PROTAC Bcl-xL degrader-2 is a potent Bcl-xL (Bcl-2 family member) degrader based on von Hippel-Lindau ligand, with an IC50 of 0.6 nM.

Product information

CAS Number: 2920415-08-1

Molecular Weight: 1329.60

Formula: C68H80N8O14S3

Chemical Name: 2-{8-[(1,3-benzothiazol-2-yl)carbamoyl]-1,2,3,4-tetrahydroisoquinolin-2-yl}-5-{3-[4-(1-{[(2S)-1-[(2S,4R)-4-hydroxy-2-({[4-(4-methyl-1,3-thiazol-5-yl)phenyl]methyl}carbamoyl)pyrrolidin-1-yl]-3,3-dimethyl-1-oxobutan-2-yl]carbamoyl}-3,6,9,12,15,18-hexaoxahenicos-20-yn-21-yl)phenoxy]propyl}-1,3-thiazole-4-carboxylic acid

Smiles: CC1N=CSC=1C1C=CC(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCOCCOCCOCCOCCOCCOCC#CC2C=CC(=CC=2)OCCCC2SC(=NC=2C(O)=O)N2CC3C(=CC=CC=3CC2)C(=O)NC2=NC3=CC=CC=C3S2)C(C)(C)C)=CC=1

InChiKey: LOJJAKUNUJJOKC-MXEISZGISA-N

InChi: InChI=1S/C68H80N8O14S3/c1-45-60(91-44-70-45)49-20-16-47(17-21-49)41-69-63(80)55-40-50(77)42-76(55)64(81)61(68(2,3)4)72-58(78)25-29-85-31-33-87-35-37-89-39-38-88-36-34-86-32-30-84-27-8-10-46-18-22-51(23-19-46)90-28-9-15-57-59(65(82)83)73-67(93-57)75-26-24-48-11-7-12-52(53(48)43-75)62(79)74-66-71-54-13-5-6-14-56(54)92-66/h5-7,11-14,16-23,44,50,55,61,77H,9,15,24-43H2,1-4H3,(H,69,80)(H,72,78)(H,82,83)(H,71,74,79)/t50-,55+,61-/m1/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 100 mg/mL (75.21 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

PROTAC Bcl-xL degrader-2 (PROTAC 6; 0.1 nM-10 μM; 24 hours) treatment decreases the level of Bcl-xL protein in THP-1 cells. PROTAC Bcl-xL degrader-2 (PROTAC 6) inhibits caspase 3/7 activity in MOLT-4 cells with an IC50 of 466 nM.

Products are for research use only. Not for human use.