Cat. No.: HY-161101

GSPT1 degrader-19

Name: GSPT1 degrader-19
Brand: MedChemExpress
SKU: HY-161101
Price: 294.00 USD
Availability: InStock
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GSPT1 degrader-19 is a molecular glue degrader targeting GSPT1, IKZF1 and IKZF3, with DC₅₀ values of 0.88 nM, 11.54 nM and 13.84 nM, respectively, in MM.1S multiple myeloma cells. GSPT1 degrader-19 induces cereblon (CRBN)-dependent ubiquitination and proteasomal degradation of IKZF1, IKZF3, GSPT1 and GSPT2, and also reduces ZFP91 protein levels via a CRBN-dependent pathway. GSPT1 degrader-19 exerts antiproliferative effects on cancer cells, induces global proteomic changes including downregulation of novel substrates, and exhibits activity against multiple myeloma and leukemia cell lines. GSPT1 degrader-19 can be used in research related to multiple myeloma and leukemia.

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Pureté : 99.30%
Formule: C₃₁H₃₇N₅O₇
Masse moléculaire:591.65

Stockage:

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

GSPT1 degrader-19 Chemical Structure

Size

Prix

Stock

Quantité

Amount: USD 0.00

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Solvant et solubilité
- In Vitro
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

^[1]

eRF3a/GSPT1

0.88 nM (DC₅₀)

IKZF1

11.54 nM (DC₅₀)

IKZF3

13.84 nM (DC₅₀)

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Cellular Effect

Cell Line	Type	Value	Description	References
MM.1S	EC50	11.08 nM	Antiproliferative activity against human MM.1S multiple myeloma cells assessed as reduction in cell viability incubated for 96 hrs by CellTiterGlo® Luminescent Cell Viability Assay. Antiproliferative activity against human MM.1S multiple myeloma cells assessed as reduction in cell viability incubated for 96 hrs by CellTiterGlo® Luminescent Cell Viability Assay.	38114468
NCI-H929	EC50	1.485 nM	Antiproliferative activity against human NCI-H929 multiple myeloma cells assessed as reduction in cell viability incubated for 96 hrs by CellTiterGlo® Luminescent Cell Viability Assay. Antiproliferative activity against human NCI-H929 multiple myeloma cells assessed as reduction in cell viability incubated for 96 hrs by CellTiterGlo® Luminescent Cell Viability Assay.	38114468

In Vitro

GSPT1 degrader-19 (E14) (96 h) potently inhibits MM.1S and NCI-H929 multiple myeloma cell proliferation with EC₅₀ values of 11.08 nM and 1.485 nM, respectively^[1].
GSPT1 degrader-19 (1-10 μM; 96 h) potently inhibits HEL and K562 human leukemia cell viability^[1].
GSPT1 degrader-19 (1-10 μM; 96 h) inhibits Nalm-6 cell viability, with near-complete inhibition at 10.0 μM after 96 h incubation^[1].
GSPT1 degrader-19 (1-10 μM; 18 h) induces CRBN-dependent degradation of IKZF1, IKZF3, and GSPT1 in MM.1S multiple myeloma cells^[1].
GSPT1 degrader-19 (16 h) potently induces CRBN-dependent degradation of GSPT1 (DC₅₀ = 0.88 nM), IKZF1 (DC₅₀ = 11.54 nM), and IKZF3 (DC₅₀ = 13.84 nM) in MM.1S multiple myeloma cells^[1].
GSPT1 degrader-19 (1.0 μM; 18 h) potently downregulates IKZF3, GSPT1, and GSPT2, and significantly decreases ZFP91 and IKZF1 levels in MM.1S multiple myeloma cells^[1].
GSPT1 degrader-19 (1-10 μM; 96 h) exerts anti-proliferative activity in MM.1S multiple myeloma cells in a CRBN-dependent manner, as activity is abolished in CRBN knockout cells^[1].
GSPT1 degrader-19 (0.1-1.0 μM; 18 h) induces neosubstrate degradation in MM.1S multiple myeloma cells in a CRBN-dependent manner, as no degradation of GSPT1, IKZF1, or IKZF3 is observed in CRBN knockout cells^[1].

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

Cell Viability Assay^[1]

Cell Line:

HEL human leukemia cells (IKZF1/3-independent)
Concentration:

1.0 μM, 10.0 μM
Incubation Time:

96 h
Result:

Reduced HEL cell viability to near 0% at both 1.0 μM and 10.0 μM after 96 h incubation.

Cell Viability Assay^[1]

Cell Line:

K562 human leukemia cells (IKZF1/3-independent)
Concentration:

1.0 μM, 10.0 μM
Incubation Time:

96 h
Result:

Reduced K562 cell viability to near 0% at 10.0 μM and to ~10% at 1.0 μM after 96 h incubation.

Cell Viability Assay^[1]

Cell Line:

Nalm-6 cells
Concentration:

1.0 μM, 10.0 μM
Incubation Time:

96 h
Result:

Reduced Nalm-6 cell viability to ~75% at 1.0 μM and to near 0% at 10.0 μM after 96 h incubation.

Western Blot Analysis^[1]

Cell Line:

MM.1S multiple myeloma cells
Concentration:

1.0 μM, 10.0 μM
Incubation Time:

18 h
Result:

Induced degradation of IKZF1, IKZF3, and GSPT1 at both 1.0 μM and 10.0 μM.

Western Blot Analysis^[1]

Cell Line:

MM.1S multiple myeloma cells
Concentration:

Serial concentrations
Incubation Time:

16 h
Result:

Induced degradation of GSPT1 with a DC₅₀ of 0.88 nM.
Induced degradation of IKZF1 with a DC₅₀ of 11.54 nM.
Induced degradation of IKZF3 with a DC₅₀ of 13.84 nM.

Cell Viability Assay^[1]

Cell Line:

CRBN knockout MM.1S multiple myeloma cells
Concentration:

1.0 μM, 10.0 μM
Incubation Time:

96 h
Result:

Completely abolished anti-proliferative activity, with cell viability remaining near 100% at both concentrations.

Western Blot Analysis^[1]

Cell Line:

CRBN knockout MM.1S multiple myeloma cells
Concentration:

0.1 μM, 1.0 μM
Incubation Time:

18 h
Result:

Failed to induce degradation of GSPT1, IKZF1, or IKZF3, with protein levels remaining similar to DMSO-treated controls.

Chemical Information

Appearance Solid
Masse moléculaire 591.65
Formule C₃₁H₃₇N₅O₇
Color Light yellow to yellow
SMILES

O=C1N(C2CCC(NC2=O)=O)C(C3=C(NCCCCNC(C(C4=CC=CC(OC)=C4)N(CC(C)C)C=O)=O)C=CC=C31)=O
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

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

Solvant et solubilité

In Vitro:

DMSO : 125 mg/mL (211.27 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

1.6902 mL

8.4509 mL

16.9019 mL

5 mM

0.3380 mL

1.6902 mL

3.3804 mL

10 mM

0.1690 mL

0.8451 mL

1.6902 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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (287 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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)
Instruction de manipulation (2659 KB)

Références

[1]. Wang Z, et al. Direct-to-biology, automated, nano-scale synthesis, and phenotypic screening-enabled E3 ligase modulator discovery. Nature communications. 2023 Dec 19;14(1):8437. [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	1.6902 mL	8.4509 mL	16.9019 mL	42.2547 mL
	5 mM	0.3380 mL	1.6902 mL	3.3804 mL	8.4509 mL
	10 mM	0.1690 mL	0.8451 mL	1.6902 mL	4.2255 mL
	15 mM	0.1127 mL	0.5634 mL	1.1268 mL	2.8170 mL
	20 mM	0.0845 mL	0.4225 mL	0.8451 mL	2.1127 mL
	25 mM	0.0676 mL	0.3380 mL	0.6761 mL	1.6902 mL
	30 mM	0.0563 mL	0.2817 mL	0.5634 mL	1.4085 mL
	40 mM	0.0423 mL	0.2113 mL	0.4225 mL	1.0564 mL
	50 mM	0.0338 mL	0.1690 mL	0.3380 mL	0.8451 mL
	60 mM	0.0282 mL	0.1408 mL	0.2817 mL	0.7042 mL
	80 mM	0.0211 mL	0.1056 mL	0.2113 mL	0.5282 mL
	100 mM	0.0169 mL	0.0845 mL	0.1690 mL	0.4225 mL

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GSPT1 degrader-19

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