HDAC Inhibitor

HDAC6-IN-29 (compound 11g), hydroxamic analogue, is a HDAC6 inhibitor. HDAC6-IN-29 has potent antiproliferative activity against CAL-51 cells (IC₅₀ = 1.17 μM) and is able to induce apoptosis and cause accumulation of cells in the S phase of the cell cycle. HDAC6-IN-29 can be used for the research of cancer.

HDAC-IN-33 is a potent HDAC inhibitor with IC₅₀s of 24, 46, and 47 nM for HDAC1, HDAC2 and HDAC6, respectively. HDAC-IN-33 possesses potent antiproliferation activities against tumor cells. HDAC-IN-33 shows potent antitumor efficacy in vivo That trigger antitumor immunity.

Hdac9 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Hdac9 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

HDAC6-IN-16 (compound 5c) is a histone deacetylase 6 (HDAC6) inhibitor, based on Quinazolin-4(3H)-One. HDAC6-IN-16 exhibits anticancer effect, inhibits colony-forming. And HDAC6-IN-16 arrests cell cycle at G2 phase and induces apoptosis.

Rodin-A is an orally active, brain-penetrant and selective histone deacetylase (HDAC)-co-repressor of repressor element-1 silencing transcription factor (CoREST) complex inhibitor with an IC₅₀ value of 1.80 μM for the CoREST complex, 0.15 μM for HDAC1, and 0.43 μM for HDAC2. Rodin-A increases the acetylation level of histone H3K9, upregulates the expression of neuron-related genes, thereby promoting the increase in dendritic spine density, the colocalization of synaptic proteins (SV2A and PSD95), and the improvement of hippocampal long-term potentiation (LTP), exerting synaptic protection and repair activity. Rodin-A is promising for research of neurodegenerative diseases related to synaptic dysfunction, especially Alzheimer’s disease.

HDAC6-IN-67 is a selective HDAC6 inhibitor (IC50 = 17.15 nM) that exhibits 19-fold selectivity over HDAC1. HDAC6-IN-67 selectively inhibits HDAC6 by interacting with Ser531 and His614. HDAC6-IN-67 induces apoptosis by inducing the cleavage of caspases 9, 8, 3, and PARP, upregulating Bax expression, and downregulating Bcl-2 expression. HDAC6-IN-67 effectively induces the acetylation of α-tubulin, without affecting histone H3 acetylation in MCF-7/ADR cells. HDAC6-IN-67 can be used for the study of breast cancer.

Antitumor agent-123 (Copmound 4d) effectively inhibits multiple kinase targets with anti-cancer effects, including JAK2, JAK3, HDAC1 and HDAC6, with IC₅₀ values of 34.6 and 2.6 μM for JAK2 and JAK3, respectively. Antitumor agent-123 exhibits moderate activity in solid tumor models.

Santacruzamate A (Standard) is the analytical standard of Santacruzamate A. This product is intended for research and analytical applications. Santacruzamate A (CAY-10683, STA) is a potent and selective HDAC2 inhibitor with an IC50 of 119 pM. STA also exerts neuroprotective property against amyloid-β protein fragment 25–35. STA can be used for cancer and neurological disease research[1][2].

Hdac3 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Hdac3 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

HDAC6-IN-55 (Compound 15B) is a potent HDAC6 inhibitor and an effective anti-inflammatory agent. HDAC6-IN-55 alleviates atopic dermatitis through anti-inflammatory effects facilitated via TLR4/MAPK, STAT3 and NF-κB pathways. HDAC6-IN-55 alleviates symptoms such as skin edema, dryness, crusting, and peeling in 2,4-dinitrochlorobenzene (DNCB)-induced atopic dermatitis mice.

Daphnegiravone D (compound 70) is an HDAC6 inhibitor with anti-hepatocellular carcinoma activity. Daphnegiravone D can induce apoptosis and selectively inhibit the proliferation of liver cancer cells through the p38 and JNK MAPK pathways.

HDAC-IN-101 is a HDAC1 inhibitor and nitroreductase/pH-activated fluorescent inducer, with an IC₅₀ of 65 nM against human HDAC1. HDAC-IN-101 blocks cancer cell proliferation by inhibiting HDAC1. HDAC-IN-101 is reduced by overexpressed nitroreductase to generate H6AQ (Ex/Em = 450 nm/500 nm), a product that emits fluorescence under low pH conditions. HDAC-IN-101 is applicable for cancer-related research.

Apicidin C (Compound 5a) is a cyclic tetrapeptide. Apicidin C has an antiprotozoal and antimalarial activity against Eimeria tenella (IC₅₀: 6 nM) by reversibly inhibiting HDAC acyivity. Apicidin C can be used for malaria infections research.

TH34 (Standard) is the analytical standard of TH34 (HY-111818). This product is intended for research and analytical applications. TH34, an HDAC6/8/10 inhibitor with IC₅₀s of 4.6 μM, 1.9 μM, and 7.7 μM respectively, shows high selectivity over HDAC1/2/3.

RGFP966 (Standard) is the analytical standard of RGFP966 (HY-13909). This product is intended for research and analytical applications. RGFP966 is a highly selective HDAC3 inhibitor with an IC₅₀ of 80 nM and shows no inhibition to other HDACs at concentrations up to 15 μM. RGFP966 can penetrate the blood brain barrier (BBB).

Givinostat (hydrochloride) (Standard) is the analytical standard of Givinostat (hydrochloride). This product is intended for research and analytical applications. Givinostat (ITF-2357) hydrochloride is a HDAC inhibitor with an IC50 of 198 and 157 nM for HDAC1 and HDAC3, respectively.

Splitomicin (Standard) is the analytical standard of Splitomicin. This product is intended for research and analytical applications. Splitomicin (Splitomycin) is a selective Sir2p inhibitor. Splitomicin inhibits NAD+-dependent HDAC activity of Sir2 protein. Splitomicin induces dose-dependent inhibition of HDAC in the yeast extract with an IC50 of 60 μM.

ACY-1083 (Standard) is the analytical standard of ACY-1083 (HY-111791). This product is intended for research and analytical applications. ACY-1083 is a selective and brain-penetrating HDAC6 inhibitor with an IC₅₀ of 3 nM and is 260-fold more selective for HDAC6 than all other classes of HDAC isoforms. ACY-1083 effectively reverses chemotherapy-induced peripheral neuropathy.

MC1742 (Standard) is the analytical standard of MC1742 (HY-110280). This product is intended for research and analytical applications. MC1742 is a potent HDAC inhibitor, with IC₅₀s of 0.1 μM, 0.11 μM, 0.02 μM, 0.007 μM, 0.61 μM, 0.04 μM and 0.1 μM for HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, HDAC10 and HDAC11, respectively. MC1742 can increase acetyl-H3 and acetyl-tubulin levels and inhibits cancer stem cells growth. MC1742 can induce growth arrest, apoptosis, and differentiation in sarcoma CSC.

KT-531 is a potent and selective inhibitor of HDAC6 with an IC₅₀ of 8.5 nM. KT-531 exhibits strong inhibition against SUP-T11 cells with an IC₅₀ of 0.42 μM. KT-531 can be used in study hematological cancers.