PROTAC Mcl1 degrader-1 - 98%, high purity , CAS No.2163793-38-0

  • ≥98%
Item Number
P651236
Grouped product items
SKUSizeAvailabilityPrice Qty
P651236-10mg
10mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$1,500.90
P651236-1mg
1mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$550.90
P651236-5mg
5mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$980.90
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Apoptosis Bcl-2 Family PROTAC PROTACs

Basic Description

Specifications & Purity≥98%
Biochemical and Physiological MechanismsPROTAC 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 IC 50 of 0.78 μM. PROTAC Mcl1 degrader-1 inhibits Bcl-2 with an IC 50 o
Storage TempStore at -20°C,Argon charged
Shipped InIce chest + Ice pads
Product 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 IC 50 of 0.78 μM. PROTAC Mcl1 degrader-1 inhibits Bcl-2 with an IC 50 of 0.54 μM

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. ?\nPROTAC 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. ?\nPROTAC Mcl1 degrader-1 (0-2 μM; 24 h) shows cytotoxicity against H23 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: HeLa cells and H23 cells Concentration: 0.3, 1.0, 3.0 and 10 μM Incubation Time: 0-24 h Result: Induced time- and concentration-dependent selective depletion of Mcl-1 or Bcl-2 protein in HeLa cells. Induced Mcl-1 depletion and PARP cleavage in H23 cells (0-10 μM; 12 h).

Form:Solid

IC50& Target:Mcl-1 0.78 μM (IC 50 ) Bcl-2 0.54 μM (IC 50 )

Associated Targets(Human)

MCL1 Tchem Induced myeloid leukemia cell differentiation protein Mcl-1 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
BCL2 Tclin Apoptosis regulator Bcl-2 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
NCI-H23 (49055 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
BCL2 Tclin Apoptosis regulator Bcl-2 (3787 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MCL1 Tchem Induced myeloid leukemia cell differentiation protein Mcl-1 (3820 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
BCL2 Tclin Protein cereblon/Apoptosis regulator Bcl-2 (74 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MDM2 Tchem Protein cereblon/E3 ubiquitin-protein ligase Mdm2 (233 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
BCL2L1 Tchem Protein cereblon/Bcl-2-like protein 1 (8 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

Names and Identifiers

IUPAC Name N'-[2-[6-(4-bromophenyl)sulfanyl-1,3-dioxobenzo[de]isoquinolin-2-yl]ethyl]-N-[6-[[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]amino]hexyl]hexanediamide
INCHI InChI=1S/C45H45BrN6O8S/c46-27-15-17-28(18-16-27)61-35-21-19-32-39-29(35)9-7-10-30(39)42(57)51(43(32)58)26-25-49-37(54)14-4-3-13-36(53)48-24-6-2-1-5-23-47-33-12-8-11-31-40(33)45(60)52(44(31)59)34-20-22-38(55)50-41(34)56/h7-12,15-19,21,34,47H,1-6,13-14,20,22-26H2,(H,48,53)(H,49,54)(H,50,55,56)
InChi Key BORXNUWYWZOREQ-UHFFFAOYSA-N
Canonical SMILES C1CC(=O)NC(=O)C1N2C(=O)C3=C(C2=O)C(=CC=C3)NCCCCCCNC(=O)CCCCC(=O)NCCN4C(=O)C5=C6C(=C(C=C5)SC7=CC=C(C=C7)Br)C=CC=C6C4=O
Isomeric SMILES C1CC(=O)NC(=O)C1N2C(=O)C3=C(C2=O)C(=CC=C3)NCCCCCCNC(=O)CCCCC(=O)NCCN4C(=O)C5=C6C(=C(C=C5)SC7=CC=C(C=C7)Br)C=CC=C6C4=O
PubChem CID 139035048
Molecular Weight 909.84

Certificates

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Chemical and Physical Properties

SolubilityDMSO : 50 mg/mL (54.95 mM; Need ultrasonic)

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Solution Calculators