PROTAC HK2 Degrader-1
- CAS No.
- 3033812-84-6
- Chemical Name:
- PROTAC HK2 Degrader-1
- Synonyms
- PROTAC HK2 Degrader-1;1H-Indazole-3-carboxamide, 1-[(2,4-dichlorophenyl)methyl]-N-[4-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]butyl]-
- CBNumber:
- CB014286595
- Molecular Formula:
- C32H28Cl2N6O5
- Molecular Weight:
- 647.51
- MDL Number:
- MOL File:
- 3033812-84-6.mol
- MSDS File:
- SDS
- TDS File:
- TDS
PROTAC HK2 Degrader-1 price
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Cayman Chemical | 39384 | C-02 ≥95% | 3033812-84-6 | 500μg | $72 | 2026-04-30 | Buy |
| Cayman Chemical | 39384 | C-02 ≥95% | 3033812-84-6 | 1mg | $137 | 2026-04-30 | Buy |
| Cayman Chemical | 39384 | C-02 ≥95% | 3033812-84-6 | 5mg | $323 | 2026-04-30 | Buy |
| ChemScene | CS-0866808 | PROTAC HK2 Degrader-1 98.98% | 3033812-84-6 | 1mg | $136 | 2026-06-04 | Buy |
| ChemScene | CS-0866808 | PROTAC HK2 Degrader-1 98.98% | 3033812-84-6 | 5mg | $300 | 2026-06-04 | Buy |
PROTAC HK2 Degrader-1 Chemical Properties, Uses, Production
Uses
PROTAC HK2 Degrader-1 is a PROTAC consisting of Lonidamine (HY-B0486) as a target protein Hexokinase 2 (HK2) inhibitor and Thalidomide (HY-14658) as a CRBN ligand-linked PROTAC. PROTAC HK2 Degrader-1 selectively inhibits the proliferation of breast cancer cells by forming a ternary complex through the ubiquitin-proteasome system to degrade Hexokinase 2 (HK2) protein leading to mitochondrial damage and cell death. PROTAC HK2 Degrader-1 effectively inhibits breast tumor growth and reduces the colonic side effects of cisplatin for breast cancer research[1].
in vivo
PROTAC HK2 Degrader-1 (50 mg/kg, Intraperitoneal injection, bid, for nine times, into six-weekold female BALB/c mice) inhibits tumor growth in 4T1 tumor models[1].
PROTAC HK2 Degrader-1 (50 mg/kg, Intraperitoneal injection, bid, for nine times, six-weekold female BALB/c mice) can induce GSDME-dependent pyroptosis to realize tumor immune response and effectively inhibit breast tumor growth[1].
PROTAC HK2 Degrader-1 (Cisplatin (HY-17394) 10mg/kg, i.v., C-02 50mg/kg, i.p., 25 days, into six-weekold female BALB/c mice) can sensitize Cisplatin (HY-17394) while reducing the colon side effects of Cisplatin (HY-17394), which has potential clinical value[1].
| Animal Model: | xenograft models , into six-weekold female BALB/c mice[1] |
| Dosage: | 50 mg/kg |
| Administration: | Intraperitoneal injection, bid, for nine times. |
| Result: | Reduced proliferation and damaged nuclei in mouse models. Increased the levels of Cytokines IL-1β, IFN-γ, and TNF-α significantly and decreased the level of TGF-β and IL-10. Elevated levels of cleaved-Casp-3 and GSDME-N in tumor tissues of mouse. |
| Animal Model: | breast tumor model in mice by injecting 4T1 cells subcutaneously into six-weekold female BALB/c mice[1] |
| Dosage: | Cisplatin (HY-17394) 10mg/kg, 50mg/kg |
| Administration: | Cisplatin (HY-17394) (10mg/kg, i.v.), 50mg/kg, i.p., 25 days |
| Result: | Inhibited tumor growth and tumor volume. Decreased HK2 protein level, while co- treated with Cisplatin (HY-17394). Could alleviate Cisplatin (HY-17394) aggravated colon damage. |
References
[1] Sang R, et al. Degradation of Hexokinase 2 Blocks Glycolysis and Induces GSDME-Dependent Pyroptosis to Amplify Immunogenic Cell Death for Breast Cancer Therapy. J Med Chem. 2023 Jun 27. DOI:10.1021/acs.jmedchem.3c00118
PROTAC HK2 Degrader-1 Preparation Products And Raw materials
Raw materials
Preparation Products
PROTAC HK2 Degrader-1 Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Tianjin Kailiqi Biotechnology Co., Ltd. | 15076683720 | klq@cw-bio.com | China | 9783 | 55 |
| Guangzhou Younan Technology Co., Ltd | 020-82000279 18988941452 | YN_research@163.com | China | 2984 | 58 |
| Selection Bioscience LLC | 18280071318 18621190837 | hr@selectionbio.com | China | 84 | 58 |
| Supplier | Advantage |
|---|---|
| Tianjin Kailiqi Biotechnology Co., Ltd. | 55 |
| Guangzhou Younan Technology Co., Ltd | 58 |
| Selection Bioscience LLC | 58 |
