PROTAC Mcl1 degrader-1 free base

PROTAC Mcl1 degrader-1, a proteolysis targeting chimera based on Cereblon ligand, is a potently and selectively Mcl-1 inhibitor.

For research use only. Not for human or veterinary use.

Target γ-secretase

Research area Neurological Disease

Purity >98% Stock Inquire

Data Sheet SDS COA

PROTAC Mcl1 degrader-1 structure

CAS No.: 2163793-38-0

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
25 mg	USD 590.00	BP-02378-25mg	In stock	Get quote
50 mg	USD 798.00	BP-02378-50mg	In stock	Get quote
100 mg	USD 1,290.00	BP-02378-100mg	In stock	Get quote
250 mg	USD 2,298.00	BP-02378-250mg	In stock	Get quote
500 mg	Inquire	BP-02378-500mg	In stock	Inquire

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Description

PROTAC Mcl1 degrader-1 (compound C3), a proteolysis targeting chimera (PROTAC) based on Cereblon ligand, is a potently and selectively Mcl-1 (Bcl-2 family member) inhibitor with an IC50 of 0.78 μM. PROTAC Mcl1 degrader-1 inhibits Bcl-2 with an IC50 of 0.54 μM .

Biological activity

In Vitro PROTAC Mcl1 degrader-1 (compound C3) induces the ubiquitination and proteasomal degradation of Mcl-1 by introducing the E3 ligase cereblon (CRBN)-binding ligand Pomalidomide (HY-10984) to Mcl-1 inhibitor S1-6 with μM-range affinity. PROTAC Mcl1 degrader-1 (0-10 μM; 0-24 h) induces selective depletion of Mcl-1 or Bcl-2 protein in HeLa cells in a time- and concentration-dependent manner. PROTAC Mcl1 degrader-1 (0-2 μM; 24 h) shows cytotoxicity against H23 cells

Identifiers

SMILES: O=C(C1=CC=CC(NCCCCCCNC(CCCCC(NCCN2C(C3=C4C(C2=O)=CC=C(C4=CC=C3)SC5=CC=C(C=C5)Br)=O)=O)=O)=C1C6=O)N6C7CCC(NC7=O)=O
InChIKey: BORXNUWYWZOREQ-UHFFFAOYSA-N

Specifications

MW (average): 909.8430
Formula: C₄₅H₄₅BrN₆O₈S
CAS No.: 2163793-38-0
Physical state: Solid
Color: White to off-white
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20°C, 3 years , 4°C, 2 years ; In solvent -20°C, 1 month

Solubility

Soluble in DMSO

In vitro: DMSO : 50 mg/mL

Documents

References

[1]. Wang Z, et al. Proteolysis Targeting Chimeras for the Selective Degradation of Mcl-1/Bcl-2 Derived from Nonselective Target Binding Ligands. J Med Chem. 2019 Aug 21.

Same target

Search γ-secretase

Same research area

Search Neurological Disease