MS6105
Based on 1 Customer Validation
MS6105 is a PROTAC degrader targeting LDHA and LDHB, with DC50 values of 38 nM and 74 nM for degrading LDHA and LDHB in PANC-1 cells, respectively, and no hook effect is observed at high concentrations. MS6105 inhibits the proliferation of pancreatic cancer cells, and no obvious toxicity is observed after intraperitoneal administration in mice. MS6105 can be used for pancreatic cancer-related research.
(Pink: LDHA and LDHB ligand (HY-175562); Blue: VHL ligand (HY-125845); Black: linker (HY-128421)).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.2%
- CAS 番号: 2891709-58-1
- 分子式: C65H81N9O9S3
- 分子量:1228.59
-
保管条件:
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
生物活性
-
化学情報
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
PROTACs アイソフォーム固有の製品をすべて表示
More
生物活性
|
LDHA 38 nM (DC50) |
LDHA 74 nM (DC50) |
MS6105 (compound 22) (10 nM-10 μM; 3 h-48 h) degrades LDHA and LDHB in PANC-1 cells in a concentration- and time-dependent manner, with a DC50 of 38 nM for LDHA degradation and 74 nM for LDHB degradation, and this degradation depends on the ubiquitin-proteasome system[1].
MS6105 (3 μM; 24 h) selectively downregulates the protein levels of LDHA and LDHB in PANC-1 cells, with most of the affected proteins involved in cellular metabolic processes[1].
MS6105 (0.1 μM-60 μM; 24 h-72 h) inhibits the proliferation of PANC-1, MiaPaCa2 and BxPC3 pancreatic cancer cells and degrades LDHA, with potency superior to that of its parent LDH inhibitor 5[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:PANC-1 pancreatic cancer cells
-
Concentration:10 nM, 30 nM, 100 nM, 300 nM, 1 μM, 3 μM and 10 μM
-
Incubation Time:48 h
-
Result:The compound potently degraded LDHA with a DC50 of 38 nM and a maximum degradation (Dmax) of 93%. It also degraded LDHB with a DC50 of 74 nM and a Dmax of 86%. No hook effect was observed at concentrations up to 10 μM.
-
Cell Line:PANC-1 pancreatic cancer cells
-
Concentration:1 μM
-
Incubation Time:1, 3, 6, 12, 24, 36 and 48 h
-
Result:LDHA and LDHB degradation was observed as early as 24 h, and the maximum degradation was reached at 48 h.
-
Cell Line:PANC-1 pancreatic cancer cells
-
Concentration:3 μM
-
Incubation Time:24 h, post 2 h pretreatment with 20 μM Ac-VHL-Me, 1 μM MG132 (HY-13259), 1 μM MLN4924 (HY-70062)
-
Result:The LDHA degradation induced by the degrader was partially rescued by pretreatment with the VHL ligand, a proteasome inhibitor, a neddylation inhibitor, or the parent LDH inhibitor.
| Species | Dose | Route | Cmax |
|---|---|---|---|
| Mice[1] | 5 mg/kg | i.p. | 1800 nM |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Swiss Albino (male)[1]
-
Dosage:5 mg/kg
-
Administration:i.p.; single dose
-
Result:Achieved a peak plasma concentration of 1800 nM at 8 hours.
Maintained measurable exposure over 24 hours.
Showed no clinical signs of toxicity.
化学情報
-
CAS 番号 2891709-58-1
-
性状 Solid
-
分子量 1228.59
-
分子式 C65H81N9O9S3
-
Color White to off-white
-
SMILES
CC1=C(SC=N1)C2=CC=C(C=C2)CNC([C@@H]3C[C@H](CN3C([C@H](C(C)(C)C)NC(CCCCCCCCCCCC(NCCCCC#CC4=CC=CC(C5=NN(C(CC6CC6)=C5CC7=CC=C(C=C7)S(N)(=O)=O)C8=NC(C(O)=O)=CS8)=C4)=O)=O)=O)O)=O
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
純度とドキュメンテーション
-
データシート (272 KB)
-
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
-
取扱説明書 (2659 KB)
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
MS6105 関連分類
HY-152261 関連分類
Powered by Bioz