{"product_id":"gk444-t82314-targetmol-bhb20444991","title":"GK444","description":"\u003cdiv class=\"bhp-desc\"\u003e\n\u003cstyle\u003e\n.bhp-desc{font-size:16px;color:#1a1a1a;line-height:1.7}\n.bhp-desc h2{font-size:18px;font-weight:700;color:#003366;margin:24px 0 10px;padding-bottom:6px;border-bottom:2px solid #003366}\n.bhp-desc p{margin:0 0 12px}\n.bhp-desc .bhp-spec-table{width:100%;border-collapse:collapse;margin:12px 0 18px}\n.bhp-desc .bhp-spec-table th{width:36%;text-align:left;padding:8px 12px;background:#e8f0fb;color:#003366;font-weight:600;vertical-align:top;border:1px solid #ccd9f0}\n.bhp-desc .bhp-spec-table td{padding:8px 12px;vertical-align:top;border:1px solid #ccd9f0}\n.bhp-desc .bhp-qc-badge{display:inline-block;background:#e6f4ea;color:#1a7a3c;border:1px solid #a8d5b5;border-radius:4px;padding:6px 14px;font-size:14px;font-weight:600}\n.bhp-desc .bhp-warning-box{background:#fff8e6;border-left:4px solid #e6a817;padding:10px 14px;margin:10px 0 14px;border-radius:0 4px 4px 0}\n\u003c\/style\u003e\n\n\u003ch2\u003eCompound Overview\u003c\/h2\u003e\n\u003cp\u003eGK444 (Compound 15a) is a potent and selective inhibitor of histone deacetylase isoforms 1 and 2 (HDAC1\/2), Class I HDAC family members. HDAC1 and HDAC2 are epigenetic regulators that remove acetyl groups from lysine residues on histone tails, compacting chromatin and repressing gene transcription. Dysregulated HDAC1\/2 activity is implicated in oncogenesis, inflammatory fibrosis, immune dysfunction, and DNA damage response, making selective HDAC1\/2 inhibition a well-validated mechanistic approach in epigenetic research.\u003c\/p\u003e\n\u003cp\u003eUnlike pan-HDAC inhibitors (e.g., vorinostat, panobinostat), GK444 selectively targets HDAC1 and HDAC2 with minimal engagement of Class IIa\/IIb isoforms, enabling mechanistic dissection of HDAC1\/2-specific transcriptional programs and fibrotic pathways without broad off-target interference.\u003c\/p\u003e\n\u003cp\u003e\u003cspan class=\"bhp-qc-badge\"\u003e✓ Selective HDAC1\/2 Inhibitor — IC50 100 nM (HDAC1) • 92 nM (HDAC2)\u003c\/span\u003e\u003c\/p\u003e\n\n\u003ch2\u003eKey Specifications\u003c\/h2\u003e\n\u003ctable class=\"bhp-spec-table\"\u003e\n  \u003ctr\u003e\n\u003cth\u003eCatalog No.\u003c\/th\u003e\n\u003ctd\u003eT82314\u003c\/td\u003e\n\u003c\/tr\u003e\n  \u003ctr\u003e\n\u003cth\u003eCompound Name\u003c\/th\u003e\n\u003ctd\u003eGK444 (Compound 15a)\u003c\/td\u003e\n\u003c\/tr\u003e\n  \u003ctr\u003e\n\u003cth\u003eTarget\u003c\/th\u003e\n\u003ctd\u003eHDAC1 \/ HDAC2 (Class I HDAC)\u003c\/td\u003e\n\u003c\/tr\u003e\n  \u003ctr\u003e\n\u003cth\u003eSelectivity\u003c\/th\u003e\n\u003ctd\u003eSelective HDAC1\/2 inhibitor\u003c\/td\u003e\n\u003c\/tr\u003e\n  \u003ctr\u003e\n\u003cth\u003eIC50 – HDAC1\u003c\/th\u003e\n\u003ctd\u003e100 nM\u003c\/td\u003e\n\u003c\/tr\u003e\n  \u003ctr\u003e\n\u003cth\u003eIC50 – HDAC2\u003c\/th\u003e\n\u003ctd\u003e92 nM\u003c\/td\u003e\n\u003c\/tr\u003e\n  \u003ctr\u003e\n\u003cth\u003eCaco-2 Cell Inhibition IC50\u003c\/th\u003e\n\u003ctd\u003e4.1 μM\u003c\/td\u003e\n\u003c\/tr\u003e\n  \u003ctr\u003e\n\u003cth\u003eForm\u003c\/th\u003e\n\u003ctd\u003ePowder\u003c\/td\u003e\n\u003c\/tr\u003e\n  \u003ctr\u003e\n\u003cth\u003ePathway(s)\u003c\/th\u003e\n\u003ctd\u003eChromatin\/Epigenetic · DNA Damage\/DNA Repair · Immune System · Inflammation\u003c\/td\u003e\n\u003c\/tr\u003e\n  \u003ctr\u003e\n\u003cth\u003eStorage (Powder)\u003c\/th\u003e\n\u003ctd\u003e−20 °C for up to 3 years\u003c\/td\u003e\n\u003c\/tr\u003e\n  \u003ctr\u003e\n\u003cth\u003eStorage (In Solvent)\u003c\/th\u003e\n\u003ctd\u003e−80 °C for up to 1 year\u003c\/td\u003e\n\u003c\/tr\u003e\n  \u003ctr\u003e\n\u003cth\u003eShipping\u003c\/th\u003e\n\u003ctd\u003eBlue ice or ambient temperature (per order specifications)\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003c\/table\u003e\n\n\u003ch2\u003eBiological Activity\u003c\/h2\u003e\n\u003cp\u003eGK444 exhibits potent isoform-selective HDAC1\/2 inhibition validated across enzyme, cellular, and in vivo models:\u003c\/p\u003e\n\u003cul\u003e\n  \u003cli\u003e\n\u003cstrong\u003eEnzyme inhibition:\u003c\/strong\u003e IC50 of 100 nM (HDAC1) and 92 nM (HDAC2) in biochemical enzyme assays, confirming nanomolar-range target engagement selectively within Class I HDACs.\u003c\/li\u003e\n  \u003cli\u003e\n\u003cstrong\u003eAntiproliferative activity:\u003c\/strong\u003e IC50 of 4.1 μM in Caco-2 colorectal carcinoma cell inhibition, consistent with HDAC1\/2-dependent regulation of cell cycle and survival genes.\u003c\/li\u003e\n  \u003cli\u003e\n\u003cstrong\u003eAnti-fibrotic activity:\u003c\/strong\u003e Attenuates TGF-β1-induced COL1A1 mRNA upregulation in primary normal human lung fibroblasts, demonstrating on-target activity in a canonical pro-fibrotic signaling model.\u003c\/li\u003e\n  \u003cli\u003e\n\u003cstrong\u003eIn vivo efficacy:\u003c\/strong\u003e Mitigates Bleomycin-induced pulmonary fibrosis in mice [1], providing translational validation in a widely accepted preclinical fibrosis model.\u003c\/li\u003e\n\u003c\/ul\u003e\n\n\u003ch2\u003eSafety \u0026amp; Handling\u003c\/h2\u003e\n\u003cdiv class=\"bhp-warning-box\"\u003e\n\u003cstrong\u003e↓ Research Use Only (RUO):\u003c\/strong\u003e GK444 is supplied for laboratory research purposes only and is not intended for diagnostic or therapeutic use in humans or animals. Consult the Safety Data Sheet (SDS) before handling.\n\u003c\/div\u003e\n\u003cp\u003eGK444 is a synthetic small molecule supplied as dry powder. Avoid inhalation and skin contact. Use appropriate personal protective equipment (PPE) and work in a well-ventilated area when preparing stock solutions in organic solvents (e.g., DMSO). Store desiccated at −20 °C. For in vitro experiments, ensure final DMSO concentration does not exceed 0.1% v\/v to avoid solvent-mediated cytotoxicity.\u003c\/p\u003e\n\u003c\/div\u003e","brand":"TargetMol","offers":[{"title":"5 mg","offer_id":53339500020077,"sku":"T82314-5MG","price":0.0,"currency_code":"USD","in_stock":false},{"title":"50 mg","offer_id":53339654291821,"sku":"T82314-50MG","price":0.0,"currency_code":"USD","in_stock":false}],"url":"https:\/\/www.ebiohippo.com\/products\/gk444-t82314-targetmol-bhb20444991","provider":"BioHippo","version":"1.0","type":"link"}