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Phosphorylases inhibitor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Adenosine Kinase (1) Antibiotic (2) Apoptosis (3) Bacterial (2) DNA/RNA Synthesis (2) Endogenous Metabolite (1) Fungal (1) HIV (2) Influenza Virus (1) Methionine Adenosyltransferase (MAT) (1) Nucleoside Antimetabolite/Analog (10) Orthopoxvirus (1) Phosphatase (2) PKA (3) PKC (3) Thymidylate Synthase (2)
By Research Areas:	Cancer (19) Endocrinology (1) Infection (6) Inflammation/Immunology (3) Metabolic Disease (6)

Inhibitors & Agonists

Screening Libraries

Biochemical Assay Reagents

Peptides

Natural
Products

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-B0307

Idoxuridine 3 Publications Verification 5-Iodo-2′-deoxyuridine; 5-IUdR; IdUrd	Phosphatase Orthopoxvirus	Infection Cancer
Idoxuridine (5-Iodo-2′-deoxyuridine, 5-IUdR, IdUrd) is an iodinated thymidine analogue that competitively inhibits *phosphorylases. Idoxuridine can inhibit* viral activity, particularly viral eye infections, including herpes simplex keratitis, by inhibiting DNA polymerase and affecting viral replication. Idoxuridine against feline herpesvirus has the IC₅₀ value of 4.3 μM . Idoxuridine shows anti-orthopoxvirus activity.

HY-A0063A

Tipiracil

5 Publications Verification

Thymidylate Synthase Nucleoside Antimetabolite/Analog Cancer

Tipiracil is a thymidine phosphorylase (TPase) inhibitor.

Tipiracil 5 Publications Verification	Thymidylate Synthase Nucleoside Antimetabolite/Analog	Cancer
Tipiracil is a thymidine phosphorylase (TPase) inhibitor.

HY-19396

Ingliforib CP 368296; GPi 296
Ingliforib (CP 368296) is a glycogen phosphorylase inhibitor, with IC₅₀s of 52, 352 and 150 nM for liver, muscle and brain glycogen phosphorylase, and has cardioprotective activity.

HY-B0307A

Idoxuridine hydrate 5-Iodo-2′-deoxyuridine hydrate; 5-IUdR hydrate; IdUrd hydrate	Phosphatase	Infection
Idoxuridine (5-Iodo-2′-deoxyuridine, 5-IUdR, IdUrd) hydrate is an iodinated thymidine analogue that competitively inhibits *phosphorylases. Idoxuridine can inhibit* viral activity, particularly viral eye infections, including herpes simplex keratitis, by inhibiting DNA polymerase and affecting viral replication. Idoxuridine against feline herpesvirus has the IC₅₀ value of 4.3 μM .

HY-128029

Glycogen phosphorylase-IN-1	Others	Metabolic Disease
Glycogen phosphorylase-IN-1 (Compound 42) is an inhibitor for human liver glycogen phosphorylase (hlGPa) and hepatocyte glycogen-derived glucose production with IC₅₀s of 53 and 380 nM, respectively. Glycogen phosphorylase-IN-1 reveals efficacy towards type 2 diabetes .

HY-A0063

Tipiracil hydrochloride 5 Publications Verification	Nucleoside Antimetabolite/Analog	Cancer
Tipiracil (hydrochloride) is a thymidine phosphorylase inhibitor (TPI), used for cancer research.

HY-100320

AVE5688	Others	Metabolic Disease
AVE5688 is an inhibitor of *glycogen phosphorylase* (GP), with IC₅₀s of 430 nM and 915 nM and K_d*s of 170 nM and 530 nM for rabbit muscle glycogen phosphorylase* (rmGPb and rmGPa, respectively); AVE5688 can be used for the research of type 2 diabetes.

HY-101496

MT-DADMe-ImmA 2 Publications Verification MTDIA; Methylthio-DADMe-Immucillin A	Others	Cancer
MT-DADMe-ImmA is an inhibitor of human 5'-methylthioadenosine phosphorylase (MTAP) with a K_i of 90 pM.

HY-108615

CP-316819 GPi 819	Others	Endocrinology
CP 316819 is a potent *glycogen phosphorylase* (GPase)** inhibitor with antihyperglycemic effect (IC₅₀ values are 17 and 34 nM against human skeletal muscle glycogen phosphorylase (huSMGPa) and liver glycogen phosphorylase (huLGPa) respectively).CP 316819 causes glycogen accumulation under normoglycemic conditions but permits glycogen utilization when glucose concentrations are low.CP-316819 prevents neuronal cell death and maintains brain electrical currents .

HY-W008638

2'-Deoxyinosine 1 Publications Verification	Endogenous Metabolite	Metabolic Disease Cancer
2’-deoxyadenosine inhibits the growth of human colon-carcinoma cell lines and is found to be associated with purine nucleoside phosphorylase (PNP) deficiency.

HY-19480

Ulodesine BCX4208
Ulodesine is a *purine nucleoside phosphorylase* (PNP)** inhibitor. Ulodesine inhibits PNP with IC₅₀ value of 2.293 nM/L. Ulodesine can be used for the research of hyporucicemia .

HY-15424

5-Iodotubercidin 5+ Cited Publications NSC 113939; 5-ITu	Adenosine Kinase	Cancer
5-Iodotubercidin (NSC 113939), an ATP mimetic, is a potent adenosine kinase inhibitor with an IC₅₀ of 26 nM. 5-Iodotubercidin (NSC 113939) initiates glycogen synthesis in isolated hepatocytes by causing inactivation of phosphorylase and activation of glycogen synthase. 5-Iodotubercidin (NSC 113939) also inhibits CK1, insulin receptor tyrosine kinase, phosphorylase kinase, PKA, CK2, PKC and Haspin .

HY-147969

Antiangiogenic agent 2	Nucleoside Antimetabolite/Analog	Cancer
Antiangiogenic agent 2 (compound 3b) is a potent thymidine phosphorylase inhibitor, with an IC₅₀ of 39.71 μM. Antiangiogenic agent 2 shows anti-angiogenic activity .

HY-118047

CI 972 anhydrous	Nucleoside Antimetabolite/Analog	Inflammation/Immunology
CI 972 anhydrous is a potent, orally active, and competitive inhibitor of *purine nucleoside phosphorylase* (PNP) (K_i**=0.83 μM) under development as a T cell-selective immunosuppressive agent .

HY-13525

CP-91149 2 Publications Verification	Others	Metabolic Disease Cancer
CP-91149 is a GP (glycogen phosphorylase) inhibitor. CP-91149 promotes glycogen resynthesis, but not its overaccumulation. CP-91149 has the potential for Type II (insulin-dependent) diabetes study .

HY-W010854

2'-Deoxyadenosine 5'-di-phos-phate disodium dADP disodium	DNA/RNA Synthesis	Others
2'-Deoxyadenosine 5'-di-phos-phate disodium (dADP disodium) is an inhibitor of bacterial poly(A) polymerase. It can be used to synthesize deoxyadenosine oligonucleotides with Escherichia coli polynucleotide phosphorylase and other enzymes .

HY-106406

Benzylacyclouridine BAU; 5-Benzylacyclouridine	Others	Cancer
Benzylacyclouridine (BAU) is a potent and specific inhibitor of uridine phosphorylase, the first enzyme in the catabolism of uridine. Benzylacyclouridine can modulate the cytotoxic side effects of 5-fluorouracil (5-FU) and its derivatives .

HY-15141

Staurosporine Maximum Cited Publications 89 Publications Verification Antibiotic AM-2282; STS; AM-2282	PKC PKA Apoptosis Bacterial Fungal Antibiotic	Infection Cancer
Staurosporine is a potent, ATP-competitive and non-selective inhibitor of protein kinases with IC₅₀s of 6 nM, 15 nM, 2 nM, and 3 nM for PKC, PKA, c-Fgr, and Phosphorylase kinase respectively. Staurosporine also inhibits TAOK2 with an IC₅₀ of 3 μM. Staurosporine is an apoptosis inducer .

HY-111926

N6-Methyladenosine 5'-monophosphate disodium salt	Others	Metabolic Disease
N6-Methyladenosine 5'-monophosphate disodium salt is an activator of *glycogen phosphorylase* b, with a K_a** value of 22 µM . N6-Methyladenosine 5'-monophosphate disodium salt is a non-competitive rat adenylate kinase II inhibitor .

HY-102071

KIN59 5'-O-Tritylinosine; 5'-O-Trityl-inosine	Nucleoside Antimetabolite/Analog	Cancer
KIN59 (5’-O-Tritylinosine) is a potent thymidine phosphorylase allosteric inhibitor. KIN59 inhibits FGF2-stimulated cell growth. KIN59 inhibits the expression of p-FGFR1, P-Akt in FGF2 (10 ng/mL) stimulated cells. KIN59 shows anti-tumor activity .

HY-100126

Tubercidin 4 Publications Verification 7-Deazaadenosine	Bacterial DNA/RNA Synthesis Influenza Virus Antibiotic	Infection
Tubercidin (7-Deazaadenosine) is an antibiotic obtained from Streptomyces tubercidicus. Tubercidin inhibits the growth of Streptococcus faecalis (8043) with an IC₅₀ of 0.02 μM . Tubercidin inhibits polymerases by incorporating DNA or RNA, thereby inhibiting DNA replication, RNA and protein synthesis . Tubercidin is a weak inhibitor of adenosine phosphorylase, and interferes with the phosphorylation of adenosine and AMP . Tubercidin has antiviral activity .

HY-16209

Forodesine hydrochloride 10+ Cited Publications BCX-1777 hydrochloride; Immucillin-H hydrochloride	Nucleoside Antimetabolite/Analog Apoptosis	Cancer
Forodesine hydrochloride (BCX-1777 hydrochloride) is a highly potent and orally active *purine nucleoside phosphorylase* (PNP)** inhibitor with IC₅₀ values ranging from 0.48 to 1.57 nM for human, mouse, rat, monkey and dog PNP. Forodesine hydrochloride is a potent human lymphocyte proliferation inhibitor. Forodesine hydrochloride could induce apoptosis in leukemic cells by increasing the dGTP levels .

HY-16210

Forodesine 10+ Cited Publications BCX-1777; Immucillin-H	Nucleoside Antimetabolite/Analog Apoptosis	Cancer
Forodesine (BCX-1777) is a highly potent and orally active *purine nucleoside phosphorylase* (PNP)** inhibitor with IC₅₀ values ranging from 0.48 to 1.57 nM for human, mouse, rat, monkey and dog PNP. Forodesine is a potent human lymphocyte proliferation inhibitor. Forodesine could induce apoptosis in leukemic cells by increasing the dGTP levels .

HY-108614

GPi688	Others	Metabolic Disease
GPi688 is a potent and orally active *glycogen phosphorylase* (GPa)** inhibitor with IC₅₀s of 19 nM, 61 nM and 12 nM for human liver GPa, rat liver GPa and human skeletal muscle GPa, respectively . GPi688 can inhibit glucagons-mediated glucose output in rat primary hepatocytes. GPi688 can be used for researching glucagon-mediated hyperglycaemia .

HY-106934

Peldesine BCX 34	Nucleoside Antimetabolite/Analog HIV	Infection Inflammation/Immunology Cancer
Peldesine (BCX 34) is a potent, competitive, reversible and orally active *purine nucleoside phosphorylase* (PNP)** inhibitor with IC₅₀s of 36 nM, 5 nM, and 32 nM for human, rat, and mouse red blood cell (RBC) PNP, respectively. Peldesine is also a T-cell proliferation inhibitor with an IC₅₀ of 800 nM. Peldesine has the potential for cutaneous T-cell lymphoma, psoriasis and HIV infection research .

HY-106934A

Peldesine dihydrochloride BCX 34 dihydrochloride	Nucleoside Antimetabolite/Analog HIV	Infection Inflammation/Immunology Cancer
Peldesine (BCX 34) dihydrochloride is a potent, competitive, reversible and orally active *purine nucleoside phosphorylase* (PNP)** inhibitor with IC₅₀s of 36 nM, 5 nM, and 32 nM for human, rat, and mouse red blood cell (RBC) PNP, respectively. Peldesine dihydrochloride is also a T-cell proliferation inhibitor with an IC₅₀ of 800 nM. Peldesine dihydrochloride has the potential for cutaneous T-cell lymphoma, psoriasis and HIV infection research .

HY-P1597

Malantide	PKA PKC	Cancer
Malantide is a synthetic dodecapeptide derived from the site phosphorylated by cAMP-dependent protein kinase (PKA) on the β-subunit of phosphorylase kinase. Malantide is a highly specific substrate for PKA with a K_m of 15 μM and shows protein inhibitor (PKI) inhibition >90% substrate phosphorylation in various rat tissue extracts . Malantide is also an efficient substrate for PKC with a K_m of 16 μM .

HY-N6732

K-252a 10+ Cited Publications SF2370; Antibiotic K 252a; Antibiotic SF 2370
K-252a, a staurosporine analog, inhibits protein kinase, with IC₅₀ values of 470 nM, 140 nM, 270 nM, and 1.7 nM for PKC, PKA, Ca ²⁺/calmodulin-dependent kinase type II, and phosphorylase kinase, respectively . K-252a is a potent inhibitor (IC₅₀ of 3 nM) of the tyrosine protein kinase (TRK) activity of the NGF receptor gp140trk, the product of the trk protooncogene .

HY-155148

MAT2A-IN-11	Methionine Adenosyltransferase (MAT)	Cancer
MAT2A Allosteric inhibitor 1 (compound 5) is a MAT2A selective inhibitor of methionine adenosyltransferase (MAT) with an IC₅₀ of 6.8 nM .

HY-P1597A

Malantide TFA	PKA PKC	Cancer
Malantide TFA is a synthetic dodecapeptide derived from the site phosphorylated by cAMP-dependent protein kinase (PKA) on the β-subunit of phosphorylase kinase. Malantide TFA is a highly specific substrate for PKA with a K_m of 15 μM and shows protein inhibitor (PKI) inhibition >90% substrate phosphorylation in various rat tissue extracts . Malantide TFA is also an efficient substrate for PKC with a K_m of 16 μM .

HY-16478

Trifluridine/tipiracil hydrochloride mixture 1 Publications Verification TAS-102; FTD/TPI	Nucleoside Antimetabolite/Analog Thymidylate Synthase	Cancer
Trifluridine/tipiracil hydrochloride mixture (TAS-102) is a potent and orally active nucleoside antitumor agent. The composition of Trifluridine/tipiracil hydrochloride mixture (TAS-102) is a 1:0.5 mixture (on a molar basis) of alpha,alpha,alpha-tri-fluorothymidine (FTD) and thymidine phosphorylase inhibitor (TPI). Trifluridine/tipiracil hydrochloride mixture (TAS-102) shows the antitumor activity mainly via the inhibition of thymidylate synthase (TS) and incorporation into DNA .

Nucleotide Compound Library	491 compounds
Nucleoside and nucleotide analogues are synthetic, chemically modified compounds that have been developed to mimic their physiological counterparts in order to exploit cellular metabolism and subsequently be incorporated into DNA and RNA to inhibit cellular division and viral replication. In addition to their incorporation into nucleic acids, nucleoside and nucleotide analogues can interact with and inhibit essential enzymes such as human and viral polymerases (that is, DNA-dependent DNA polymerases, RNA-dependent DNA polymerases or RNA-dependent RNA polymerases), kinases, ribonucleotide reductase, DNA methyltransferases, purine and pyrimidine nucleoside phosphorylase and thymidylate synthase. These actions of nucleoside and nucleotide analogues have potential therapeutic benefits — for example, in the inhibition of cancer cell growth, the inhibition of viral replication as well as other indications. MCE offers a unique collection of 491 nucleotide compounds including nucleotide, nucleoside and their structural analogues. MCE Nucleotide Compound Library is a useful tool to discover anti-cancer and antiviral drugs for high throughput screening (HTS) and high content screening (HCS).

2'-Deoxyadenosine 5'-di-phos-phate disodium dADP disodium	Gene Sequencing and Synthesis
2'-Deoxyadenosine 5'-di-phos-phate disodium (dADP disodium) is an inhibitor of bacterial poly(A) polymerase. It can be used to synthesize deoxyadenosine oligonucleotides with Escherichia coli polynucleotide phosphorylase and other enzymes .

Malantide	PKA PKC	Cancer
Malantide is a synthetic dodecapeptide derived from the site phosphorylated by cAMP-dependent protein kinase (PKA) on the β-subunit of phosphorylase kinase. Malantide is a highly specific substrate for PKA with a K_m of 15 μM and shows protein inhibitor (PKI) inhibition >90% substrate phosphorylation in various rat tissue extracts . Malantide is also an efficient substrate for PKC with a K_m of 16 μM .

Malantide TFA	PKA PKC	Cancer
Malantide TFA is a synthetic dodecapeptide derived from the site phosphorylated by cAMP-dependent protein kinase (PKA) on the β-subunit of phosphorylase kinase. Malantide TFA is a highly specific substrate for PKA with a K_m of 15 μM and shows protein inhibitor (PKI) inhibition >90% substrate phosphorylation in various rat tissue extracts . Malantide TFA is also an efficient substrate for PKC with a K_m of 16 μM .

2'-Deoxyinosine 1 Publications Verification	Natural Products Classification of Application Fields Source classification Metabolic Disease Endogenous metabolite Disease Research Fields	Endogenous Metabolite
2’-deoxyadenosine inhibits the growth of human colon-carcinoma cell lines and is found to be associated with purine nucleoside phosphorylase (PNP) deficiency.

Staurosporine Maximum Cited Publications 89 Publications Verification Antibiotic AM-2282; STS; AM-2282	Infection Alkaloids Structural Classification Microorganisms Classification of Application Fields Source classification Marine natural products Disease Research Fields Marine microorganism Indole Alkaloids	PKC PKA Apoptosis Bacterial Fungal Antibiotic
Staurosporine is a potent, ATP-competitive and non-selective inhibitor of protein kinases with IC₅₀s of 6 nM, 15 nM, 2 nM, and 3 nM for PKC, PKA, c-Fgr, and Phosphorylase kinase respectively. Staurosporine also inhibits TAOK2 with an IC₅₀ of 3 μM. Staurosporine is an apoptosis inducer .

Tubercidin 4 Publications Verification 7-Deazaadenosine	Infection Structural Classification Microorganisms Classification of Application Fields Antibiotics Source classification Antiviral Antibacterial Disease Research Disease Research Fields Other Antibiotics	Bacterial DNA/RNA Synthesis Influenza Virus Antibiotic
Tubercidin (7-Deazaadenosine) is an antibiotic obtained from Streptomyces tubercidicus. Tubercidin inhibits the growth of Streptococcus faecalis (8043) with an IC₅₀ of 0.02 μM . Tubercidin inhibits polymerases by incorporating DNA or RNA, thereby inhibiting DNA replication, RNA and protein synthesis . Tubercidin is a weak inhibitor of adenosine phosphorylase, and interferes with the phosphorylation of adenosine and AMP . Tubercidin has antiviral activity .

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Phosphorylases inhibitor

Inhibitors & Agonists

Screening Libraries

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Natural
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