2. Metabolic Enzyme/Protease
  3. Hexokinase
  4. PROTAC HK2 Degrader-1

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.

For research use only. We do not sell to patients.

PROTAC HK2 Degrader-1 Chemical Structure

PROTAC HK2 Degrader-1 Chemical Structure

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1 mg USD 126 In-stock
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Based on 1 publication(s) in Google Scholar

PROTAC HK2 Degrader-1 Related Antibodies

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1 Publications Citing Use of MCE PROTAC HK2 Degrader-1

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Description

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].

IC50 & Target

DC50: 2.56 μM (Hexokinase 2, HK2 in 4T1); 0.79 μM ((Hexokinase 2, HK2 in MDA-MB-231)
In Vitro

PROTAC HK2 Degrader-1 inhibits the proliferation of 786-O, 4T1, PANC-1, HGC-27, and MCF-1 with IC50s of 34.07 μM, 5.08 μM, 31.53 μM, 6.11 μM, and 21.65 μM, respectively[1].
PROTAC HK2 Degrader-1 degrades HK2 with DC50 values of was 2.56 μM (4T1) and 0.79 μM (MDA-MB-231), respectively[1].
PROTAC HK2 Degrader-1 (0.01-200 μM, 36 h) selectively suppresses breast cancer cell proliferation and stimulates HK2 protein degradation via the ubiquitin mediated proteasome pathway in a time and concentration dependent manner[1].
PROTAC HK2 Degrader-1 (10 μM for 4T1, 0.5 μM for MDA-MB-231, 24 h) degraded HK2 protein via the ubiquitin−proteasome system by forming a ternary complex[1].
PROTAC HK2 Degrader-1 (20 μM, 36 h) mediates degradation of HK2 that causing mitochondrial damage, releasing cytochrome C to activate caspase-3, then PROTAC HK2 Degrader-1 cleaves GSDME to trigger thermal coma and promotes cellular release of danger signals, such as ATP, HMGB1, CRT, etc., thus inducing cellular immune death[1].
PROTAC HK2 Degrader-1 (20 μM, 36 h) can induce PD-L1 protein to internalize from the cell membrane to the cytoplasm and reduce the total amount of PD-L1 protein[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

PROTAC HK2 Degrader-1 Related Antibodies

Cell Cytotoxicity Assay[1]

Cell Line: 4T1, MDA-MB-231, PUMC-HUVEC-T1
Concentration: 20 μM
Incubation Time: 72 h (MTT), 48 h (CCK-8)
Result: Showed the greatest impact on 4T1 and HGC-27 cells, with IC50 dosages of 5.08 and 6.11 μM.
Selectively suppressed breast cancer cell proliferation and stimulates HK2 protein degradation.
Prevented 4T1 cells to form a colony and had little influence on HUVECT-1.

Western Blot Analysis[1]

Cell Line: 4T1, MDAMB-231
Concentration: 20 μM; 0.01, 0.05, 0.1, 0.5, 1.0, 2.0, 5.0, 10, 20, 50, 100, 150, 200 μM; 10 μM; 0.5 μM.
Incubation Time: 36 h; 24 h
Result: Degraded 71.06% of HK2 at 20 μM in 4T1 and MDAMB-231 cells.
DC50=2.56 μM (4T1) and 0.79 μM (MDA-MB-231), respectivley.
Promoted the degradation of HK2 protein within 12 h, with the greatest degradation impact at 36 h in 4T1 cells and MDA-MB-231 cells.
Degradation capacity was reduced, because pretreatment with Tha and LND occupy the protein pocket and disrupt the formation of the ternary complex of HK2, CRBN and C-02.
Increased the expression of VDAC and Bax and decreased the level of Bcl-2 protein.
had lower levels of full-length caspase-3 and higher levels of cleaved caspase-3.
Cleaved GSDME through cleaved caspase-3, increasing the N-terminus of GSDME protein and thus triggering pyroptosis in 4T1 cells.

Immunofluorescence[1]

Cell Line: 4T1 and MDA-MB-231
Concentration: 20 μM
Incubation Time: 36 h
Result: Caused the degradation of HK2 protein in a concentration dependent manner.
Significantly reduced the visual yellow fluorescence of HK2 protein.
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

647.51

Formula

C32H28Cl2N6O5
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(N1)CCC(N(C(C2=C3C=CC=C2NCCCCNC(C4=NN(C5=C4C=CC=C5)CC6=C(C=C(C=C6)Cl)Cl)=O)=O)C3=O)C1=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (154.44 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5444 mL 7.7219 mL 15.4438 mL
5 mM 0.3089 mL 1.5444 mL 3.0888 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
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Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.5444 mL 7.7219 mL 15.4438 mL 38.6094 mL
5 mM 0.3089 mL 1.5444 mL 3.0888 mL 7.7219 mL
10 mM 0.1544 mL 0.7722 mL 1.5444 mL 3.8609 mL
15 mM 0.1030 mL 0.5148 mL 1.0296 mL 2.5740 mL
20 mM 0.0772 mL 0.3861 mL 0.7722 mL 1.9305 mL
25 mM 0.0618 mL 0.3089 mL 0.6178 mL 1.5444 mL
30 mM 0.0515 mL 0.2574 mL 0.5148 mL 1.2870 mL
40 mM 0.0386 mL 0.1930 mL 0.3861 mL 0.9652 mL
50 mM 0.0309 mL 0.1544 mL 0.3089 mL 0.7722 mL
60 mM 0.0257 mL 0.1287 mL 0.2574 mL 0.6435 mL
80 mM 0.0193 mL 0.0965 mL 0.1930 mL 0.4826 mL
100 mM 0.0154 mL 0.0772 mL 0.1544 mL 0.3861 mL
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PROTAC HK2 Degrader-1 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PROTAC HK2 Degrader-1HexokinaseHexokinase 2HK2lonidamineLNDthalidomideTha4T1MDA-MB-231MCF-7PROTACbreast cancer.Inhibitorinhibitorinhibit

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