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Cat. No.: HY-131188

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PROTAC Bcl-xL degrader-1

PROTAC Bcl-xL degrader-1 is a PROTAC that comprises a Bcl-xL (Bcl-2 family member) ligand binding group, a linker and an IAP E3 ligases binding group. PROTAC Bcl-xL degrader-1 is a potent Bcl-xL degrader, and shows toxicity for human platelets and MyLa 1929 cells with IC₅₀ values of 62 nM and 8.5 μM, respectively.
(Pink: Bcl-xL ligand (HY-44432); Blue: IAP ligand (HY-184595); Black: linker).

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

CAS No.: 2450351-07-0
Formula: C₇₆H₉₆ClF₃N₁₀O₁₁S₃
Molecular Weight:1514.28

Storage:

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

Data Sheet (266 KB)

PROTAC Bcl-xL degrader-1 Chemical Structure

CAS No.: 2450351-07-0

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Use of MCE Products

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

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Protocols (1)
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

PROTAC Bcl-xL degrader-1 is a PROTAC that comprises a Bcl-xL (Bcl-2 family member) ligand binding group, a linker and an IAP E3 ligases binding group. PROTAC Bcl-xL degrader-1 is a potent Bcl-xL degrader, and shows toxicity for human platelets and MyLa 1929 cells with IC₅₀ values of 62 nM and 8.5 μM, respectively^[1]. (Pink: Bcl-xL ligand (HY-44432); Blue: IAP ligand (HY-184595); Black: linker).

IC₅₀ & Target

^[1]

cIAP1

Bcl-xL

All PROTACs Isoforms :

All Bcl-2 Family Isoforms :

In Vitro

PROTAC Bcl-xL degrader-1 (Compound 8a; 0.01-3 μM; 16 hours; MyLa 1929 cells) treatment potently and dose-dependently induces BCL-XL degradation in MyLa 1929 cells^[1].
PROTAC Bcl-xL degrader-1 (Compound 8a) is able to induce remarkable BCL-XL degradation in a dose-dependent manner across all tested cell lines (A549, MDA-MB-231, SW620, MeWo, SK-MEL28, and CHL-1 cell lines), suggesting the broad application across cancer types^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.

Western Blot Analysis^[1]

View Protocol

Cell Line:

MyLa 1929 cells
Concentration:

0.01 μM, 0.03 μM, 0.1 μM, 0.3 μM, 1 μM, 3 μM
Incubation Time:

16 hours
Result:

Potently and dose-dependently induced BCL-XL degradation in MyLa 1929 cells.

Chemical Information

CAS No. 2450351-07-0
Molecular Weight 1514.28
Formula C₇₆H₉₆ClF₃N₁₀O₁₁S₃
SMILES

ClC1=CC=C(C=C1)C2=C(CC(C)(CC2)C)CN3CCN(CC3)C4=CC=C(C=C4)C(NS(C5=CC=C(C(S(=O)(C(F)(F)F)=O)=C5)N[C@H](CCN6CCN(CC6)C(CCCOC7=CC8=C(C=C7)[C@H](NC([C@@H]9C(C)(C[C@@]([H])(N9C%10=O)OCC[C@@H]%10NC([C@@H](NC)C)=O)C)=O)CCC8)=O)CSC%11=CC=CC=C%11)(=O)=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Protocols

All Cell Biology

Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (266 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)

References

[1]. Xuan Zhang, et al. Discovery of IAP-recruiting BCL-X L PROTACs as Potent Degraders Across Multiple Cancer Cell Lines. Eur J Med Chem. 2020 Aug 1;199:112397. [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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