Cat. No.: HY-170828

SMD-1087

SMD-1087 is a VHL-recruiting SMARCA2 PROTAC degrader with a DC₅₀ of 8 nM. SMD-1087 induces ubiquitination and degradation of SMARCA2 via the proteasome pathway. SMD-1087 reduces PBRM1 protein levels, inhibits the growth of SMARCA4-deficient cancer cells, and suppresses tumor growth in mouse xenograft models. SMD-1087 can be used for research on SMARCA4-deficient human cancers, including lung cancer and melanoma.
(Pink: SMARCA2 ligand (HY-170817); Blue: VHL ligand (HY-112078); Black: linker (HY-W890392)).

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CAS No.: 3033586-04-5
Formule: C₅₆H₆₈ClN₇O₅S
Masse moléculaire:986.70

Stockage:

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

Data Sheet (285 KB)

SMD-1087 Chemical Structure

CAS No.: 3033586-04-5

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Use of MCE Products

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

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

Activité biologique

Description

SMD-1087 is a VHL-recruiting SMARCA2 PROTAC degrader with a DC₅₀ of 8 nM. SMD-1087 induces ubiquitination and degradation of SMARCA2 via the proteasome pathway. SMD-1087 reduces PBRM1 protein levels, inhibits the growth of SMARCA4-deficient cancer cells, and suppresses tumor growth in mouse xenograft models. SMD-1087 can be used for research on SMARCA4-deficient human cancers, including lung cancer and melanoma^[1]^[2]. (Pink: SMARCA2 ligand (HY-170817); Blue: VHL ligand (HY-112078); Black: linker (HY-W890392)).

IC₅₀ & Target

^[2]

SMARCA2

8 nM (DC₅₀)

PBRM1

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Cellular Effect

Cell Line	Type	Value	Description	References
HeLa	DC₅₀	8 nM	Degradation of SMARCA2 protein in HeLa cells genetically modified to express SMARCA2-HiBiT assessed via Nano-Glo HiBiT Lytic Detection Assay after 24 h incubation. Degradation of SMARCA2 protein in HeLa cells genetically modified to express SMARCA2-HiBiT assessed via Nano-Glo HiBiT Lytic Detection Assay after 24 h incubation.	39745064
HeLa	DC₅₀	> 10000 nM	Degradation of SMARCA4 protein in HeLa cells genetically modified to express SMARCA4-HiBiT assessed via Nano-Glo HiBiT Lytic Detection Assay after 24 h incubation. Degradation of SMARCA4 protein in HeLa cells genetically modified to express SMARCA4-HiBiT assessed via Nano-Glo HiBiT Lytic Detection Assay after 24 h incubation.	39745064
HeLa	DC₅₀	142 nM	Degradation of SMARCA2 protein in HeLa cells genetically modified to express SMARCA2-HiBiT assessed via Nano-Glo HiBiT Lytic Detection Assay after 4 h incubation. Degradation of SMARCA2 protein in HeLa cells genetically modified to express SMARCA2-HiBiT assessed via Nano-Glo HiBiT Lytic Detection Assay after 4 h incubation.	39745064
HeLa	DC₅₀	89 nM	Degradation of SMARCA2 protein in HeLa cells genetically modified to express SMARCA2-HiBiT assessed via Nano-Glo HiBiT Lytic Detection Assay after 8 h incubation. Degradation of SMARCA2 protein in HeLa cells genetically modified to express SMARCA2-HiBiT assessed via Nano-Glo HiBiT Lytic Detection Assay after 8 h incubation.	39745064
HeLa	DC₅₀	49 nM	Degradation of SMARCA2 protein in HeLa cells genetically modified to express SMARCA2-HiBiT assessed via Nano-Glo HiBiT Lytic Detection Assay after 24 h incubation. Degradation of SMARCA2 protein in HeLa cells genetically modified to express SMARCA2-HiBiT assessed via Nano-Glo HiBiT Lytic Detection Assay after 24 h incubation.	39745064
HeLa	DC₅₀	44 nM	Degradation of SMARCA2 protein in HeLa cells genetically modified to express SMARCA2-HiBiT assessed via Nano-Glo HiBiT Lytic Detection Assay after 48 h incubation. Degradation of SMARCA2 protein in HeLa cells genetically modified to express SMARCA2-HiBiT assessed via Nano-Glo HiBiT Lytic Detection Assay after 48 h incubation.	39745064
HeLa	DC₅₀	> 1000 nM	Degradation of SMARCA4 protein in HeLa cells genetically modified to express SMARCA4-HiBiT assessed via Nano-Glo HiBiT Lytic Detection Assay after 4 to 48 h incubation. Degradation of SMARCA4 protein in HeLa cells genetically modified to express SMARCA4-HiBiT assessed via Nano-Glo HiBiT Lytic Detection Assay after 4 to 48 h incubation.	39745064
SK-MEL-5	DC₅₀	81.1 nM	Degradation of SMARCA2 protein in SK-Mel-5 SMARCA4 mutant melanoma cells assessed via Western blot after 24 h incubation. Degradation of SMARCA2 protein in SK-Mel-5 SMARCA4 mutant melanoma cells assessed via Western blot after 24 h incubation.	39745064
NCI-H838	DC₅₀	76.2 nM	Degradation of SMARCA2 protein in H838 SMARCA4 mutant lung cancer cells assessed via Western blot after 24 h incubation. Degradation of SMARCA2 protein in H838 SMARCA4 mutant lung cancer cells assessed via Western blot after 24 h incubation.	39745064
NCI-H1792	DC₅₀	100 nM	Degradation of PBRM1 protein in H1792 SMARCA4 wild-type cells assessed via Western blot after 24 h incubation. Degradation of PBRM1 protein in H1792 SMARCA4 wild-type cells assessed via Western blot after 24 h incubation.	39745064
NCI-H1792	GI₅₀	> 1000 nM	Cell growth inhibition in H1792 SMARCA2/4 wild-type cancer cells assessed via cell viability measurement after 7-day incubation. Cell growth inhibition in H1792 SMARCA2/4 wild-type cancer cells assessed via cell viability measurement after 7-day incubation.	39745064
SK-MEL-28	GI₅₀	> 1000 nM	Cell growth inhibition in SK-Mel-28 SMARCA2/4 wild-type cancer cells assessed via cell viability measurement after 7-day incubation. Cell growth inhibition in SK-Mel-28 SMARCA2/4 wild-type cancer cells assessed via cell viability measurement after 7-day incubation.	39745064
NCI-H838	GI₅₀	142 nM	Cell growth inhibition in H838 SMARCA4 deficient cancer cells assessed via cell viability measurement after 7-day incubation. Cell growth inhibition in H838 SMARCA4 deficient cancer cells assessed via cell viability measurement after 7-day incubation.	39745064
SK-MEL-5	GI₅₀	22.3 nM	Cell growth inhibition in SK-Mel-5 SMARCA4 deficient cancer cells assessed via cell viability measurement after 7-day incubation. Cell growth inhibition in SK-Mel-5 SMARCA4 deficient cancer cells assessed via cell viability measurement after 7-day incubation.	39745064

In Vitro

SMD-1087 potently degrades SMARCA2 with a DC₅₀ of 6-13 nM and 88-92% maximum degradation, while being > 1000-fold selective over SMARCA4^[1].
SMD-1087 (24 h) potently and selectively degrades SMARCA2 (DC₅₀ = 8 nM, Dmax = 89%) over SMARCA4 (DC₅₀ > 10,000 nM, Dmax = 20%) in modified HeLa cells after 24 h treatment, with > 1,250-fold selectivity^[2].
SMD-1087 (4-48 h) induces time-dependent degradation of SMARCA2 in modified HeLa cells, with increasing potency and efficiency over 4 to 24 h, while showing minimal activity against SMARCA4 across all tested treatment durations^[2].
SMD-1087 (0.01-1000 nM; 24 h) dose-dependently degrades SMARCA2 but not SMARCA4 in H1792 SMARCA4 wild-type cells after 24 h treatment^[2].
SMD-1087 (0.01-1000 nM; 24 h) potently degrades SMARCA2 (DC₅₀ = 81.1 nM, D_max = 87%) in SK-Mel-5 SMARCA4^G12C mutant cells after 24 h treatment^[2].
SMD-1087 (0.01-1000 nM; 24 h) potently degrades SMARCA2 (DC₅₀ = 76.2 nM, D_max = 89%) in H838 SMARCA4 mutant cells after 24 h treatment^[2].
SMD-1087 (up to 1 μM; 24 h) degrades PBRM1 (DC₅₀ ~100 nM, D_max = 62% at 1 μM) in H1792 SMARCA4 wild-type cells after 24 h treatment^[2].
SMD-1087 (0.1-1000 nM; 24 h) induces partial PBRM1 protein degradation in H1792 cells at concentrations of 10 nM and above after 24-hour incubation, with maximum degradation observed at 1000 nM.
SMD-1087 (up to 1 μM; 7 days) does not inhibit cell growth in H1792 and SK-Mel-28 SMARCA2/4 wild-type cell lines after 7-day treatment at concentrations up to 1 μM^[2].
SMD-1087 (up to 1 μM; 7 days) potently inhibits cell growth in SMARCA4 deficient H838 (GI₅₀ = 142 nM, I_max = 79%) and SK-Mel-5 (GI₅₀ = 22.3 nM, I_max = 93%) cell lines after 7-day treatment^[2].

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

Western Blot Analysis^[2]

Cell Line:

H1792 SMARCA4 wild-type cells
Concentration:

0.01, 0.03, 0.1, 0.3, 1, 3, 10, 30, 100, 300, 1000 nM
Incubation Time:

24 h
Result:

Degraded SMARCA2 in a dose-dependent manner.
Showed minimal degradation of SMARCA4 even at the highest tested concentration.

Western Blot Analysis^[2]

Cell Line:

SK-Mel-5 SMARCA4 mutant melanoma cells
Concentration:

0.01, 0.03, 0.1, 0.3, 1, 3, 10, 30, 100, 300, 1000 nM
Incubation Time:

24 h
Result:

Potently degraded SMARCA2 with a DC₅₀ of 81.1 nM and a D_max of 87%.

Western Blot Analysis^[2]

Cell Line:

H838 SMARCA4 mutant lung cancer cells
Concentration:

0.001, 0.01, 0.1, 1, 10, 100, 1000 nM
Incubation Time:

24 h
Result:

Potently degraded SMARCA2 with a DC₅₀ of 76.2 nM and a D_max of 89%.

Western Blot Analysis^[2]

Cell Line:

H1792 SMARCA4 wild-type cells
Concentration:

0.1, 1, 10,100, 1000, 10000 nM
Incubation Time:

24 h
Result:

Degraded PBRM1 in a dose-dependent manner, with a DC₅₀ of ~100 nM and a D_max of 62% at 1 μM.

Cell Viability Assay^[2]

Cell Line:

H1792 and SK-Mel-28 SMARCA2/4 wild-type cancer cell lines
Concentration:

0.0001, 0.001, 0.01, 0.1, 1 μM
Incubation Time:

7 days
Result:

Showed no cell growth inhibition activity at concentrations up to 1 μM, with a GI₅₀ > 1000 nM and I_max of 0% in both cell lines.

Cell Viability Assay^[2]

Cell Line:

H838 and SK-Mel-5 SMARCA4 deficient cancer cell lines
Concentration:

0.0001, 0.001, 0.01, 0.1, 1 μM
Incubation Time:

7 days
Result:

Inhibited cell growth in a dose-dependent manner: in H838 cells, GI₅₀ = 142 nM with an I_max of 79%; in SK-Mel-5 cells, GI₅₀ = 22.3 nM with an I_max of 93%.

Western Blot Analysis^[2]

Cell Line:

H1792 cells
Concentration:

0.1, 1, 10, 100, 1000 nM
Incubation Time:

24 h
Result:

Reduced PBRM1 protein levels.

Chemical Information

CAS No. 3033586-04-5
Masse moléculaire 986.70
Formule C₅₆H₆₈ClN₇O₅S
SMILES

C[C@H](NC([C@@H]1C[C@H](CN1C([C@@H](NC([C@@H]2CC[C@H](CC2)CN3CCC(CC3)C4=CC(N5C6=C7C(Cl)=CC=C6)=C(C=C4)C8(CCCCC8)C5=NC7=O)=O)C(C)(C)C)=O)O)=O)C9=CC=C(C=C9)C%10=C(C)N=CS%10
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (285 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]. Yang L, et al. Discovery of SMD-3236: A Potent, Highly Selective and Efficacious SMARCA2 Degrader for the Treatment of SMARC4-Deficient Human Cancers. Journal of medicinal chemistry. 2025 Jan 23;68(2):1155-1178. [Content Brief]

[2]. Leng L, et al. Discovery of High-Affinity SMARCA2/4 Bromodomain Ligands and Development of Potent and Exceptionally Selective SMARCA2 PROTAC Degraders. Journal of medicinal chemistry. 2025 Jan 23;68(2):1113-1133. [Content Brief]

Calculators

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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.

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SMD-1087

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