General Information of the Protein
Protein ID
PT05418
Protein Name
Transient receptor potential cation channel subfamily V member 4
Secondarily
Protein Name
Osm-9-like TRP channel 4
Transient receptor potential protein 12
Vanilloid receptor-like channel 2
Vanilloid receptor-like protein 2
Vanilloid receptor-related osmotically-activated channel
Gene Name
TRPV4
Secondarily
Gene Name
Trp12
Vrl2
Vroac
Sequence
MADPGDGPRAAPGEVAEPPGDESGTSGGEAFPLSSLANLFEGEEGSSSLSPVDASRPAGPGDGRPNLRMKFQGAFRKGVPNPIDLLESTLYESSVVPGPKKAPMDSLFDYGTYRHHPSDNKRWRRKVVEKQPQSPKAPAPQPPPILKVFNRPILFDIVSRGSTADLDGLLSFLLTHKKRLTDEEFREPSTGKTCLPKALLNLSNGRNDTIPVLLDIAERTGNMREFINSPFRDIYYRGQTSLHIAIERRCKHYVELLVAQGADVHAQARGRFFQPKDEGGYFYFGELPLSLAACTNQPHIVNYLTENPHKKADMRRQDSRGNTVLHALVAIADNTRENTKFVTKMYDLLLLKCSRLFPDSNLETVLNNDGLSPLMMAAKTGKIGVFQHIIRREVTDEDTRHLSRKFKDWAYGPVYSSLYDLSSLDTCGEEVSVLEILVYNSKIENRHEMLAVEPINELLRDKWRKFGAVSFYINVVSYLCAMVIFTLTAYYQPLEGTPPYPYRTTVDYLRLAGEVITLFTGVLFFFTSIKDLFTKKCPGVNSLFVDGSFQLLYFIYSVLVVVSAALYLAGIEAYLAVMVFALVLGWMNALYFTRGLKLTGTYSIMIQKILFKDLFRFLLVYLLFMIGYASALVTLLNPCTNMKVCDEDQSNCTVPTYPACRDSETFSAFLLDLFKLTIGMGDLEMLSSAKYPVVFILLLVTYIILTFVLLLNMLIALMGETVGQVSKESKHIWKLQWATTILDIERSFPVFLRKAFRSGEMVTVGKSSDGTPDRRWCFRVDEVNWSHWNQNLGIINEDPGKSEIYQYYGFSHTVGRLRRDRWSSVVPRVVELNKNSSADEVVVPLDNLGNPNCDGHQQGYAPKWRTDDAPL
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Organism
Mus musculus, Mouse
Protein Classification
Ion channel
>
Voltage-gated ion channel
>
Transient receptor potential channel
Function
Non-selective calcium permeant cation channel involved in osmotic sensitivity and mechanosensitivity (PubMed:11094154). Activation by exposure to hypotonicity within the physiological range exhibits an outward rectification (PubMed:12093812, PubMed:14691263, PubMed:16368742, PubMed:16571723). Also activated by heat, low pH, citrate and phorbol esters (PubMed:14691263). Increase of intracellular Ca(2+) potentiates currents. Channel activity seems to be regulated by a calmodulin-dependent mechanism with a negative feedback mechanism (By similarity). Acts as a regulator of intracellular Ca(2+) in synoviocytes (By similarity). Plays an obligatory role as a molecular component in the nonselective cation channel activation induced by 4-alpha-phorbol 12,13-didecanoate and hypotonic stimulation in synoviocytes and also regulates production of IL-8 (By similarity). Together with PKD2, forms mechano- and thermosensitive channels in cilium (PubMed:18695040). Promotes cell-cell junction formation in skin keratinocytes and plays an important role in the formation and/or maintenance of functional intercellular barriers (PubMed:20413591). Negatively regulates expression of PPARGC1A, UCP1, oxidative metabolism and respiration in adipocytes (PubMed:23021218). Regulates expression of chemokines and cytokines related to pro-inflammatory pathway in adipocytes (PubMed:23021218). Together with AQP5, controls regulatory volume decrease in salivary epithelial cells (PubMed:16571723). Required for normal development and maintenance of bone and cartilage (By similarity). In its inactive state, may sequester DDX3X at the plasma membrane. When activated, the interaction between both proteins is affected and DDX3X relocalizes to the nucleus (By similarity).
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Uniprot ID
Primary ID:
Q9EPK8

Secondarily ID:
A0JNY0
Q91XR5
Q9EQZ4
Q9ERZ7
Q9ES76
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Ensembl ID
ENSG00000111199
Subcellular Location
Cell membrane
Apical cell membrane
Cell junction
Adherens junction
Cell projection
Cilium
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000006 , HEK293
Compound ID Compound Name Compound Formula
CP0858290
4alpha-Phorbol 12,13-dihexanoate
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C32H48O8
 4
1
EC50 = 70 nM
   TI
   LI
   LO
   TS
2
EC50 = 360 nM
   TI
   LI
   LO
   TS
3
EC50 = 2790 nM
   TI
   LI
   LO
   TS
4
EC50 = 2840 nM
   TI
   LI
   LO
   TS
CP0858293
Lumi-4alpha-Phorbol 12,13-didecanoate
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C40H64O7
 4
1
EC50 = 175 nM
   TI
   LI
   LO
   TS
2
EC50 = 240 nM
   TI
   LI
   LO
   TS
3
EC50 = 3640 nM
   TI
   LI
   LO
   TS
4
EC50 = 9360 nM
   TI
   LI
   LO
   TS
CP0784818
4a-phorbol-12,13-didecanoate
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C40H64O8
 4
1
EC50 = 320 nM
   TI
   LI
   LO
   TS
2
EC50 = 370 nM
   TI
   LI
   LO
   TS
3
EC50 = 6300 nM
   TI
   LI
   LO
   TS
4
EC50 > 6000 nM
   TI
   LI
   LO
   TS
CP0911046
4alpha-Phorbol 13-decanoate
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C30H46O7
 1
1
EC50 = 450 nM
   TI
   LI
   LO
   TS
CP0858291
4alpha-Phorbol 12,13-dimyristate
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C48H80O8
 1
1
EC50 = 2830 nM
   TI
   LI
   LO
   TS
CP0654026
Butyric acid (1aS,1bS,4aS,7aS,8R,9S,9aR)-9-butyryloxy-4a,7b-dihydroxy-3-((R)-hydroxymethyl)-1,1,6,8-tetramethyl-5-oxo-1,1a,1b,4,4a,5,7a,7b,8,9-decahydro-cyclopropa[3,4]benzo[1,2-e]azulen-9a-yl ester
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C28H40O8
 1
1
EC50 = 22470 nM
   TI
   LI
   LO
   TS
CP0510011
4alpha-Phorbol 12,13-dinonanoate
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C38H60O8
 1
1
EC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0852735
4alpha-Phorbol 12,13-dioctanoate
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C36H56O8
 1
1
EC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0913804
4alpha-phorbol diacetate
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C24H32O8
 1
1
EC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0945225
4-Deoxy-4alpha-Phorbol 12,13-didecanoate
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C40H64O7
 1
1
EC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0350860
2-methyl-1-(3-morpholin-4-ylpropyl)-5-phenyl-N-[3-(trifluoromethyl)phenyl]pyrrole-3-carboxamide
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C26H28F3N3O2
 1
1
IC50 = 17 nM
   TI
   LI
   LO
   TS
CP0101210
2-nitro-N-[4-(4-propan-2-ylpiperazin-1-yl)sulfonylphenyl]-4-(trifluoromethyl)benzamide
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C21H23F3N4O5S
 2
1
IC50 = 57 nM
   TI
   LI
   LO
   TS
2
IC50 = 320 nM
   TI
   LI
   LO
   TS
CP0315551
2,4-dichloro-N-propan-2-yl-N-[2-(propan-2-ylamino)ethyl]benzenesulfonamide
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C14H22Cl2N2O2S
 1
1
IC50 = 5900 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0784818
4a-phorbol-12,13-didecanoate
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C40H64O8
 1
1 EC50 = 370 nM
CP0350860
2-methyl-1-(3-morpholin-4-ylpropyl)-5-phenyl-N-[3-(trifluoromethyl)phenyl]pyrrole-3-carboxamide
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C26H28F3N3O2
 1
1 IC50 = 17 nM
CP0315551
2,4-dichloro-N-propan-2-yl-N-[2-(propan-2-ylamino)ethyl]benzenesulfonamide
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C14H22Cl2N2O2S
 1
1 IC50 = 5900 nM
Similar Protein(s) and Bioactivity Statistics
90% Identity
Protein ID Protein Name Protein Organism
PT04567 Transient receptor potential cation channel subfamily V member 4 Rattus norvegicus, Rat