General Information of Target

Target ID LDTP04179
Target Name Transcription factor SOX-9 (SOX9)
Gene Name SOX9
Gene ID 6662
Synonyms
Transcription factor SOX-9
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MNLLDPFMKMTDEQEKGLSGAPSPTMSEDSAGSPCPSGSGSDTENTRPQENTFPKGEPDL
KKESEEDKFPVCIREAVSQVLKGYDWTLVPMPVRVNGSSKNKPHVKRPMNAFMVWAQAAR
RKLADQYPHLHNAELSKTLGKLWRLLNESEKRPFVEEAERLRVQHKKDHPDYKYQPRRRK
SVKNGQAEAEEATEQTHISPNAIFKALQADSPHSSSGMSEVHSPGEHSGQSQGPPTPPTT
PKTDVQPGKADLKREGRPLPEGGRQPPIDFRDVDIGELSSDVISNIETFDVNEFDQYLPP
NGHPGVPATHGQVTYTGSYGISSTAATPASAGHVWMSKQQAPPPPPQQPPQAPPAPQAPP
QPQAAPPQQPAAPPQQPQAHTLTTLSSEPGQSQRTHIKTEQLSPSHYSEQQQHSPQQIAY
SPFNLPHYSPSYPPITRSQYDYTDHQNSSSYYSHAAGQGTGLYSTFTYMNPAQRPMYTPI
ADTSGVPSIPQTHSPQHWEQPVYTQLTRP
Target Bioclass
Transcription factor
Subcellular location
Nucleus
Function
Transcription factor that plays a key role in chondrocytes differentiation and skeletal development. Specifically binds the 5'-ACAAAG-3' DNA motif present in enhancers and super-enhancers and promotes expression of genes important for chondrogenesis, including cartilage matrix protein-coding genes COL2A1, COL4A2, COL9A1, COL11A2 and ACAN, SOX5 and SOX6. Also binds to some promoter regions. Plays a central role in successive steps of chondrocyte differentiation. Absolutely required for precartilaginous condensation, the first step in chondrogenesis during which skeletal progenitors differentiate into prechondrocytes. Together with SOX5 and SOX6, required for overt chondrogenesis when condensed prechondrocytes differentiate into early stage chondrocytes, the second step in chondrogenesis. Later, required to direct hypertrophic maturation and block osteoblast differentiation of growth plate chondrocytes: maintains chondrocyte columnar proliferation, delays prehypertrophy and then prevents osteoblastic differentiation of chondrocytes by lowering beta-catenin (CTNNB1) signaling and RUNX2 expression. Also required for chondrocyte hypertrophy, both indirectly, by keeping the lineage fate of chondrocytes, and directly, by remaining present in upper hypertrophic cells and transactivating COL10A1 along with MEF2C. Low lipid levels are the main nutritional determinant for chondrogenic commitment of skeletal progenitor cells: when lipids levels are low, FOXO (FOXO1 and FOXO3) transcription factors promote expression of SOX9, which induces chondrogenic commitment and suppresses fatty acid oxidation. Mechanistically, helps, but is not required, to remove epigenetic signatures of transcriptional repression and deposit active promoter and enhancer marks at chondrocyte-specific genes. Acts in cooperation with the Hedgehog pathway-dependent GLI (GLI1 and GLI3) transcription factors. In addition to cartilage development, also acts as a regulator of proliferation and differentiation in epithelial stem/progenitor cells: involved in the lung epithelium during branching morphogenesis, by balancing proliferation and differentiation and regulating the extracellular matrix. Controls epithelial branching during kidney development.
Uniprot ID
P48436
Ensemble ID
ENST00000245479.3
HGNC ID
HGNC:11204
ChEMBL ID
CHEMBL4523231

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 10 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
STPyne
 Probe Info 
K141(8.80)  LDD0277  [1]
m-APA
 Probe Info 
12.30  LDD0403  [2]
DBIA
 Probe Info 
C72(4.21)  LDD3332  [3]
BTD
 Probe Info 
C72(1.67)  LDD2090  [4]
HHS-482
 Probe Info 
Y172(0.89)  LDD0285  [5]
HHS-475
 Probe Info 
Y127(0.21); Y172(1.50)  LDD0264  [6]
W1
 Probe Info 
C72(0.99)  LDD0239  [7]
NAIA_4
 Probe Info 
N.A.  LDD2226  [8]
ENE
 Probe Info 
N.A.  LDD0006  [9]
IPM
 Probe Info 
N.A.  LDD0005  [9]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0548  1-(4-(Benzo[d][1,3]dioxol-5-ylmethyl)piperazin-1-yl)-2-nitroethan-1-one MDA-MB-231 C72(1.24)  LDD2142  [4]
 LDCM0519  1-(6-methoxy-3,4-dihydroquinolin-1(2H)-yl)-2-nitroethan-1-one MDA-MB-231 C72(1.17)  LDD2112  [4]
 LDCM0510  3-(4-(Hydroxydiphenylmethyl)piperidin-1-yl)-3-oxopropanenitrile MDA-MB-231 C72(1.01)  LDD2103  [4]
 LDCM0156  Aniline NCI-H1299 12.30  LDD0403  [2]
 LDCM0116  HHS-0101 DM93 Y127(0.21); Y172(1.50)  LDD0264  [6]
 LDCM0117  HHS-0201 DM93 Y127(0.29); Y172(1.46)  LDD0265  [6]
 LDCM0118  HHS-0301 DM93 Y127(0.18); Y172(1.47)  LDD0266  [6]
 LDCM0119  HHS-0401 DM93 Y127(0.27); Y172(1.58)  LDD0267  [6]
 LDCM0120  HHS-0701 DM93 Y127(0.42); Y172(1.51)  LDD0268  [6]
 LDCM0123  JWB131 DM93 Y172(0.89)  LDD0285  [5]
 LDCM0124  JWB142 DM93 Y172(1.33)  LDD0286  [5]
 LDCM0125  JWB146 DM93 Y172(1.00)  LDD0287  [5]
 LDCM0126  JWB150 DM93 Y172(4.22)  LDD0288  [5]
 LDCM0127  JWB152 DM93 Y172(1.97)  LDD0289  [5]
 LDCM0128  JWB198 DM93 Y172(1.27)  LDD0290  [5]
 LDCM0129  JWB202 DM93 Y172(0.97)  LDD0291  [5]
 LDCM0130  JWB211 DM93 Y172(0.96)  LDD0292  [5]
 LDCM0022  KB02 22RV1 C72(2.53)  LDD2243  [3]
 LDCM0023  KB03 22RV1 C72(3.01)  LDD2660  [3]
 LDCM0024  KB05 MKN45 C72(4.21)  LDD3332  [3]
 LDCM0497  Nucleophilic fragment 11b MDA-MB-231 C72(1.67)  LDD2090  [4]
 LDCM0507  Nucleophilic fragment 16b MDA-MB-231 C72(3.03)  LDD2100  [4]
 LDCM0511  Nucleophilic fragment 18b MDA-MB-231 C72(1.61)  LDD2104  [4]
 LDCM0513  Nucleophilic fragment 19b MDA-MB-231 C72(1.68)  LDD2106  [4]
 LDCM0544  Nucleophilic fragment 39 MDA-MB-231 C72(1.14)  LDD2137  [4]
 LDCM0547  Nucleophilic fragment 41 MDA-MB-231 C72(1.36)  LDD2141  [4]
 LDCM0112  W16 Hep-G2 C72(0.99)  LDD0239  [7]

References

1 A Paal-Knorr agent for chemoproteomic profiling of targets of isoketals in cells. Chem Sci. 2021 Oct 15;12(43):14557-14563. doi: 10.1039/d1sc02230j. eCollection 2021 Nov 10.
Mass spectrometry data entry: PXD028270
2 Quantitative and Site-Specific Chemoproteomic Profiling of Targets of Acrolein. Chem Res Toxicol. 2019 Mar 18;32(3):467-473. doi: 10.1021/acs.chemrestox.8b00343. Epub 2019 Jan 15.
3 DrugMap: A quantitative pan-cancer analysis of cysteine ligandability. Cell. 2024 May 9;187(10):2536-2556.e30. doi: 10.1016/j.cell.2024.03.027. Epub 2024 Apr 22.
Mass spectrometry data entry: PXD047840
4 Nucleophilic covalent ligand discovery for the cysteine redoxome. Nat Chem Biol. 2023 Nov;19(11):1309-1319. doi: 10.1038/s41589-023-01330-5. Epub 2023 May 29.
Mass spectrometry data entry: PXD039908 , PXD029761
5 Chemoproteomic profiling of kinases in live cells using electrophilic sulfonyl triazole probes. Chem Sci. 2021 Jan 21;12(9):3295-3307. doi: 10.1039/d0sc06623k.
6 Discovery of a Cell-Active SuTEx Ligand of Prostaglandin Reductase 2. Chembiochem. 2021 Jun 15;22(12):2134-2139. doi: 10.1002/cbic.202000879. Epub 2021 Apr 29.
7 Oxidant-Induced Bioconjugation for Protein Labeling in Live Cells. ACS Chem Biol. 2023 Jan 20;18(1):112-122. doi: 10.1021/acschembio.2c00740. Epub 2022 Dec 21.
8 N-Acryloylindole-alkyne (NAIA) enables imaging and profiling new ligandable cysteines and oxidized thiols by chemoproteomics. Nat Commun. 2023 Jun 15;14(1):3564. doi: 10.1038/s41467-023-39268-w.
Mass spectrometry data entry: PXD041264
9 A modification-centric assessment tool for the performance of chemoproteomic probes. Nat Chem Biol. 2022 Aug;18(8):904-912. doi: 10.1038/s41589-022-01074-8. Epub 2022 Jul 21.
Mass spectrometry data entry: PXD027758 , PXD027755 , PXD027760 , PXD027762 , PXD027756 , PXD027591 , PXD007149 , PXD030064 , PXD032392 , PXD027789 , PXD027767 , PXD027764