2. PROTAC Epigenetics Apoptosis
  3. PROTACs Epigenetic Reader Domain Apoptosis
  4. PROTAC SMARCA2/4 degrader-38

PROTAC SMARCA2/4 degrader-38 is a degrader SMARCA2/4 PROTAC (DC50: 3.0 nM and 4.0 nM respectively). PROTAC SMARCA2/4 degrader-38 promotes the ubiquitination and degradation of SMARCA2/4. PROTAC SMARCA2/4 degrader-38 blocks the G0/G1 cell cycle and induces apoptosis. PROTAC SMARCA2/4 degrader-38 can be used in acute myeloid leukemia (AML) research. (Pink: SMARCA2/4 ligand; Blue: VHL ligand (HY-112078); Black: linker; Target Protein Ligand-Linker Conjugates (HY-173343)).

For research use only. We do not sell to patients.

PROTAC SMARCA2/4 degrader-38

PROTAC SMARCA2/4 degrader-38 Chemical Structure

CAS No. : 3081688-77-6

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

PROTAC SMARCA2/4 degrader-38 Related Antibodies

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Description

PROTAC SMARCA2/4 degrader-38 is a degrader SMARCA2/4 PROTAC (DC50: 3.0 nM and 4.0 nM respectively). PROTAC SMARCA2/4 degrader-38 promotes the ubiquitination and degradation of SMARCA2/4. PROTAC SMARCA2/4 degrader-38 blocks the G0/G1 cell cycle and induces apoptosis. PROTAC SMARCA2/4 degrader-38 can be used in acute myeloid leukemia (AML) research. (Pink: SMARCA2/4 ligand; Blue: VHL ligand (HY-112078); Black: linker; Target Protein Ligand-Linker Conjugates (HY-173343))[1].

IC50 & Target[1]

SMARCA2

3.0 nM (DC50)

SMARCA4

4.0 nM (DC50)

VHL

 

In Vitro

PROTAC SMARCA2/4 degrader-38 (Compound A11) (25-100 nM, 3 d) inhibits the proliferation activity of MV-4-11 cell lines (IC50: 4.9 nM) and MOLM-13 cell lines (IC50: 23.3 nM) in AML cells, and SU-DHL-4 (IC50: 87.7 nM) and WSU-DLCL-2 (IC50: 336.7 nM) in diffuse large B-cell lymphoma[1].
PROTAC SMARCA2/4 degrader-38 (100-1000 nM, 48 h) induces cell cycle arrest at G0/G1 phase in MV-4-11 and MOLM-13 cells in a concentration-dependent manner[1].
PROTAC SMARCA2/4 degrader-38 (100-1000 nM, 72 h) induces apoptosis in MV-4-11 and MOLM-13 cells[1].
PROTAC SMARCA2/4 degrader-38 (11.1-1000 nM, 24 h) inhibits the transcriptional expression of AML oncogenes in a concentration-dependent manner[1].

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

PROTAC SMARCA2/4 degrader-38 Related Antibodies

Cell Cycle Analysis[1]

Cell Line: MV-4-11 cells and MOLM-13 cells
Concentration: 100 nM, 300 nM and 1000 nM
Incubation Time: 48 h
Result: Induced a large accumulation of G0/G1 cells in MV-4-11 and MOLM-13 cells.

Apoptosis Analysis[1]

Cell Line: MV-4-11 cells and MOLM-13 cells
Concentration: 100 nM, 300 nM and 1000 nM
Incubation Time: 72 h
Result: Induced apoptosis in MV-4-11 and MOLM-13 cells.

Western Blot Analysis[1]

Cell Line: MOLM-13 cells; MV-4-11 cells
Concentration: 100 nM, 300 nM and 1000 nM; 11.1 nM, 33.3 nM, 100 nM, 300 nM and 1000 nM
Incubation Time: 72 h; 24 h
Result: Up-regulated apoptosis-related cleaved poly ADP-ribose polymerase (PARP) and cleaved caspase-3 proteins levels.
Down-regulated MYC protein level.

RT-PCR[1]

Cell Line: MV-4-11 cells
Concentration: 11.1 nM, 33.3 nM, 100 nM, 300 nM and 1000 nM
Incubation Time: 24 h
Result: Down-regulated the expression of E2F1, CDC25A, TRAP1, PU. 1, CD44 and BCL-2 genes.
Parmacokinetics
Species Dose Route Plasma Concentration Tmax T1/2 AUC MRT Bioavailability
Rat 1 mg/kg i.v. 1953 ng/mL 0.033 h 1.91 h 358 ng·h/mL 0.70 h /
Rat 10 mg/kg p.o. 6.41 ng/mL 0.42 h 2.10 h 8.22 ng·h/mL 0.81 h 0.62 %
Molecular Weight

773.94

Formula

C43H47N7O5S
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C([C@H]1N(C([C@@H](NC(C2(C3=CC=C(C4=CC(C5=CC=CC=C5O)=NN=C4N)C=C3)CC2)=O)C(C)(C)C)=O)C[C@H](O)C1)N[C@H](C6=CC=C(C7=C(C)N=CS7)C=C6)C
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 (129.21 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.2921 mL 6.4604 mL 12.9209 mL
5 mM 0.2584 mL 1.2921 mL 2.5842 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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In Vivo Dissolution Calculator
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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 1.2921 mL 6.4604 mL 12.9209 mL 32.3022 mL
5 mM 0.2584 mL 1.2921 mL 2.5842 mL 6.4604 mL
10 mM 0.1292 mL 0.6460 mL 1.2921 mL 3.2302 mL
15 mM 0.0861 mL 0.4307 mL 0.8614 mL 2.1535 mL
20 mM 0.0646 mL 0.3230 mL 0.6460 mL 1.6151 mL
25 mM 0.0517 mL 0.2584 mL 0.5168 mL 1.2921 mL
30 mM 0.0431 mL 0.2153 mL 0.4307 mL 1.0767 mL
40 mM 0.0323 mL 0.1615 mL 0.3230 mL 0.8076 mL
50 mM 0.0258 mL 0.1292 mL 0.2584 mL 0.6460 mL
60 mM 0.0215 mL 0.1077 mL 0.2153 mL 0.5384 mL
80 mM 0.0162 mL 0.0808 mL 0.1615 mL 0.4038 mL
100 mM 0.0129 mL 0.0646 mL 0.1292 mL 0.3230 mL
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PROTAC SMARCA2/4 degrader-38 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:

PROTAC SMARCA2/4 degrader-383081688-77-6PROTACsEpigenetic Reader DomainApoptosisAnticancerMV-4-11MOLM-13SU-DHL-4WSU-DLCL-2AMLInhibitorinhibitorinhibit

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