradation in human MV4-11 cells incubated for 24 hrs, measured by immunoblot analysis.	34042448
MV4-11	DC₅₀	30 nM	Induction of IKZF1 protein degradation in human MV4-11 cells incubated for 24 hrs, measured by immunoblot analysis. Induction of IKZF1 protein degradation in human MV4-11 cells incubated for 24 hrs, measured by immunoblot analysis.	34042448
MHH-CALL-4	DC₅₀	15 nM	Induction of GSPT1 protein degradation in human MHH-CALL-4 cells incubated for 4 hrs, measured by immunoblot analysis. Induction of GSPT1 protein degradation in human MHH-CALL-4 cells incubated for 4 hrs, measured by immunoblot analysis.	34042448
MHH-CALL-4	DC₅₀	3.5 nM	Induction of GSPT1 protein degradation in human MHH-CALL-4 cells incubated for 24 hrs, measured by immunoblot analysis. Induction of GSPT1 protein degradation in human MHH-CALL-4 cells incubated for 24 hrs, measured by immunoblot analysis.	34042448
MHH-CALL-4	DC₅₀	117 nM	Induction of IKZF1 protein degradation in human MHH-CALL-4 cells incubated for 24 hrs, measured by immunoblot analysis. Induction of IKZF1 protein degradation in human MHH-CALL-4 cells incubated for 24 hrs, measured by immunoblot analysis.	34042448
HEK-293T	EC50	0.1 nM	Induction of HiBit-tagged GSPT1 protein degradation in human HEK293T cells incubated for 4 hrs, measured by Nano-Glo HiBiT lytic detection system. Induction of HiBit-tagged GSPT1 protein degradation in human HEK293T cells incubated for 4 hrs, measured by Nano-Glo HiBiT lytic detection system.	34042448

In Vitro

SJ6986 (Compound 6) inhibits the proliferation of MV4-11, MHH-CALL-4, MB002, MB004 and HD-MB03 cells after 72 h, with EC₅₀ values of 1.5, 0.4, 726, 336 and 3583 nM^[1].
SJ6986 (0.001-10 μM; 4 h, 24 h) rapidly degrades GSPT1 in MV4-11 cells, with a DC₅₀ of 9.7 nM at 4 h and 2.1 nM at 24 h; it also induces delayed and less potent degradation of IKZF1, with a DC₅₀ of 30 nM at 24 h^[1].
SJ6986 (0.001-10 μM; 4 h, 24 h) rapidly degrades GSPT1 in MHH-CALL-4 cells, with a DC₅₀ of 15 nM at 4 h and 3.5 nM at 24 h; it also induces delayed and weak degradation of IKZF1, with a DC₅₀ of 117 nM at 24 h^[1].
The antiproliferative activity of SJ6986 (72 h) in MV4-11 cells is completely dependent on the degradation of GSPT1^[1].
SJ6986 (1 μM; 4 h) selectively degrades GSPT1 and GSPT2 in MV4-11 cells^[1].
SJ6986 (1 h) potently binds to the CRBN-DDB1 complex in a cell-free competitive fluorescence polarization assay, with an IC₅₀ of 15 nM^[1].
SJ6986 (4 h) efficiently degrades HiBit-tagged GSPT1 in HEK293T cells, with an EC₅₀ of 0.1 nM after 4 h of incubation^[1].

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

Western Blot Analysis^[1]

Cell Line:

MV4-11 cells
Concentration:

0.001, .01, 0.1, 1, 10 μM
Incubation Time:

4 h; 24 h
Result:

Induced dose-dependent GSPT1 degradation with a DC₅₀ of 9.7 nM and 90% maximal degradation at 100 nM after 4 h.
Did not significantly reduce IKZF1 levels after 4 h.
Induced GSPT1 degradation with a DC₅₀ of 2.1 nM and nearly complete degradation after 24 h.
Induced IKZF1 degradation with a DC₅₀ of 30 nM after 24 h.

Western Blot Analysis^[1]

Cell Line:

MHH-CALL-4 cells
Concentration:

0.001, .01, 0.1, 1, 10 μM
Incubation Time:

4 h; 24 h
Result:

Induced dose-dependent GSPT1 degradation with a DC₅₀ of 15 nM after 4 h.
Did not significantly reduce IKZF1 levels after 4 h.
Induced GSPT1 degradation with a DC₅₀ of 3.5 nM and nearly complete degradation after 24 h.
Induced IKZF1 degradation with a DC₅₀ of 117 nM and maximal degradation less than 50% after 24 h.

Parmacokinetics

Species	Dose	Route	T_max	C₀/C_max	F	T_1/2	CL	V_ss
Mice^[1]	3 mg/kg	i.v.	/	47.16 μg/mL	/	3.44 h	0.46 mL/min/kg	0.15 L/kg
Mice^[1]	10 mg/kg	p.o.	0.25 h	31.66 μg/mL	84 %	/	/	/

Chemical Information

CAS. Nr. 2765625-93-0
Appearance Solid
Molecular Weight 497.40
Formel C₂₀H₁₄F₃N₃O₇S
Color White to yellow
SMILES

O=S(C1=CC=CC=C1OC(F)(F)F)(NC2=CC3=C(C(N(C(CC4)C(NC4=O)=O)C3=O)=O)C=C2)=O
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (1)

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Leukemia

Targeting of IRAK4 and GSPT1 enhances therapeutic efficacy in AML via c-Myc destabilization. [Abstract]

2025 Sep;39(9):2163-2173. PMID: 40670672

SJ6986 purchased from MedChemExpress. Usage Cited in: Leukemia. 2025 Sep;39(9):2163-2173. [Abstract]

Immunoblots for c-MYC and GSPT1 in THP1 and HL60 cells cultured with CA-4948 (10 µM) or vehicle for 14 days and then treated with the indicated GSPT1 degraders (SJ6986; 10 µM; CC-885, 0.5 nM) for 24 h.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (201.05 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0105 mL

10.0523 mL

20.1045 mL

5 mM

0.4021 mL

2.0105 mL

4.0209 mL

10 mM

0.2010 mL

1.0052 mL

2.0105 mL

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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (5.03 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (290 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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]. Nishiguchi G, et al. Identification of Potent, Selective, and Orally Bioavailable Small-Molecule GSPT1/2 Degraders from a Focused Library of Cereblon Modulators. Journal of medicinal chemistry. 2021 Jun 10;64(11):7296-7311. [Content Brief]

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.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. 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	2.0105 mL	10.0523 mL	20.1045 mL	50.2614 mL
	5 mM	0.4021 mL	2.0105 mL	4.0209 mL	10.0523 mL
	10 mM	0.2010 mL	1.0052 mL	2.0105 mL	5.0261 mL
	15 mM	0.1340 mL	0.6702 mL	1.3403 mL	3.3508 mL
	20 mM	0.1005 mL	0.5026 mL	1.0052 mL	2.5131 mL
	25 mM	0.0804 mL	0.4021 mL	0.8042 mL	2.0105 mL
	30 mM	0.0670 mL	0.3351 mL	0.6702 mL	1.6754 mL
	40 mM	0.0503 mL	0.2513 mL	0.5026 mL	1.2565 mL
	50 mM	0.0402 mL	0.2010 mL	0.4021 mL	1.0052 mL
	60 mM	0.0335 mL	0.1675 mL	0.3351 mL	0.8377 mL
	80 mM	0.0251 mL	0.1257 mL	0.2513 mL	0.6283 mL
	100 mM	0.0201 mL	0.1005 mL	0.2010 mL	0.5026 mL

Bioz

SJ6986

1 Cited Publications

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SJ6986

Publications Citing Use of MedChemExpress (MCE) SJ6986

Alle Eukaryotic Release Factor (eRF) Isoform-spezifische Produkte anzeigen