1. Cell Cycle/DNA Damage Epigenetics
  2. HDAC
  3. GK444

GK444 (Compound 15a) is a HDAC1/2 inhibitor (IC50: 100 and 92 nM for HDAC1/2 respectively). GK444 inhibits Caco-2 cells with IC50 of 4.1 μM. GK444 also reduces TGF-β1 induced COL1A1 mRNA levels in primary normal human lung fibroblasts. GK444 inhibits Bleomycin (HY-108345)-induced lung fibrosis in mice.

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GK444

GK444 Chemical Structure

CAS No. : 3032392-39-2

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Description

GK444 (Compound 15a) is a HDAC1/2 inhibitor (IC50: 100 and 92 nM for HDAC1/2 respectively). GK444 inhibits Caco-2 cells with IC50 of 4.1 μM. GK444 also reduces TGF-β1 induced COL1A1 mRNA levels in primary normal human lung fibroblasts. GK444 inhibits Bleomycin (HY-108345)-induced lung fibrosis in mice[1].

IC50 & Target

100 and 92 nM for HDAC1/2[1].

Cellular Effect
Cell Line Type Value Description References
A549 IC50
6.8 μM
Compound: 15a; GK444
Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 37795958]
Caco-2 IC50
1.9 μM
Compound: 15a; GK444
Antiproliferative activity against human Caco-2 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human Caco-2 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 37795958]
SF-268 IC50
4.8 μM
Compound: 15a; GK444
Antiproliferative activity against human SF-268 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human SF-268 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 37795958]
Molecular Weight

548.63

Formula

C33H32N4O4

CAS No.
SMILES

O=C([C@@H]1CCC(N1CC2=CC=CC=C2)=O)NCC3=CC=C(OCC4=CC=C(C(NC5=CC=CC=C5N)=O)C=C4)C=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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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.

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Product Name:
GK444
Cat. No.:
HY-155328
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