c-Kit
SCFR; CD117
c-Kit (Mast/stem cell growth factor receptor, SCFR or CD117) is a proteinthat in humans is encoded by the KIT gene. c-Kit (CD117) is an important cell surface marker used to identify certain types of hematopoietic(blood) progenitors in the bone marrow. c-Kit is a cytokine receptor expressed on the surface of hematopoietic stem cells as well as other cell types. Altered forms of this receptor may be associated with some types of cancer. c-Kit is a receptor tyrosine kinase type III, which binds to stem cell factor. When c-Kit binds to stem cell factor (SCF) it forms adimer that activates its intrinsic tyrosine kinase activity, that in turn phosphorylates and activates signal transduction molecules that propagate the signal in the cell. Signalling through c-Kit plays a role in cell survival, proliferation, and differentiation.
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c-Kit Related Products (211)
Related Products (211)
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Recombinant Proteins (20)
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Antibodies (3)
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Lenvatinib-d5
0 ImagesCat. No.: HY-10981S1Synonyms: E7080-d5; MK-7902-d5
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CSF1R/c-Kit-IN-1
0 ImagesCat. No.: HY-187340CSF1R/c-Kit-IN-1 is a CSF-1R and c-Kit inhibitor, with an IC50 of 5.88 nM against human CSF-1R and an IC50 of 1.47 nM against human c-Kit. CSF1R/c-Kit-IN-1 binds to the ATP-binding pocket of CSF-1R, forming a hinge interaction with Cys666 via the oxazole nitrogen atom and adjacent amino group, and binds to residues in the hydrophobic binding pocket. CSF1R/c-Kit-IN-1 binds to the ATP-binding pocket of c-Kit, maintains a hinge interaction through its 2-amino-oxazole core, and binds to a broader hydrophobic surface near the solvent-exposed region via its morpholine substituent. CSF1R/c-Kit-IN-1 inhibits CSF-1-induced phosphorylation of ERK, which is a downstream readout of the CSF-1R signaling pathway. CSF1R/c-Kit-IN-1 can be used in the research of neuroinflammation-related neurodegenerative diseases.
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SU11657
0 ImagesCat. No.: HY-138032CAS No.: 326914-17-4Synonyms: N,N-Dimethyl sunitinibSU11657 (N,N-Dimethyl sunitinib) is an orally active multi-targeted tyrosine kinase inhibitor with IC50 values of 0.04 μM (c-Kit), 0.005 μM (PDGFR), 0.013 μM (VEGFR1), 0.017 μM (VEGFR2) and 50 nM (FLT3), respectively. SU11657 exhibits anti-angiogenic activity. SU11657 delays leukemia progression, synergizes with ATRA (HY-14649) to reduce leukemia burden, and inhibits symptoms and tissue damage associated with rheumatoid arthritis. SU11657 can be used in research related to FLT3-mutated acute promyelocytic leukemia, rheumatoid arthritis, neuroblastoma, and benign/atypical meningioma.
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c-Fms-IN-12
0 ImagesCat. No.: HY-147864CAS No.: 2145102-33-4c-Fms-IN-12 (Compound 4g) is an FMS kinase inhibitor. c-Fms-IN-12 can also inhibits c-KIT. c-Fms-IN-12 is a potential broad-spectrum anticancer agent against multiple cancer types. c-Fms-IN-12 induces A549 cell apoptosis.
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CSF1R/c-Kit-IN-2
0 ImagesCat. No.: HY-187341CSF1R/c-Kit-IN-2 is a dual CSF-1R/c-Kit inhibitor with a c-Kit-biased profile, exhibiting inhibitory activity against CSF-1R (IC50 = 6.84 nM), c-Kit (IC50 = 0.95 nM), FYN (IC50 = 11.4 nM), ABL1 (IC50 = 14.2 nM), and CSK (IC50 = 118 nM). CSF1R/c-Kit-IN-2 can be used for the research of neuroinflammation-associated neurodegenerative diseases.
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c-Kit-IN-7
0 ImagesCat. No.: HY-168580CAS No.: 2941026-35-1
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c-Met-IN-14
0 ImagesCat. No.: HY-150582CAS No.: 2443380-34-3c-Met-IN-14 (compound 26af) is a selective inhibitor of c-Met kinase from N-sulfonylamidine-based derivatives, with an IC50 value of 2.89 nM. c-Met-IN-14 shows anticancer activity by blocking phosphorylation of c-Met, and arrests cell cycle at G2/M phase. c-Met-IN-14 induces apoptosis of A549 cells in a dose-dependent manner.
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Dovitinib-d8
0 ImagesCat. No.: HY-50905SCAS No.: 1246819-84-0
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Pimicotinib hydrochloride
0 ImagesCat. No.: HY-153920ACAS No.: 2866305-19-1Synonyms: ABSK021 hydrochloridePimicotinib (ABSK021) hydrochloride is a selective and orally active CSF1R inhibitor with an IC50 value of 19.48 nM (determined by inhibiting ADP production). Pimicotinib hydrochloride exhibits anti-tumor activity.
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AK177
0 ImagesCat. No.: HY-181886AK177 is an allosteric activator of IRE1α ribonuclease, with values of 480 nM and 180 nM against non-phosphorylated and phosphorylated IRE1α, respectively. AK177 promotes IRE1α-mediated cleavage of XBP1 mRNA probe in a concentration-dependent manner and binds stably to its kinase domain. However, AK177 shows poor kinase selectivity, and due to poor membrane permeability at the cellular level, it induces no significant downstream pathway activation or antiproliferative activity.
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Kit-IN-1
0 ImagesCat. No.: HY-187462CAS No.: 3080682-21-6Kit-IN-1 is a kinome-selective and orally active KIT inhibitor with a human IC50 value of 2.8 nM. Kit-IN-1 binds to KIT in an allosteric mode, stabilizes the inactive DFG-out conformation of KIT, and blocks the stem cell factor (SCF)-mediated KIT phosphorylation signaling pathway. Kit-IN-1 inhibits SCF-induced ear swelling in rats and prevents increased vascular permeability. Kit-IN-1 can be used in studies related to mast cell-driven chronic inflammation.
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Regorafenib monohydrate (Standard)
0 ImagesSynonyms: BAY 73-4506 monohydrate (Standard)Regorafenib (monohydrate) (Standard) is the analytical standard of Regorafenib (monohydrate). This product is intended for research and analytical applications. Regorafenib (BAY 73-4506) monohydrate is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor, with IC50 values of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib monohydrate shows very robust antitumor and antiangiogenic activity.
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Kit-IN-2
0 ImagesCat. No.: HY-189056CAS No.: 3080682-14-7Kit-IN-2 is an orally active and highly selective KIT inhibitor. Kit-IN-2 stabilizes the inactive (DFG-out) conformation of KIT. Kit-IN-2 inhibits mast cell-mediated inflammatory responses by blocking stem cell factor-induced ear swelling and vascular permeability in rats. Kit-IN-2 exhibits favorable pharmacokinetic properties in rats. Kit-IN-2 can be used for studies related to acute allergy.
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PLX647 dihydrochloride
0 ImagesCat. No.: HY-13838ACAS No.: 1779796-38-1PLX647 dihydrochloride is an orally active, highly specific dual FMS and KIT kinase inhibitor, with IC50s of 28 and 16 nM, reapectively. PLX647 dihydrochloride shows selectivity for FMS and KIT over a panel of 400 kinases at a concentration of 1 μM except FLT3 and KDR (IC50s=91 and 130 nM, respectively).
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GW632046X
0 ImagesCat. No.: HY-160690CAS No.: 681002-67-5GW632046X is a Fluc (Firefly luciferase) inhibitor with an IC50 value of 0.58 µM.
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c-Kit-IN-14
0 ImagesCat. No.: HY-180653CAS No.: 3041025-49-1
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BLU-654
0 ImagesCat. No.: HY-182043CAS No.: 2999638-62-7BLU-654 is an orally active antineoplastic agent and KIT inhibitor. BLU-654 is a highly selective inhibitor targeting wild-type KIT, PDGFRβ, and KITV654A over most other kinases in the kinome. BLU-654 exerts sustained antineoplastic activity in KITV654A cell-derived xenograft mouse models. BLU-654 can be used in research related to Imatinib (HY-15463)-resistant gastrointestinal stromal tumors.
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KBP-7018 hydrochloride
0 ImagesCat. No.: HY-117873ACAS No.: 1613437-67-4KBP-7018 hydrochloride is an orally active, tyrosine kinase-selective multi-kinase inhibitor with an IC50 value of 10 nM against c-KIT, 7.6 nM against RET, and 25 nM against human PDGFR. KBP-7018 hydrochloride improves survival rates in a mouse model of pulmonary fibrosis. KBP-7018 hydrochloride can be used in research related to idiopathic pulmonary fibrosis.
