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You are here:Home-Inhibitors & Agonists-Epigenetics-HDAC

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HDAC (Histone deacetylases) are a class of enzymes that remove acetyl groups (O=C-CH3) from an ε-N-acetyl lysine amino acid on ahistone, allowing the histones to wrap the DNA more tightly. This is important because DNA is wrapped around histones, and DNA expression is regulated by acetylation and de-acetylation. Its action is opposite to that of histone acetyltransferase. HDAC proteins are now also called lysine deacetylases (KDAC), to describe their function rather than their target, which also includes non-histone proteins. Together with the acetylpolyamine amidohydrolases and the acetoin utilization proteins, the histone deacetylases form an ancient protein superfamily known as the histone deacetylase superfamily.

Cat. No. Product Name CAS No. Information
GY02457

ACY-738

1375465-91-0

ACY-738 (ACY738) is a potent and specific HDAC6 inhibitor (IC50=1.7 nM) with improved brain bioavailability; displays 60-1500 fold selectivity over class I HDACs; induces dramatic increase in α-tubulin acetylation in brain and stimulates mouse exploratory behaviors; increases the innervation of the neuromuscular junctions in the gastrocnemius muscle and improves the motor and sensory nerve conduction in the mutant HSPB1-induced CMT2 mouse model.

GY07008

trans CM-414

1624792-73-9

trans CM-414 is a first-in-class, dual inhibitor of PDE5 and HDAC that inhibits HDAC1/2/3/6 (IC50=310/490/322/91 nM, respectively) and PDE5 (IC50=60 nM); does not inhibit class IIa HDAC isoforms, MMP-3, MMP-10, and PDE9 (IC50>10 uM), has modest or weak activity for HDAC8/11/10 (IC50=640/550/2400 nM); diminishes brain Aβ and pTau levels, increases the inactive form of GSK3β, reverts the decrease in dendritic spine density on hippocampal neurons, and reverses the cognitive deficits in Tg2576 mice.

GY07007

cis CM-414

1624792-70-6

cis CM-414 is a first-in-class, dual inhibitor of PDE5 and HDAC that inhibits HDAC1/2/3/6 (IC50=310/490/322/91 nM, respectively) and PDE5 (IC50=60 nM); does not inhibit class IIa HDAC isoforms, MMP-3, MMP-10, and PDE9 (IC50>10 uM), has modest or weak activity for HDAC8/11/10 (IC50=640/550/2400 nM); diminishes brain Aβ and pTau levels, increases the inactive form of GSK3β, reverts the decrease in dendritic spine density on hippocampal neurons, and reverses the cognitive deficits in Tg2576 mice.

GY07006

CM-414

2007971-51-7

CM-414 is a first-in-class, dual inhibitor of PDE5 and HDAC that inhibits HDAC1/2/3/6 (IC50=310/490/322/91 nM, respectively) and PDE5 (IC50=60 nM); does not inhibit class IIa HDAC isoforms, MMP-3, MMP-10, and PDE9 (IC50>10 uM), has modest or weak activity for HDAC8/11/10 (IC50=640/550/2400 nM); diminishes brain Aβ and pTau levels, increases the inactive form of GSK3β, reverts the decrease in dendritic spine density on hippocampal neurons, and reverses the cognitive deficits in Tg2576 mice.

GY06952

SB-429201

1027971-34-1

SB-429201 is a potent, selective HDAC1 inhibitor with IC50 of 1.5 uM; increases histone acetylation in SW620 cells.

GY06951

SB-379278A

146366-04-3

SB-379278A is a potent and selective HDAC8 inhibitor with IC50 of 0.5 uM.

GY06950

NCC-149

1316652-41-1

NCC-149 is a potent and selective HDAC8 inhibitor with IC50 of 70 nM; displays high selectivity over major HDACs (HDAC1: IC50 38 uM, HDAC2 >100 uM, HDAC4: IC50: 44 uM,HDAC6: IC50 2.4 uM).

GY06949

HDAC8-IN-20a

1884231-52-0

HDAC8-IN-20a is a potent, selective HDAC8 inhibitor with IC50 of 27 nM; efficiently blocks the activation of growth receptor survival signaling and shifts the cell cycle arrest and differentiation phenotype toward effective cell death of neuroblastoma cell lines combined with crizotinib, efficiently kills neuroblastoma cell lines carrying wildtype ALK, amplified ALK and those carrying the activating ALK F1174L mutation, as well as cells carrying the activating R1275Q mutation.

GY10082

Class I and IIB HDAC inhibitor 42

2245323-24-2

Class I and IIB HDAC inhibitor 42 is a novel potent, selective class I and IIB inhibitor (HDAC1 Ki=0.27 nM) for topical treatment of cutaneous t-cell lymphoma.

GY10173

RTS-V5

RTS-V5 (Dual HDAC-proteasome inhibitor RTS-V5) is the first-in-class, dual HDAC-proteasome inhibitor with IC50 of 0.27 uM (HDAC6), inhibits HDAC8 (IC50=0.53 uM), and low activity against HDAC/1/2/3; demonstrates cytotoxicity against leukemia and multiple myeloma cell lines as well as therapy-refractory primary patient-derived leukemia cells.

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