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Tyrosine Kinase/Adaptors

Discoidin Domain Receptor (DDR)

IGF-1R

The insulin-like growth factor 1 (IGF-1) receptor is a protein found on the surface of human cells. It is a transmembrane receptor that is activated by a hormone called insulin-like growth factor 1 (IGF-1) and by a related hormone called IGF-2. It belongs to the large class of tyrosine kinase receptors. This receptor mediates the effects of IGF-1, which is a polypeptide protein hormone similar in molecular structure to insulin. IGF-1 plays an important role in growth and continues to have anabolic effects in adults – meaning that it can induce hypertrophy of skeletal muscle and other target tissues. Mice lacking the IGF-1 receptor die late in development, and show a dramatic reduction in body mass, testifying to the strong growth-promoting effect of this receptor.

Filter HomeSignaling PathwaysTyrosine Kinase/AdaptorsIGF-1R

Semaglutide

T19850910463-68-2

Semaglutide is a glucagon-like peptide 1 receptor (GLP-1R) agonist(EC50 of 6.2 pM in a reporter assay using BHK cells expressing the human receptor).

Apoptosis Autophagy Bcl-2 Family Glucagon Receptor IGF-1R p38 MAPK

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Linsitinib

OSI-906

T6017867160-71-2

OSI-906 (Linsitinib (OSI-906)) is an orally bioavailable small molecule inhibitor of the insulin-like growth factor 1 receptor (IGF-1R) with potential antineoplastic activity. Linsitinib selectively inhibits IGF-1R, which may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. Overexpressed in a variety of human cancers, IGF-1R stimulates cell proliferation, enables oncogenic transformation, and suppresses apoptosis.

IGF-1R

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Semaglutide Acetate

Semaglutide Acetate(910463-68-2 Free base)

T19850L1997361-85-9

Semaglutide Acetate is a GLP-1R agonist (EC50=6.2 pM) with long-acting, selective, competitive, and oral efficacy. Semaglutide acetate can be used in the study of type 2 diabetes.

Apoptosis Autophagy Bcl-2 Family Glucagon Receptor IGF-1R p38 MAPK

$129

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Insulin (human)

Insulin(human), INSULIN

T822111061-68-0

Insulin (human) is a peptide hormone that promotes glycogen synthesis and regulates glucose levels in the blood. Insulin (human) has hypoglycemic activity and is used clinically to treat hyperglycemia in diabetic patients.

IGF-1R

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GIP (3-42), human

Gastric Inhibitory Polypeptide (3-42) (human)

T375891802086-25-4

GIP (3-42), human (Gastric Inhibitory Polypeptide (3-42) (human)) is a peptide that acts as a glucose-dependent proinsulinotropic polypeptide (GIP) receptor antagonist and regulates insulin secretion and the metabolic effects of GIP in vivo, which can be used to study type 2 diabetes.

IGF-1R

$196

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Insulin(cattle)

Insulin from bovine pancreas

TP112511070-73-8

Insulin(cattle) is a peptide hormone that promotes glycogen synthesis and regulates glucose levels in the blood. Insulin has hypoglycemic activity and is used clinically to treat hyperglycemia in diabetic patients.

IGF-1R

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Ganitumab

AMG 479

T76810905703-97-1

Ganitumab (AMG 479) is a highly potent monoclonal antibody targeting the type 1 insulin-like growth factor receptor (IGF1R). Recognized for binding IGF1R at low concentrations with a KD value of 0.22 nM, Ganitumab inhibits IGF1R interactions with IGF1 and IGF2 in mice, making it useful for cancer research.

IGF-1R

$289

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AVJ16

T99802775241-92-2

AVJ16 as a member of the insulin growth factor 2 mRNA-binding protein family, binds to the mRNA of certain genes to regulate protein translation.

Apoptosis IGF-1R IGF-2R

$139

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GIP (human) acetate

GIP (human) acetate(100040-31-1 Free base)

TP2018L

GIP (human) acetate is a stimulator of glucose-dependent insulin secretion and a weak inhibitor of gastric acid secretion. GIP (human) acetate plays a vital role in lipid metabolism and the development of obesity.

IGF-1R

$238

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BN201

OCS05, OCS 05, G-79, BN 201, ACT-01, ACT01

T146931361200-34-1

BN201 (OCS-05) is a drug with neuroprotective and myelin repair effects, which acts mainly by activating serum glucocorticoid kinase-2 (SGK2), which in turn activates the FOXO3 pathway to promote neuronal survival and myelin repair. It is mainly used for the treatment of inflammatory neurological diseases such as multiple sclerosis (MS) and experimental autoimmune encephalomyelitis (EAE).BN201 is able to regulate multiple kinases in the insulin growth factor 1 (IGF1) pathway and cross the blood-brain barrier.

FOXO IGF-1R Others SGK

$239

6-8 weeks

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NVP-ADW742

ADW742, ADW

T6079475488-23-4

NVP-ADW742 (ADW) is an IGF-1R inhibitor with IC50 of 0.17 μM, >16-fold more potent against IGF-1R than InsR; little activity to HER2, PDGFR, VEGFR-2, Bcr-Abl and c-Kit.

Apoptosis IGF-1R

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Urolithin C

TN7108165393-06-6

Urolithin C is a gut metabolite of ellagic acid. Urolithin C induces apoptosis in PC12 cells through a mitochondria-mediated pathway.

Apoptosis Calcium Channel Endogenous Metabolite IGF-1R Reactive Oxygen Species ROS

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Picropodophyllin

PPP, Picropodophyllotoxin, AXL1717

T6943477-47-4

Picropodophyllin (Picropodophyllin (PPP)) (PPP) is a specific IGF-1R inhibitor (IC50: 1 nM). Picropodophyllin specifically inhibits the activity and downregulates the cellular expression of IGF1R without interfering with activities of other growth factor receptors, such as receptors for insulin, epidermal growth factor, platelet-derived growth factor, fibroblast growth factor and mast/stem cell growth factor (KIT).

Apoptosis IGF-1R

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BMS-536924

CS-0117, BMS 536924

T6419468740-43-4

BMS-536924 (BMS 536924) is an ATP-competitive IGF-1R/IR inhibitor with IC50 of 100 nM/73 nM, modest activity for Mek, Fak, and Lck with very little activity for Akt1, MAPK1/2.

Apoptosis FAK IGF-1R MEK Src

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Ginsenoside Rg5

T6S1487186763-78-0

1. Ginsenoside Rg5 could be a beneficial agent for the treatment of Alzheimer's disease. 2. Ginsenoside Rg5 suppresses LPS-induced nitric oxide (NO) production and proinflammatory TNF-α secretion. 3. Ginsenoside Rg5 can ameliorate lung inflammation possib

COX IGF-1R NF-κB

$115

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Brigatinib

AP-26113

T36211197953-54-0

Brigatinib (AP-26113) is a highly potent and selective inhibitor of ALK.

ALK EGFR FLT IGF-1R ROS

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BMS-754807

T23491001350-96-4

Dual IGF-1R/InsR Inhibitor BMS-754807 is an oral small molecule inhibitor of insulin-like growth factor 1 receptor (IGF-1R) and insulin receptor (InsR) tyrosine kinases with potential antineoplastic activity.

c-Met/HGFR IGF-1R Trk receptor

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KW-2450 free base

T68405904899-25-8In house

KW-2450 free base is an orally bioavailable inhibitor of insulin-like growth factor 1 receptor (IGF-1R) and insulin receptor (IR) tyrosine kinases with potential antineoplastic activity. IGF-1R/IR inhibitor KW-2450 free base selectively binds to and inhibits the activities of IGF-1R and IR, which may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. IGF-R1 and IR tyrosine kinases, overexpressed in a variety of human cancers, play significant roles in the stimulation of cellular proliferation, oncogenic transformation, and suppression of apoptosis.

Apoptosis Aurora Kinase IGF-1R

$588

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HNMPA

T21761132541-52-7In house

HNMPA is a membrane impermeable inhibitor of insulin receptor tyrosine kinase. HNMPA inhibits tyrosine and serine autophosphorylation by the human insulin receptor. HNMPA exhibits no effect on cyclic AMP-dependent protein kinase or protein kinase C activities.

IGF-1R

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Teprotumumab

R 1507, HZN 001

T767271036734-93-6

Teprotumumab is a human monoclonal antibody that blocks the IGF-1 receptor (IGF-1R). Teprotumumab binds to the extracellular α-subunit domain ligand of IGF-1R. Teprotumumab inhibits TSH and IGF-1 action in fibrocytes. Teprotumumab reduces TSH-dependent IL-6 and IL-8 expression and Akt phosphorylation. Teprotumumab can be used in the study of thyroid-associated eye diseases.

IGF-1R TSH Receptor

$163

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Ceritinib

LDK378

T17911032900-25-6

Ceritinib (LDK378) is an ALK tyrosine kinase inhibitor (IC50=200 pM) with selective, ATP-competitive, and oral activity. Ceritinib also inhibits IGF-1R, InsR, and STK22D (IC50=8/7/23 nM). Ceritinib has antitumor activity.

ALK IGF-1R Serine Protease

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GSK1904529A

GSK 4529

T60031089283-49-7In house

GSK1904529A (GSK 4529) is a specific inhibitor of IGF-1R (IC50=27 nM) and IR(IC50=25 nM) .

Apoptosis IGF-1R Raf Syk VEGFR

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Protonstatin-1

T71812521972-99-6

Protonstatin-1 is used as a hypoglycemic agent and as a compound for the treatment of Alzheimer's disease, inhibits IGFIR kinase activity and can be used in cancer research.

IGF-1R Proton pump

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I-OMe-Tyrphostin AG 538

I-OMe-AG 538

T115931094048-77-7In house

I-OMe-Tyrphostin AG 538 is a specific IGF-1R inhibitor and ATP-competitive inhibitor of PI5P4Kα (IC50: 1 µM).I-OMe-Tyrphostin AG 538 inhibits IGF-1R-mediated signaling and exhibits preferential cytotoxicity to nutrient-deficient PANC1 cells.

IGF-1R PI3K

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