LL-K8-22
Based on 1 Customer Validation
LL-K8-22 is a potent, selective and durable PROTAC CDK8-cyclin C dual degrader, with DC50 values of 2.52 and 2.64 μM, respectively. LL-K8-22 also suppresses STAT1 Ser 727 phosphorylation. LL-K8-22 inhibits E2F- and MYC-driven carcinogenic transcriptional programs. LL-K8-22 can be used for triplenegative breast cancer (TNBC) research.
(Pink: CDK8 ligand (HY-168683); Blue: hyt ligand (HY-N2427); Black: linker).
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 99.06%
- CAS No.: 3034487-84-5
- 화학식: C37H43N5O
- 분자량:573.77
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보관:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Cell Cycle/DNA Damage Compound Library
HY-L004
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Immunology/Inflammation Compound Library
HY-L007
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JAK/STAT Compound Library
HY-L008
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Kinase Inhibitor Library
HY-L009
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Stem Cell Signaling Compound Library
HY-L017
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Anti-Cancer Compound Library
HY-L025
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Anti-Aging Compound Library
HY-L034
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Differentiation Inducing Compound Library
HY-L038
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Anti-Breast Cancer Compound Library
HY-L074
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Anti-Lung Cancer Compound Library
HY-L075
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Anti-Pancreatic Cancer Compound Library
HY-L077
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Anti-Blood Cancer Compound Library
HY-L079
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Anti-Obesity Compound Library
HY-L087
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Transcription Factor-Targeted Library
HY-L090
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Cancer Stem Cells Compound Library
HY-L135
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PROTAC Library
HY-L151
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Highly Selective Inhibitors Library
HY-L158
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Anti-Hematopathy Compound Library
HY-L171
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HY-L034M
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Posttranslational Modification Library
HY-L226
All PROTACs Isoforms
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Biological Activity
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CDK8 2.52 μM (DC50) |
STAT1 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
5.87 μM
Compound: LL-K8-22
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Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation incubated for 4 days by Celltiter glo luminescent assay
Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation incubated for 4 days by Celltiter glo luminescent assay
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[PMID: 36930701] |
| MDA-MB-231 | IC50 |
6.22 μM
Compound: LL-K8-22
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Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation incubated for 4 days by Celltiter glo luminescent assay
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation incubated for 4 days by Celltiter glo luminescent assay
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[PMID: 36930701] |
| MDA-MB-468 | IC50 |
5.73 μM
Compound: LL-K8-22
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Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell proliferation incubated for 4 days by Celltiter glo luminescent assay
Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell proliferation incubated for 4 days by Celltiter glo luminescent assay
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[PMID: 36930701] |
LL-K8-22 (0-10 μM, 24 h) degrades the CDK8-cyclin C complex in a dose-dependent manner[1].
LL-K8-22 (0-20 μM, 4 days) suppresses tumor cell proliferation[1].
LL-K8-22 (0-8 μM, 24 h) inhibits CDK8-cyclin C downstream signaling[1].
LL-K8-22 significantly downregulated EAPP (E2F family binding protein)[1].
LL-K8-22 dose not affect CDK8 and CCNC mRNA levels[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-468 cells
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Concentration:0, 0.625, 1.25, 2.5, 5, and 10 μM
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Incubation Time:24 h
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Result:Induced selective and synchronous degradation of CDK8 and cyclin C protein expression in a dose-dependent manner with DC50 of 2.52 and 2.64 μM, respectively. Significantly degraded CDK8 without reducing CDK19 (a highly homologous protein of CDK8) and did not degrade other cyclin proteins except cyclin C.
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Cell Line:MDA-MB-468, HCT-116, and MDA-MB-231 cells
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Concentration:0, 0.625, 1.25, 2.5, 5, and 10 μM
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Incubation Time:24 h
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Result:Induced selective and synchronous degradation of CDK8 and cyclin C protein expression in a dose-dependent manner with DC50 of 2.52 and 2.64 μM, respectively. Significantly degraded CDK8 without reducing CDK19 (a highly homologous protein of CDK8) and did not degrade other cyclin proteins except cyclin C.
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Cell Line:MDA-MB-468 cells
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Concentration:0, 2, 4, and 8 μM
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Incubation Time:24 h
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Result:Reduced Ser 2 and Ser 5 phosphorylation of the C-terminal domain of RNA pol II in a dose-dependent manner. Only inhibited the Ser 727 phosphorylation of STAT1 and did not affect Janus kinase (JAK)-mediated phosphorylation of Tyr 701.
Chemical Information
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CAS No. 3034487-84-5
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Appearance Solid
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분자량 573.77
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화학식 C37H43N5O
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Color White to off-white
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SMILES
O=C(CN1C=C(C2=CC=C(C3=CN=CC4=CC=CC=C43)C=C2)C=N1)N5CCN(CCCC67CC8CC(CC(C8)C7)C6)CC5
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 125 mg/mL (217.86 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (274 KB)
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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)
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Handling Instructions (2659 KB)
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 | 1.7429 mL | 8.7143 mL | 17.4286 mL | 43.5715 mL |
| 5 mM | 0.3486 mL | 1.7429 mL | 3.4857 mL | 8.7143 mL | |
| 10 mM | 0.1743 mL | 0.8714 mL | 1.7429 mL | 4.3571 mL | |
| 15 mM | 0.1162 mL | 0.5810 mL | 1.1619 mL | 2.9048 mL | |
| 20 mM | 0.0871 mL | 0.4357 mL | 0.8714 mL | 2.1786 mL | |
| 25 mM | 0.0697 mL | 0.3486 mL | 0.6971 mL | 1.7429 mL | |
| 30 mM | 0.0581 mL | 0.2905 mL | 0.5810 mL | 1.4524 mL | |
| 40 mM | 0.0436 mL | 0.2179 mL | 0.4357 mL | 1.0893 mL | |
| 50 mM | 0.0349 mL | 0.1743 mL | 0.3486 mL | 0.8714 mL | |
| 60 mM | 0.0290 mL | 0.1452 mL | 0.2905 mL | 0.7262 mL | |
| 80 mM | 0.0218 mL | 0.1089 mL | 0.2179 mL | 0.5446 mL | |
| 100 mM | 0.0174 mL | 0.0871 mL | 0.1743 mL | 0.4357 mL |
LL-K8-22 Related Classifications
HY-149209 Related Classifications
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