oncogenic signaling

Pathways Recommended:	Neuronal Signaling JAK/STAT Signaling

By Targets:	Apoptosis (6) c-Myc (1) CDK (1) Farnesyl Transferase (2) Hedgehog (2) HSP (1) MEK (1) PAK (3) PKC (1) PROTACs (1) Ras (3) Smo (1)
By Research Areas:	Cancer (11) Infection (2) Inflammation/Immunology (1)

Targets Recommended: RGS Protein

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-108508

SMANT hydrochloride	Smo Hedgehog	Cancer
SMANT hydrochloride is a Smoothened (Smo) signaling inhibitor. SMANT hydrochloride is antagonist of Smo accumulation within the primary cilium (PC). SMANT hydrochloride has an equivalent activity in inhibiting SmoM2 (oncogenic form of Smo) and wild-type Smo .

HY-15872A

FTI-277 hydrochloride 3 Publications Verification	Farnesyl Transferase Apoptosis Ras	Infection Cancer
FTI-277 hydrochloride is an inhibitor of farnesyl transferase (FTase); a highly potent Ras CAAX peptidomimetic which antagonizes both H- and K-Ras oncogenic signaling. FTI-277 hydrochloride can inhibit hepatitis delta virus (HDV) infection.

HY-150926

G12Si-1	Ras	Cancer
G12Si-1 is a selective K-Ras(G12S) covalent inhibitor, which can inhibit oncogenic signaling of K-Ras(G12S). G12Si-1 shows good ability to covalently engage recombinant K-Ras(G12S) at the mutant serine residue. G12Si-1 can also affect nucleotide cycling of K-Ras by blocking Sos-catalyzed exchange and decreasing the rate of EDTA promoted exchange .

HY-15872

FTI-277	Farnesyl Transferase Apoptosis Ras	Infection Cancer
FTI-277 is an inhibitor of farnesyl transferase (FTase); a highly potent Ras CAAX peptidomimetic which antagonizes both H- and K-Ras oncogenic signaling. FTI-277 can inhibit hepatitis delta virus (HDV) infection.

HY-N11794

7-Ketologanin	Others	Others
7-Ketologanin is an iridoid glucoside. 7-Ketologanin can be isolated from the Stems of Viburnum erosum. 7-Ketologanin involves in biosynthetic pathway of oleuropein. Oleuropein, is a bioactive phenolic compound, modulates several oncogenic signalling pathways .

HY-106381

Aurothiomalate sodium	PKC	Inflammation/Immunology Cancer
Aurothiomalate sodium is a potent and selective oncogenic PKC_ι signaling inhibitor. Aurothiomalate sodium inhibits tumor cell proliferation and not cell apoptosis. Aurothiomalate sodium is a potent thioredoxin reductase (TrxR) inhibitor. Aurothiomalate sodium, an anti-rheumatoid agent, exhibits potent anti-tumor activity .

HY-13007

PF-3758309 Maximum Cited Publications 7 Publications Verification PF-03758309	PAK Apoptosis	Cancer
PF-3758309 (PF-03758309) is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (K_d= 2.7 nM; K_i=18.7 nM). PF-3758309 has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation .

HY-13007B

PF-3758309 dihydrochloride PF-03758309 dihydrochloride	PAK Apoptosis	Cancer
PF-3758309 (PF-03758309) dihydrochloride is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (K_d= 2.7 nM; K_i=18.7 nM). PF-3758309 dihydrochloride has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation .

HY-13007A

PF-3758309 hydrochloride PF-03758309 hydrochloride	PAK Apoptosis	Cancer
PF-3758309 (PF-03758309) hydrochloride is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (K_d= 2.7 nM; K_i=18.7 nM). PF-3758309 hydrochloride has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation .

HY-100627

APS-2-79	MEK	Cancer
APS-2-79 is a KSR-dependent MEK antagonist. APS-2-79 inhibits ATP ^biotin binding to KSR2 within the KSR2-MEK1 complexe with an IC₅₀ of 120 nM. APS-2-79 makes the stabilization of the KSR inactive state antagonizes oncogenic Ras-MAPK signaling .

HY-100627A

APS-2-79 hydrochloride
APS-2-79 hydrochloride is a KSR-dependent MEK antagonist. APS-2-79 inhibits ATP ^biotin binding to KSR2 within the KSR2-MEK1 complexe with an IC₅₀ of 120 nM. APS-2-79 makes the stabilization of the KSR inactive state antagonizes oncogenic Ras-MAPK signaling .

HY-156084

LL-K9-3	CDK PROTACs Apoptosis c-Myc	Cancer
LL-K9-3 is a potent small-molecule degrader of CDK9-cyclin T1. LL-K9-3 has anti-proliferative and pro-apoptotic activities and suppresses downstream signaling of CDK9 and AR. Moreover, LL-K9-3 inhibits AR and Myc-driven oncogenic transcriptional programs .

HY-143400

HSP70-IN-3	HSP Hedgehog	Cancer
HSP70-IN-3 is a potent HSP70 inhibitor (IC₅₀s of 1.1 and 1.9 μM in ASZ001 and C3H10T1/2, respectively). HSP70-IN-3 has anti-Hh (Hedgehog signaling) activity and anti-proliferative activity and reduces expression of the oncogenic transcription factor GLI1 .

Cat. No.	Product Name

HY-L064

Glutamine Metabolism Compound Library	903 compounds
Glutamine is an important metabolic fuel that helps rapidly proliferating cells meet the increased demand for ATP, biosynthetic precursors, and reducing agents. Glutamine Metabolism pathway involves the initial deamination of glutamine by glutaminase(GLS), yielding glutamate and ammonia. Glutamate is converted to the TCA cycle intermediate α-ketoglutarate (α-KG) by either glutamate dehydrogenase (GDH) or by the alanine or aspartate transaminases (TAs), to produce both ATP and anabolic carbons for the synthesis of amino acids, nucleotides and lipids. During periods of hypoxia or mitochondrial dysfunction, α-KG can be converted to citrate in a reductive carboxylation reaction catalyzed by IDH2. The newly formed citrate exits the mitochondria where it is used to synthesize fatty acids and amino acids and produce the reducing agent, NADPH. Cancer cells display an altered metabolic circuitry that is directly regulated by oncogenic mutations and loss of tumor suppressors. Mounting evidence indicates that altered glutamine metabolism in cancer cells has critical roles in supporting macromolecule biosynthesis, regulating signaling pathways, and maintaining redox homeostasis, all of which contribute to cancer cell proliferation and survival. Thus, intervention in glutamine metabolic processes could provide novel approaches to improve cancer treatment. MCE owns a unique collection of 903 compounds targeting the mainly proteins and enzymes involved in glutamine metabolism pathway. Glutamine Metabolism compound library is a useful tool for intervention in glutamine metabolic processes.

Glutamine Metabolism Compound Library

903 compounds

Glutamine is an important metabolic fuel that helps rapidly proliferating cells meet the increased demand for ATP, biosynthetic precursors, and reducing agents. Glutamine Metabolism pathway involves the initial deamination of glutamine by glutaminase(GLS), yielding glutamate and ammonia. Glutamate is converted to the TCA cycle intermediate α-ketoglutarate (α-KG) by either glutamate dehydrogenase (GDH) or by the alanine or aspartate transaminases (TAs), to produce both ATP and anabolic carbons for the synthesis of amino acids, nucleotides and lipids. During periods of hypoxia or mitochondrial dysfunction, α-KG can be converted to citrate in a reductive carboxylation reaction catalyzed by IDH2. The newly formed citrate exits the mitochondria where it is used to synthesize fatty acids and amino acids and produce the reducing agent, NADPH.

Cancer cells display an altered metabolic circuitry that is directly regulated by oncogenic mutations and loss of tumor suppressors. Mounting evidence indicates that altered glutamine metabolism in cancer cells has critical roles in supporting macromolecule biosynthesis, regulating signaling pathways, and maintaining redox homeostasis, all of which contribute to cancer cell proliferation and survival. Thus, intervention in glutamine metabolic processes could provide novel approaches to improve cancer treatment.

MCE owns a unique collection of 903 compounds targeting the mainly proteins and enzymes involved in glutamine metabolism pathway. Glutamine Metabolism compound library is a useful tool for intervention in glutamine metabolic processes.

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N11794

7-Ketologanin	Structural Classification Iridoids Terpenoids Source classification Viburnum erosum Thunb. Plants Adoxaceae	Others
7-Ketologanin is an iridoid glucoside. 7-Ketologanin can be isolated from the Stems of Viburnum erosum. 7-Ketologanin involves in biosynthetic pathway of oleuropein. Oleuropein, is a bioactive phenolic compound, modulates several oncogenic signalling pathways .

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oncogenic signaling

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