Protein / target
Mast/stem cell growth factor receptor Kit
Protein at a glance
Biological role
Transmembrane receptor protein tyrosine kinase activity
Primary system
Nervous system
Strongest disease association
cutaneous mastocytosis
Therapeutic maturity
Clinically validated target
Druggability
Small molecule
Clinical development
20 approved · 18 in clinical development
Derived from structured UniProt, Open Targets and literature data on this page.
Protein profile
Canonical identity and biological annotation from UniProt.
Function
Tyrosine-protein kinase that acts as a cell-surface receptor for the cytokine KITLG/SCF and plays an essential role in the regulation of cell survival and proliferation, hematopoiesis, stem cell maintenance, gametogenesis, mast cell development, migration and function, and in melanogenesis. In response to KITLG/SCF binding, KIT can activate several signaling pathways. Phosphorylates PIK3R1, PLCG1, SH2B2/APS and CBL. Activates the AKT1 signaling pathway by phosphorylation of PIK3R1, the regulatory subunit of phosphatidylinositol 3-kinase. Activated KIT also transmits signals via GRB2 and activation of RAS, RAF1 and the MAP kinases MAPK1/ERK2 and/or MAPK3/ERK1. Promotes activation of STAT family members STAT1, STAT3, STAT5A and STAT5B. Activation of PLCG1 leads to the production of the cellular signaling molecules diacylglycerol and inositol 1,4,5-trisphosphate. KIT signaling is modulated by protein phosphatases, and by rapid internalization and degradation of the receptor. Activated KIT promotes phosphorylation of the protein phosphatases PTPN6/SHP-1 and PTPRU, and of the transcription factors STAT1, STAT3, STAT5A and STAT5B. Promotes phosphorylation of PIK3R1, CBL, CRK (isoform Crk-II), LYN, MAPK1/ERK2 and/or MAPK3/ERK1, PLCG1, SRC and SHC1
Subcellular location
Domains and Gene Ontology detail (80)Hide
Domains & features
Gene Ontology
- Cacrosomal vesicle
- Ccell-cell junction
- Ccytoplasmic side of plasma membrane
- Cexternal side of plasma membrane
- Cextracellular space
- Cplasma membrane
- Creceptor complex
- FATP binding
- Fcytokine binding
- Fgrowth factor binding
- Fmetal ion binding
- Fprotease binding
Biological roles
What this protein does, drawn together from its UniProt function, Gene Ontology terms and Reactome pathways.
View supporting evidenceHide supporting evidence
Kinase signalling
- ·Tyrosine-protein kinase that acts as a cell-surface receptor for the cytokine KITLG/SCF…
- ·protein tyrosine kinase activity
- ·transmembrane receptor protein tyrosine kinase activity
- ·positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction
Immune signalling
- ·Tyrosine-protein kinase that acts as a cell-surface receptor for the cytokine KITLG/SCF…
- ·cytokine binding
- ·B cell differentiation
- ·cytokine-mediated signaling pathway
Transcriptional regulation
- ·Tyrosine-protein kinase that acts as a cell-surface receptor for the cytokine KITLG/SCF…
- ·TFAP2 (AP-2) family regulates transcription of growth factors and their receptors
- ·Transcriptional and post-translational regulation of MITF-M expression and activity
Muscle contraction
- ·positive regulation of colon smooth muscle contraction
- ·positive regulation of pyloric antrum smooth muscle contraction
- ·positive regulation of small intestine smooth muscle contraction
Cell adhesion
- ·cell-cell junction
Proteolysis
- ·protease binding
View underlying pathways (22)Hide underlying pathways
Concepts derived from UniProt GO Reactome — each badge above shows which sources supported that role.
Interaction neighbourhood
Proteins with the strongest functional or physical association. Node size and line weight reflect STRING confidence; hover or select a partner to inspect one association.
Functional and physical associations from STRING v12.0. Only associations with this protein are drawn — partner-to-partner links are not part of this evidence.
Drugs targeting this protein
Whether each drug engages this protein directly or through a complex, and how many other targets are recorded for it. Direct binders with few recorded targets are listed first.
Stem cell growth factor receptor inhibitor
Appears in clinical studies involving tenosynovial giant cell tumor, diffuse type, neoplasm, Alzheimer disease, pigmented villonodular synovitis
Stem cell growth factor receptor inhibitor
Appears in clinical studies involving chronic myelogenous leukemia, BCR-ABL1 positive, myelodysplastic/myeloproliferative disease, gastrointestinal stromal tumor, dermatofibrosarcoma protuberans
Stem cell growth factor receptor inhibitor
Appears in clinical studies involving gastrointestinal stromal tumor, renal cell carcinoma, gastrointestinal stromal tumor, neuroendocrine neoplasm
Stem cell growth factor receptor inhibitor
Appears in clinical studies involving colorectal cancer, metastatic colorectal cancer, colorectal neoplasm, neoplasm
ChEMBL mechanism, action type and target identity. Open Targets clinical status and indications.
Translational evidence
Why this target matters therapeutically — disease associations, drugs in development, tractability and safety, from Open Targets.
Strongest genetic associations
Human genetic evidence — the most direct causal link between this target and a disease.
Highest-confidence therapeutic associations
Diseases where a drug acting on this target has already reached clinical development.
Show all associationsHide all associations
Open Targets ranks 2,858 associations for this target and we store the top 10 by aggregated score. The long tail is largely literature co-mention and RNA-expression evidence, not evidence that this target drives those diseases.
Known drugs · 38 total
colorectal cancer · Kaposi's sarcoma · soft tissue sarcoma
renal cell carcinoma · hepatocellular carcinoma · renal cell carcinoma
gastrointestinal stromal tumor
renal cell carcinoma · endometrial cancer · triple-negative breast carcinoma
tenosynovial giant cell tumor
renal cell carcinoma · thyroid gland carcinoma · hepatocellular carcinoma
gastric adenocarcinoma · gastric cancer · gastroesophageal junction adenocarcinoma
gastrointestinal stromal tumor · gastrointestinal stromal tumor · neoplasm
gastrointestinal stromal tumor · gastrointestinal stromal tumor · neoplasm
pulmonary arterial hypertension · pulmonary hypertension
Tractability
Safety liabilities
Clinical trials
Trials of drugs that target this protein — reached indirectly through those drugs, so a trial listed here studies the drug, not the protein.
Show remaining trials (24)Hide
ClinicalTrials.gov via the drug-target graph.
Forefront confidence
Our own weighting of the evidence behind each disease association. Human genetics and clinical evidence count for most; literature co-mention counts for little, because two entities sharing an abstract is not evidence that one drives the other.
The evidence agreement range shows how closely the independent evidence families agree — it is not a statistical confidence interval, and nothing here is fitted to outcome data. Derived from Open Targets evidence types under Forefront weighting; the underlying per-type scores are shown above so the calculation can be checked.
What's happening now
Recent activity around this target, drawn from one canonical event stream. Every item is reached through 4 drugs that target this protein, so each event is news about that drug rather than about the protein directly.
- Label change
Label change: IMATINIB MESYLATE (NDA021588)
- Label change
Label change: IMATINIB MESYLATE (NDA021588)
- New publicationBrain-wide microglia replacement using a nonconditioning strategy ameliorates pathology in mouse models of neurological disorders.
- New publicationEfficacy of pembrolizumab in microsatellite-stable, tumor mutational burden-high metastatic colorectal cancer: genomic signatures and clinical outcomes.
- Label change
Label change: IMATINIB (ANDA204644)
- New publicationLenvatinib Plus Pembrolizumab Versus Standard of Care for Previously Treated Metastatic Colorectal Cancer: Final Analysis of the Randomized, Open-Label, Phase III LEAP-017 Study.
- New publicationMachine-learning and mechanistic modeling of metastatic breast cancer after neoadjuvant treatment.
- Supplemental approval
Supplemental approval: IMATINIB MESYLATE (NDA021588)
- New publicationKIT mutations and expression: current knowledge and new insights for overcoming IM resistance in GIST.
- Label change
Label change: IMATINIB (ANDA204644)
- Label change
Label change: IMATINIB (ANDA204644)
- Label change
Label change: IMATINIB (ANDA204644)
Objective event titles are shown unmodified; the event kind and significance line are derived from structured fields. Forefront AttentionEvent stream aggregating Europe PMC Regulatory filings ClinicalTrials.gov.