Free shipping on all orders over $ 500

PROTAC SGK3 degrader-1

Cat. No. M10382
PROTAC SGK3 degrader-1 Structure
Synonym:

SGK3-PROTAC1

Size Price Availability Quantity
1mg USD 450  USD450 In stock
5mg USD 700  USD700 In stock
10mg USD 1200  USD1200 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
Biological Activity

PROTAC SGK3 degrader-1 (SGK3-PROTAC1) is a potent SGK3 degrader, it is a PROTAC conjugate of the 308-R SGK inhibitor with the VH032 VHL binding ligand, targeting SGK3 (Serum/Glucocorticoid Regulated Kinase Family Member 3). SGK3-PROTAC1 (0.3 μM) induces 50% degradation of endogenous SGK3 within 2 h, with maximal 80% degradation observed within 8 h, accompanied by a loss of phosphorylation of NDRG1, an SGK3 substrate. Low doses of SGK3-PROTAC1 (0.1−0.3 μM) restores sensitivity of SGK3 dependent ZR-75-1 and CAMA-1 breast cancer cells to Akt and PI3K inhibitors, whereas the cis epimer analogue incapable of binding to the VHL E3 ligase has no impact. SGK3-PROTAC1 suppresses proliferation of ZR-75-1 and CAMA-1 cancer cell lines treated with a PI3K inhibitor more effectively than could be achieved by a conventional SGK isoform inhibitor.

Chemical Information
Molecular Weight 1157.38
Formula C57H73FN10O11S2
CAS Number 2381320-35-8
Solubility (25°C) DMSO ≥ 90 mg/mL
Storage -20°C, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Hannah Tovell, et al. ACS Chem Biol. Design and Characterization of SGK3-PROTAC1, an Isoform Specific SGK3 Kinase PROTAC Degrader

Related PROTAC Products
DGY-09-192

DGY-09-192 is a bivalent degrader that couples the pan-FGFR inhibitor BGJ398 to the CRL2VHL E3 ligase-recruiting ligand, which induces degradation of FGFR1/2 and largely avoids degradation of FGFR3/4.DGY-09-192 exhibits a nanomolar DC50 against both wild-type FGFR2 and several FGFR2 fusions. In addition, DGY-09-192 has antiproliferative activity in gastric and cholangiocarcinoma cells.

BTX-6654

BTX-6654 is a targeted and specific cerebellar-based bifunctional SOS1 PROTAC degrader.BTX-6654 reduces the downstream signaling markers pERK and pS6 and displays antiproliferative activity in a wide range of KRAS-mutant cells.

ND1-YL2

ND1-YL2 is a PROTAC that selectively degrades SRC-1 via the N-degron pathway.

PRT3789

PRT3789 is a PROTAC degrader targeting SMARCA2 with more than 1,000-fold selectivity for SMARCA2 compared to SMARCA4 at the cellular level for studies related to non-small cell lung cancer (NSCLC).

KT-294

KT-294 is a potential first-in-class, PROTAC protein degrader targeting TYK2 for research related to immune system diseases.

  Catalog
Abmole Inhibitor Catalog




Keywords: PROTAC SGK3 degrader-1, SGK3-PROTAC1 supplier, PROTAC, inhibitors, activators


Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.