2. PROTAC Cell Cycle/DNA Damage Stem Cell/Wnt JAK/STAT Signaling
  3. PROTACs CDK STAT Early 2 Factor (E2F)
  4. LL-K8-22

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: Ligand for target protein (HY-168683); Black: Linker (HY-Y0340); Blue: Ligand for E3 ligase (HY-N2427)) .

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

LL-K8-22 Chemical Structure

LL-K8-22 Chemical Structure

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5 mg USD 410 In-stock
10 mg USD 660 In-stock
25 mg USD 1320 In-stock
50 mg USD 2100 In-stock
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Based on 1 publication(s) in Google Scholar

LL-K8-22 Related Antibodies

Top Publications Citing Use of Products

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

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STAT3 STAT5 STAT6 STAT1

  • Biological Activity

  • Purity & Documentation

  • References

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Description

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: Ligand for target protein (HY-168683); Black: Linker (HY-Y0340); Blue: Ligand for E3 ligase (HY-N2427)) [1].

IC50 & Target

CDK8

2.52 μM (DC50)

STAT1

 

In Vitro

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.

LL-K8-22 Related Antibodies

Western Blot Analysis[1]

Cell Line: MDA-MB-468 cells
Concentration: 0, 0.625, 1.25, 2.5, 5, and 10 μM
Incubation Time: 24 h
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.

Cell Proliferation Assay[1]

Cell Line: MDA-MB-468, HCT-116, and MDA-MB-231 cells
Concentration: 0, 0.625, 1.25, 2.5, 5, and 10 μM
Incubation Time: 24 h
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.

Western Blot Analysis[1]

Cell Line: MDA-MB-468 cells
Concentration: 0, 2, 4, and 8 μM
Incubation Time: 24 h
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.
Molecular Weight

573.77

Formula

C37H43N5O
Appearance

Solid

Color

White to off-white

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
Shipping

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

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7429 mL 8.7143 mL 17.4286 mL
5 mM 0.3486 mL 1.7429 mL 3.4857 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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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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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 1.7429 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
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LL-K8-22 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:

LL-K8-22PROTACsCDKSTATEarly 2 Factor (E2F)Cyclin dependent kinaseMDA-MB-468 cellsHCT-116MDA-MB-231 cellsCyclin-dependent kinasesEAPPtriplenegative breast cancerInhibitorinhibitorinhibit

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