Protein / target
Mast/stem cell growth factor receptor Kit
Protein at a glance
Biological role
Transmembrane receptor protein tyrosine kinase
Strongest disease association
Cutaneous mastocytosis
Therapeutic position
Established drug target
Research activity
Emerging research
Derived from structured UniProt, Open Targets and literature data on this page.
Protein profile
Canonical identity and biological annotation from UniProt.
Function overview
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.
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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
Cell proliferation & survival
- ·Tyrosine-protein kinase that acts as a cell-surface receptor for the cytokine KITLG/SCF…
- ·positive regulation of cell population proliferation
- ·regulation of cell population proliferation
- ·PIP3 activates AKT signaling
Cell migration
- ·cell chemotaxis
- ·cell migration
- ·germ cell migration
- ·mast cell chemotaxis
Receptor tyrosine kinase signalling
- ·transmembrane receptor protein tyrosine kinase activity
Oncogenic signalling
- ·Constitutive Signaling by Aberrant PI3K in Cancer
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
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.
Approved medicines with mapped indications
Approved therapies targeting this protein, grouped by what they are approved to treat — the disease-first view of the medicines below. Relationships come from the canonical approved-indication graph (ChEMBL phase-4), the same source as the drug cards.
20 medicines meet Open Targets' target-level approved-medicine definition; the 6 shown here are those on this page with a canonical approved disease indication in the graph. Approved indications from ChEMBL (phase-4), via the canonical drug→disease graph.
Drugs targeting this protein
How approved and investigational drugs engage this protein — mechanism and action type, direct vs complex targeting, and how broadly each acts across other targets. A drug-first view (the section above groups the approved ones disease-first); direct binders with few recorded targets are listed first.
Stem cell growth factor receptor inhibitor
Indicated for Neoplasms
Stem cell growth factor receptor inhibitor
Indicated for Gastrointestinal Stromal Tumors, Neoplasms
Stem cell growth factor receptor inhibitor
Indicated for Gastrointestinal Stromal Tumors, Leukemia, Myelogenous, Chronic, BCR-ABL Positive, Myelodysplastic-Myeloproliferative Diseases, Precursor Cell Lymphoblastic Leukemia-Lymphoma
Stem cell growth factor receptor inhibitor
Indicated for Carcinoma, Renal Cell, Gastrointestinal Stromal Tumors, Neuroendocrine Tumors, Neoplasms
Stem cell growth factor receptor inhibitor
Indicated for Colorectal Neoplasms, Neoplasms
Stem cell growth factor receptor inhibitor
View all 8 targeting drugsHide
Stem cell growth factor receptor inhibitor
Indicated for Leukemia, Myeloid, Acute, Mastocytosis, Mastocytosis, Systemic, Neoplasms
Stem cell growth factor receptor inhibitor
ChEMBL mechanism, action type, target identity and approved indications. Open Targets clinical status.
Translational evidence
Why this target matters therapeutically, strongest evidence first. Disease associations are gene-level (via the gene that encodes this protein) and open into the full confidence synthesis; the development universe, tractability and safety annotations are target-level, from Open Targets.
Strongest disease associations · via encoding gene KIT
Gene-level evidence surfaced through the gene KITthat encodes this protein — not a direct protein–disease relationship. Ranked by Forefront's causal-directness weighting, so genetically- and clinically-evidenced diseases lead over ones that merely share the literature.
View evidence synthesis (5)Hide
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 per-type scores above show the calculation.
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Drug development
38 compounds recorded · 20 approved · 18 in clinical development
View all recorded compounds (10)Hide
Open Targets known-drugs universe. Drug name and highest clinical stage only — the disease relationship is NOT read from this slice (it carries trial-context noise); approved indications come from the canonical graph above.
Tractability
Small molecules — Strong
Antibodies — Supported
Protein degraders — Emerging
View underlying tractability evidence (15)Hide
Raw Open Targets tractability assessment buckets, by modality.
Safety-related annotations
Terms indexed against this target in Open Targets' safety data, with their datasource. These are annotations, not causal claims: the direction of effect (whether activation or inhibition is implicated), species and evidence strength are not captured here, so an entry does not mean that modulating this target is known to cause that condition.
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. Ranked by active status, then clinical phase and recency, and spread across the targeting drugs.
View all trials (26)Hide
ClinicalTrials.gov via the drug-target graph.
What's happening now
Recent therapeutic activity around this target — regulatory actions, clinical trials and safety signals for 3 drugs that target this protein, plus publications where such a drug is a genuine subject. Every item is reached indirectly through the drug, not the protein itself; incidental mentions (a paper that merely measures a drug) and press items are excluded.
- Label change
Label change: IMATINIB MESYLATE (NDA021588)
- Label change
Label change: IMATINIB MESYLATE (NDA021588)
- 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.
- New publicationGenomic profiling in GIST: Implications in clinical outcome and future challenges.
- Label change
Label change: IMATINIB (ANDA204644)
- 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.
Research activity
Papers linked directly to this protein. This is the protein's own literature — descriptor-derived papers are kept separate below.
Most cited
Recent
Europe PMC papers linked directly to this protein.