2. PROTAC Epigenetics Immunology/Inflammation GPCR/G Protein Apoptosis
  3. PROTACs Histone Acetyltransferase Interleukin Related CXCR TNF Receptor CD28
  4. GSK699

GSK699 is a KAT2A/B/PCAF/GCN5 PROTAC degrader. GSK699 induces proteasome-dependent degradation of KAT2A, KAT2B, PCAF and GCN5, regulates the histone acetyltransferase activity of the SAGA complex, and reduces the level of histone H3K9ac. GSK699 inhibits the growth of neuroblastoma, acute myeloid leukemia and small cell lung cancer cells. GSK699 reduces the production of inflammatory cytokines and chemokines, and impairs LPS-stimulated immune cell responses. GSK699 is applicable to research related to acute myeloid leukemia, small cell lung cancer, neuroblastoma and inflammatory diseases.
(Pink: GCN5/PCAF ligand (HY-101027); Blue: Cereblon ligand (HY-103596); Black: linker).

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

GSK699

GSK699 Chemical Structure

CAS No. : 2260944-68-9

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GSK699 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

GSK699 is a KAT2A/B/PCAF/GCN5 PROTAC degrader. GSK699 induces proteasome-dependent degradation of KAT2A, KAT2B, PCAF and GCN5, regulates the histone acetyltransferase activity of the SAGA complex, and reduces the level of histone H3K9ac. GSK699 inhibits the growth of neuroblastoma, acute myeloid leukemia and small cell lung cancer cells. GSK699 reduces the production of inflammatory cytokines and chemokines, and impairs LPS-stimulated immune cell responses. GSK699 is applicable to research related to acute myeloid leukemia, small cell lung cancer, neuroblastoma and inflammatory diseases[1]. (Pink: GCN5/PCAF ligand (HY-101027); Blue: Cereblon ligand (HY-103596); Black: linker).

IC50 & Target[1]

IL-6

 

GCN5/PCAF

 

Cereblon

 

Cellular Effect
Cell Line Type Value Description References
THP-1 DC50
1.5 nM
Compound: 92; GSK983
Protac activity against E3 ubiquitin ligase/PCAF in human THP-1 cells assessed as induction of PCAF protein degradation
Protac activity against E3 ubiquitin ligase/PCAF in human THP-1 cells assessed as induction of PCAF protein degradation
[PMID: 31035238]
THP-1 DC50
3 nM
Compound: 92; GSK983
Protac activity against E3 ubiquitin ligase/GCN5 in human THP-1 cells assessed as induction of GCN5 protein degradation
Protac activity against E3 ubiquitin ligase/GCN5 in human THP-1 cells assessed as induction of GCN5 protein degradation
[PMID: 31035238]
In Vitro

GSK699 potently degrades KAT2A (DC50 = 2.2 nM) and KAT2B (DC50 = 0.08 nM) in MOLM-13 cells, and inhibits the proliferation of MOLM-13 cells with an activity of GI50 = 64 nM[1].
GSK699 potently degrades KAT2A (DC50 = 1.5 nM) and KAT2B (DC50 = 0.1 nM) in NCI-H1048 cells, and inhibits the proliferation of NCI-H1048 cells with a GI50 of 32 nM[1].
GSK699 inhibits the proliferation of KELLY neuroblastoma cells in vitro[1].
Treatment of wild-type primary mouse HSPCs with GSK699 (100 nM; 48 h) significantly reduces intracellular H3K9ac levels, upregulates cell surface Sca-1 expression, and increases the frequency of immunophenotypic HSCs and megakaryocyte progenitor cells[2].
Treatment of c-Kit+ Sca-1+Lin− wild-type primary mouse hematopoietic stem and progenitor cells (HSPCs) with GSK699 (100 nM; 48 h) induces transcriptomic changes that are highly correlated with those caused by Tada2b knockout in HSPCs[2].
GSK699 (0.03-1000 nM; 18 h) potently induces concentration-dependent degradation of PCAF in THP1 cells[3].
GSK699 (100 nM; 5-6 days) potently reduces the production of IL-6, IL-12p70, IL-10, IL-1β, IFN-γ, TNF and IL-8 in human monocyte-derived dendritic cells stimulated with LPS (HY-D1056)[3].
GSK699 (100 nM; 6 days) reduces the production of multiple inflammatory mediators in LPS-stimulated human monocyte-derived dendritic cells, including IL-6, CXCL12, IL12A, TNF, IL-12p70, IL10, CXCL1/GROα, CXCL11/I-TAC, CCL16, CCL7, CCL20/MIP-3α, CXCL10, CXCL1, CCL8 and CCL19/MIP-3β, and upregulates CD1C, FCER1A, CD28 and CD8A[3].

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

GSK699 Related Antibodies

Western Blot Analysis[3]

Cell Line: THP1 human monocytic leukemia cells
Concentration: 0.03 nM, 0.1 nM, 0.3 nM, 1 nM, 3 nM, 10 nM, 30 nM, 100 nM, 300 nM, 1000 nM
Incubation Time: 18 h
Result: Induced potent, concentration-dependent degradation of PCAF in THP1 cells.
Left 65% of PCAF remaining relative to DMSO control at 0.03 nM.
Left 62% of PCAF remaining relative to DMSO control at 0.1 nM.
Left 53% of PCAF remaining relative to DMSO control at 0.3 nM.
Left 29% of PCAF remaining relative to DMSO control at 1 nM.
Left 16% of PCAF remaining relative to DMSO control at 3 nM.
Left 8% of PCAF remaining relative to DMSO control at 10 nM.
Left 4% of PCAF remaining relative to DMSO control at 30 nM.
Left 3% of PCAF remaining relative to DMSO control at 100 nM.
Left 3% of PCAF remaining relative to DMSO control at 300 nM.
Left 6% of PCAF remaining relative to DMSO control at 1000 nM.
Showed a slight hook effect (increased remaining PCAF) at the highest concentration (1000 nM).

Real Time qPCR[3]

Cell Line: LPS-stimulated human CD14+ monocyte-derived dendritic cells (DCs)
Concentration: 100 nM
Incubation Time: 6 days (differentiation)
Result: Altered LPS-induced mRNA expression of numerous genes in human monocyte-derived dendritic cells.
Significantly down-regulated chemokine and cytokine genes including CXCL12, IL6, IL12A, IL10, CCL16, CCL7, CXCL10, CXCL1, and CCL8.
Increased CD1C, FCER1A, CD28, and CD8A mRNA levels.
Significantly down-regulated TNF mRNA but by less than 3-fold.
Parmacokinetics
Species Dose Route CL CLunbound T1/2 Vdss AUC0-last
Mice[1] 1 mg/kg i.v. 36 mL/min/kg 27692 mL/min/kg 1.4 h 1.2 L/kg 0.00062 nM·h/mL
Molecular Weight

895.84

Formula

C45H51BrN8O7
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(N(CCCN(C1=CC=C(CCCOC2=CC=CC(C(N3C(CC4)C(NC4=O)=O)=O)=C2C3=O)C=C1)C)C)C5=CC=C([C@@H]6CN(C)C[C@H](NC(C=NN7C)=C(Br)C7=O)C6)C=C5
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 : 50 mg/mL (55.81 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 1.1163 mL 5.5814 mL 11.1627 mL
5 mM 0.2233 mL 1.1163 mL 2.2325 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.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 98.80%

SDS (251 KB)

COA (246 KB) HNMR (364 KB) LCMS (95 KB)

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 1.1163 mL 5.5814 mL 11.1627 mL 27.9068 mL
5 mM 0.2233 mL 1.1163 mL 2.2325 mL 5.5814 mL
10 mM 0.1116 mL 0.5581 mL 1.1163 mL 2.7907 mL
15 mM 0.0744 mL 0.3721 mL 0.7442 mL 1.8605 mL
20 mM 0.0558 mL 0.2791 mL 0.5581 mL 1.3953 mL
25 mM 0.0447 mL 0.2233 mL 0.4465 mL 1.1163 mL
30 mM 0.0372 mL 0.1860 mL 0.3721 mL 0.9302 mL
40 mM 0.0279 mL 0.1395 mL 0.2791 mL 0.6977 mL
50 mM 0.0223 mL 0.1116 mL 0.2233 mL 0.5581 mL
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GSK699 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:

GSK6992260944-68-9GSK 699GSK-699PROTACsHistone AcetyltransferaseInterleukin RelatedCXCRTNF ReceptorCD28HATsHATILCXC chemokine receptorsC-X-C motif chemokine receptorsTumor Necrosis Factor ReceptorTNFRKAT2A/B/PCAF/GCN5 PROTAC degraderacute myeloid leukemiasmall cell lung cancerneuroblastomaMOLM-13 cellsNCI-H1048 cellsKELLY neuroblastoma cellsHSPCshuman monocyte-derived dendritic cellsInhibitorinhibitorinhibit

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