Sirtuin Inhibitor

By Targets:	Sirtuin (19) Apoptosis (4) Autophagy (1) c-Myc (1) HBV (1) Histone Methyltransferase (1) HSP (1) Keap1-Nrf2 (1) Ligands for Target Protein for PROTAC (1) Parasite (3) Phosphatase (2) Reverse Transcriptase (2) SARS-CoV (3) Topoisomerase (2)
By Research Areas:	Cancer (15) Cardiovascular Disease (3) Infection (4) Inflammation/Immunology (2) Metabolic Disease (3) Neurological Disease (2)
Click Chemistry:	Alkynes (1)

Targets Recommended: Sirtuin

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-156781

Sirtuin-1 inhibitor 1	Sirtuin	Metabolic Disease
Sirtuin-1 inhibitor 1 (Compound 8) is an inhibitor of *Sirtuin*-1 that plays important roles in obesity-induced diabetes and aging-related diseases .

HY-124113

4'-Bromo-resveratrol 4′‐BR	Sirtuin Apoptosis	Cancer
4'-Bromo-resveratrol is a potent and dual inhibitor *Sirtuin-1* and *Sirtuin-3. 4'-Bromo-resveratrol inhibits* melanoma cell growth through mitochondrial metabolic reprogramming. 4'-Bromo-resveratrol imparts antiproliferative effects in melanoma cells through a metabolic reprogramming and affecting the cell cycle and apoptosis signaling .

HY-155725

Z26395438

Sirtuin Others

Z26395438 (compound 1) is a potent Sirtuin-1 inhibitor, with an IC₅₀ value of 1.6 μM .
HY-149524

SIRT5 inhibitor 8

Sirtuin Cancer

SIRT5 inhibitor 8 (compound 10) is a competitive inhibitor (IC₅₀: 5.38 μM) of sirtuin SIRT5 with anticancer potential .
HY-149525

SIRT5 inhibitor 9

Sirtuin Cancer

SIRT5 inhibitor 9 (compound 14) is a competitive inhibitor (IC₅₀: 4.07 μM) of sirtuin SIRT5 with anticancer potential .
HY-112587

MC3482

3 Publications Verification

Sirtuin Cancer

MC3482 is a specific sirtuin5 (SIRT5) inhibitor.

Z26395438	Sirtuin	Others
Z26395438 (compound 1) is a potent Sirtuin-1 inhibitor, with an IC₅₀ value of 1.6 μM .

SIRT5 inhibitor 8	Sirtuin	Cancer
SIRT5 inhibitor 8 (compound 10) is a competitive inhibitor (IC₅₀: 5.38 μM) of sirtuin SIRT5 with anticancer potential .

SIRT5 inhibitor 9	Sirtuin	Cancer
SIRT5 inhibitor 9 (compound 14) is a competitive inhibitor (IC₅₀: 4.07 μM) of sirtuin SIRT5 with anticancer potential .

MC3482 3 Publications Verification	Sirtuin	Cancer
MC3482 is a specific sirtuin5 (SIRT5) inhibitor.

HY-163316

SIRT4-IN-1	Sirtuin	Metabolic Disease Cancer
SIRT4-IN-1 (compound 69) is selective sirtuin 4 (Sirt4) inhibitor with an IC₅₀ of 16 μM.SIRT4-IN-1 shows no relevant effects on other sirtuin isoforms .

HY-112634

SIRT5 inhibitor 1

5 Publications Verification

Sirtuin Others

SIRT5 inhibitor 1 is a potent Human Sirtuin 5 deacylase inhibitor, with an IC₅₀ of 0.11 μM.
HY-112427

Sirt2-IN-1

Sirtuin Inflammation/Immunology Cancer

Sirt2-IN-1 (Compound 9) is a sirtuin 2 (Sirt2) inhibitor with an IC₅₀ of 163 nM .
HY-108986

JFD00244

Sirtuin SARS-CoV Cancer

JFD00244 is a sirtuin 2 (SIRT2) inhibitor, with anti-tumor effect. JFD00244 is also a Nsp-16 inhibitor against SARS-CoV-2 .

SIRT5 inhibitor 1 5 Publications Verification	Sirtuin	Others
SIRT5 inhibitor 1 is a potent Human Sirtuin 5 deacylase inhibitor, with an IC₅₀ of 0.11 μM.

Sirt2-IN-1	Sirtuin	Inflammation/Immunology Cancer
Sirt2-IN-1 (Compound 9) is a sirtuin 2 (Sirt2) inhibitor with an IC₅₀ of 163 nM .

JFD00244	Sirtuin SARS-CoV	Cancer
JFD00244 is a sirtuin 2 (SIRT2) inhibitor, with anti-tumor effect. JFD00244 is also a Nsp-16 inhibitor against SARS-CoV-2 .

HY-13515

Sirtinol Maximum Cited Publications 13 Publications Verification	Sirtuin Autophagy Apoptosis	Cancer
Sirtinol is a **sirtuin (SIRT)** inhibitor, with IC₅₀s of 48 μM, 57.7 μM and 131 μM for ySir2, hSIRT2 and hSIRT2, respectively .

HY-122936

Tanshindiol C	Histone Methyltransferase Keap1-Nrf2 Sirtuin	Cardiovascular Disease Cancer
Tanshindiol C is a S-adenosylmethionine-competitive EZH2 (Histone Methyltransferase) inhibitor with an IC₅₀ of 0.55 μM for inhibiting the methyltransferase activity. Tanshindiol C is also an activator of both Nrf2 and **Sirtuin 1 (Sirt1)** in macrophages. Tanshindiol C possesses anti-cancer activity, and can be used for atherosclerosis research .

HY-119857

AGK7 SIRT2 Inhibitor,Inactive Control	Sirtuin	Neurological Disease
AGK7 is a potent inhibitor of sirtuin 2 (SIRT2). AGK7 rescues alpha-synuclein toxicity and modified inclusion morphology in a cellular model of Parkinson's disease. AGK7 protects against dopaminergic cell death both in vitro and in a Drosophila model of Parkinson's disease .

HY-139144

YM-08

Sirtuin HSP Neurological Disease Cancer

YM-08 (Compounds 7a) is a brain-penetrant inhibitors of SIRT2,with the IC₅₀ of 19.9 μM. YM-08 also is inhibitor of Hsp70 .

YM-08	Sirtuin HSP	Neurological Disease Cancer
YM-08 (Compounds 7a) is a brain-penetrant inhibitors of *SIRT2*,with the IC₅₀ of 19.9 μM. YM-08 also is inhibitor of Hsp70 .

HY-107454

OSS_128167 Maximum Cited Publications 13 Publications Verification	Sirtuin HBV	Infection Metabolic Disease Inflammation/Immunology Cancer
OSS_128167 is a potent selective **sirtuin 6 (SIRT6)** inhibitor with IC₅₀s of 89 μM, 1578 μM and 751 μM for *SIRT6, SIRT1 and SIRT2, respectively. OSS_128167 has anti-HBV* activity that inhibits HBV transcription and replication. OSS_128167 has anti-cancer, anti-inflammation and anti-viral effects .

HY-111522

RK-9123016	Sirtuin c-Myc	Cancer
RK-9123016 is a potent inhibitor of SIRT2. RK-9123016 inhibits the enzymatic activity of SIRT2 with an IC₅₀ value of 0.18 µM but not other human sirtuin members including SIRT1 and SIRT3 at 100 µM. RK-9123016 increases the acetylation level of eukaryotic translation initiation factor 5A (eIF5A), a physiological substrate of SIRT2, and reduces cell viability of human breast cancer cells accompanied with a decrease in c-Myc expression .

HY-B0879

Suramin	Phosphatase Sirtuin Reverse Transcriptase Topoisomerase SARS-CoV Parasite Apoptosis	Infection Cardiovascular Disease Cancer
Suramin is a reversible and competitive protein-tyrosine phosphatases (PTPases) inhibitor . Suramin is a potent inhibitor of *sirtuins: SirT1 (IC₅₀=297 nM), SirT2 (IC₅₀=1.15 μM), and SirT5 (IC₅₀=22 μM) . Suramin is a competitive inhibitor* of reverse transcriptase (DNA topoisomerase II: IC₅₀=5 μM) . Suramin is a potent SARS-CoV-2 RNA-dependent RNA polymerase (RdRp) inhibitor .Suramin efficiently inhibits IP5K and is an antiparasitic, anti-neoplastic and anti-angiogenic agent .

HY-W020111

7-Chloro-4-(piperazin-1-yl)quinoline	Sirtuin Parasite	Infection
7-Chloro-4-(piperazin-1-yl)quinolone is an important scaffold in medicinal chemistry. 7-Chloro-4-(piperazin-1-yl)quinolone is a potent *sirtuin* inhibitor and also inhibits the serotonin uptake (IC₅₀ of 50 μM). 7-Chloro-4-(piperazin-1-yl)quinolone exhibits antimalarial activity on D10 and K1 strains of *P. falciparum* with IC₅₀s of 1.18 μM and 0.97 μM, respectively .

HY-B0879A

Suramin sodium salt Maximum Cited Publications 13 Publications Verification Suramin hexasodium salt	Phosphatase Sirtuin Reverse Transcriptase Topoisomerase SARS-CoV Parasite Apoptosis	Infection Cardiovascular Disease Cancer
Suramin sodium salt (Suramin hexasodium salt) is a reversible and competitive protein-tyrosine phosphatases (PTPases) inhibitor . Suramin sodium salt is a potent inhibitor of *sirtuins: SirT1 (IC₅₀=297 nM), SirT2 (IC₅₀=1.15 μM), and SirT5 (IC₅₀=22 μM) . Suramin sodium salt is a competitive inhibitor* of reverse transcriptase (DNA topoisomerase II: IC₅₀=5 μM) . Suramin sodium salt is a potent SARS-CoV-2 RNA-dependent RNA polymerase (RdRp) inhibitor . Suramin sodium salt efficiently inhibits IP5K and is an antiparasitic, anti-neoplastic and anti-angiogenic agent .

HY-107453

SirReal1-O-propargyl PROTAC Sirt2-binding moiety 1	Ligands for Target Protein for PROTAC	Cancer
SirReal1-O-propargyl is a selective and highly potent **Sirtuin 2 (Sirt2)** inhibitor, with an IC₅₀ of 2.4 μM. SirReal1-O-propargyl, the SirReal1-based moiety, binds to the cereblon ligand via a linker to form PROTAC to degrade Sirt2 . SirReal1-O-propargyl is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Cat. No.	Product Name

HY-L024

Histone Modification Research Compound Library	629 compounds
A histone modification, a covalent post-translational modification (PTM) to histone proteins, includes methylation, phosphorylation, acetylation, ubiquitylation, and sumoylation, etc. In general, histone modifications are catalyzed by specific enzymes that act predominantly at the histone N-terminal tails involving amino acids such as lysine or arginine, as well as serine, threonine, tyrosine, etc. The PTMs made to histones can impact gene expression by altering chromatin structure or recruiting histone modifiers. Histone modifications act in diverse biological processes such as transcriptional activation/inactivation, chromosome packaging, and DNA damage/repair. Deregulation of histone modification contributes to many diseases, including cancer and autoimmune diseases. MCE owns a unique collection of 629 bioactive compounds targeting Epigenetic Reader Domain, HDAC, Histone Acetyltransferase, Histone Demethylase, Histone Methyltransferase, Sirtuin, etc. Histone Modification Research Compound Library is a useful tool for histone modification research and drug screening.

Histone Modification Research Compound Library

629 compounds

A histone modification, a covalent post-translational modification (PTM) to histone proteins, includes methylation, phosphorylation, acetylation, ubiquitylation, and sumoylation, etc. In general, histone modifications are catalyzed by specific enzymes that act predominantly at the histone N-terminal tails involving amino acids such as lysine or arginine, as well as serine, threonine, tyrosine, etc. The PTMs made to histones can impact gene expression by altering chromatin structure or recruiting histone modifiers. Histone modifications act in diverse biological processes such as transcriptional activation/inactivation, chromosome packaging, and DNA damage/repair. Deregulation of histone modification contributes to many diseases, including cancer and autoimmune diseases.

MCE owns a unique collection of 629 bioactive compounds targeting Epigenetic Reader Domain, HDAC, Histone Acetyltransferase, Histone Demethylase, Histone Methyltransferase, Sirtuin, etc. Histone Modification Research Compound Library is a useful tool for histone modification research and drug screening.

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-122936

Tanshindiol C	Structural Classification Terpenoids Labiatae Samanea saman (Jacq.) Merr. Diterpenoids Plants	Histone Methyltransferase Keap1-Nrf2 Sirtuin
Tanshindiol C is a S-adenosylmethionine-competitive EZH2 (Histone Methyltransferase) inhibitor with an IC₅₀ of 0.55 μM for inhibiting the methyltransferase activity. Tanshindiol C is also an activator of both Nrf2 and **Sirtuin 1 (Sirt1)** in macrophages. Tanshindiol C possesses anti-cancer activity, and can be used for atherosclerosis research .

Cat. No.	Product Name		Classification

HY-107453

SirReal1-O-propargyl PROTAC Sirt2-binding moiety 1		Alkynes
SirReal1-O-propargyl is a selective and highly potent **Sirtuin 2 (Sirt2)** inhibitor, with an IC₅₀ of 2.4 μM. SirReal1-O-propargyl, the SirReal1-based moiety, binds to the cereblon ligand via a linker to form PROTAC to degrade Sirt2 . SirReal1-O-propargyl is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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