2. PROTAC Epigenetics
  3. PROTACs Epigenetic Reader Domain
  4. SMD-3040

SMD-3040 is a potent and selective SMARCA2 PROTAC degrader (DC50: 12 nM; Dmax: 91%). SMD-3040 can inhibit tumor cell proliferation and exhibits antitumor activity. SMD-3040 can be used in the study of tumors such as melanoma. (SMARCA2/4-ligand (HY-171765); HY-112078 VHL ligand (HY-112078))

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SMD-3040 Chemical Structure

SMD-3040 Chemical Structure

CAS No. : 3033109-92-8

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Based on 1 publication(s) in Google Scholar

Other Forms of SMD-3040:

SMD-3040 Related Antibodies

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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Description

SMD-3040 is a potent and selective SMARCA2 PROTAC degrader (DC50: 12 nM; Dmax: 91%). SMD-3040 can inhibit tumor cell proliferation and exhibits antitumor activity. SMD-3040 can be used in the study of tumors such as melanoma[1]. (SMARCA2/4-ligand (HY-171765); HY-112078 VHL ligand (HY-112078))

In Vitro

SMD-3040 (0-1 μM; 1-48 h) can effectively degrade SMARCA2 in cells such as Hela, SK-Mel-5 and SK-Mel-28[1].
SMD-3040 (7 days) significantly inhibits cell growth in SMARCA4-deficient cancer cell lines (such as SK-Mel-5, H838, A549, etc.) with GI50 of 8.8-119 nM[1].

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

SMD-3040 Related Antibodies

Western Blot Analysis[1]

Cell Line: SK-Mel-5 and SK-Mel-28 cells
Concentration: 0.01, 0.03, 0.1, 0.3, 1, 3, 10, 30, 100, 300 and 1000 nM
Incubation Time: 24 h
Result: Inhibited the level of SMARCA2.
Had DC50 values of 20 and 35 nM in K-Mel-5 and SK-Mel-28 cells.
In Vivo

SMD-3040 (25-50 mg/kg; intravenous injection; twice weekly; two weeks) exhibits antitumor activity in a xenograft mouse model of human melanoma[1].

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

Animal Model: Xenograft mouse models treated SK-Mel-5 melanoma cell line carrying SMARCA4 gene deletion[1]
Dosage: 25 and 50 mg/kg
Administration: Intravenous injection; twice weekly; two weeks
Result: Effectively inhibited tumor growth in two different smarca4-deficient xenograft models.
Was well-tolerated in mice.
Molecular Weight

943.21

Formula

C52H66N10O5S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N[C@H](C(N1[C@H](C(N[C@H](C2=CC=C(C3=C(C)N=CS3)C=C2)C)=O)C[C@@H](O)C1)=O)C(C)(C)C)[C@H]4CC[C@H](CN5CC6(CCC(N7N=CC(C8=C(N)N=NC(C9=C(O)C=CC=C9)=C8)=C7)CC6)C5)CC4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (106.02 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.0602 mL 5.3010 mL 10.6021 mL
5 mM 0.2120 mL 1.0602 mL 2.1204 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. 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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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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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. 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 1.0602 mL 5.3010 mL 10.6021 mL 26.5052 mL
5 mM 0.2120 mL 1.0602 mL 2.1204 mL 5.3010 mL
10 mM 0.1060 mL 0.5301 mL 1.0602 mL 2.6505 mL
15 mM 0.0707 mL 0.3534 mL 0.7068 mL 1.7670 mL
20 mM 0.0530 mL 0.2651 mL 0.5301 mL 1.3253 mL
25 mM 0.0424 mL 0.2120 mL 0.4241 mL 1.0602 mL
30 mM 0.0353 mL 0.1767 mL 0.3534 mL 0.8835 mL
40 mM 0.0265 mL 0.1325 mL 0.2651 mL 0.6626 mL
50 mM 0.0212 mL 0.1060 mL 0.2120 mL 0.5301 mL
60 mM 0.0177 mL 0.0884 mL 0.1767 mL 0.4418 mL
80 mM 0.0133 mL 0.0663 mL 0.1325 mL 0.3313 mL
100 mM 0.0106 mL 0.0530 mL 0.1060 mL 0.2651 mL
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SMD-3040 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:

SMD-30403033109-92-8SMD3040SMD 3040PROTACsEpigenetic Reader DomainSMARCA2SMARCA4xenograft modelsPROTAC degraderSK-Mel-5H838A549Inhibitorinhibitorinhibit

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