General Information of Target

Target ID LDTP04157
Target Name Stromal cell-derived factor 1 (CXCL12)
Gene Name CXCL12
Gene ID 6387
Synonyms
SDF1; SDF1A; SDF1B; Stromal cell-derived factor 1; SDF-1; hSDF-1; C-X-C motif chemokine 12; Intercrine reduced in hepatomas; IRH; hIRH; Pre-B cell growth-stimulating factor; PBSF) [Cleaved into: SDF-1-beta(3-72; SDF-1-alpha(3-67)]
3D Structure
Download
2D Sequence (FASTA)
Download
3D Structure (PDB)
Download
Sequence
MNAKVVVVLVLVLTALCLSDGKPVSLSYRCPCRFFESHVARANVKHLKILNTPNCALQIV
ARLKNNNRQVCIDPKLKWIQEYLEKALNKRFKM
Target Type
Clinical trial
Target Bioclass
Cytokine and receptor
Family
Intercrine alpha (chemokine CxC) family
Subcellular location
Secreted
Function
Chemoattractant active on T-lymphocytes and monocytes but not neutrophils. Activates the C-X-C chemokine receptor CXCR4 to induce a rapid and transient rise in the level of intracellular calcium ions and chemotaxis. SDF-1-beta(3-72) and SDF-1-alpha(3-67) show a reduced chemotactic activity. Binding to cell surface proteoglycans seems to inhibit formation of SDF-1-alpha(3-67) and thus to preserve activity on local sites. Also binds to atypical chemokine receptor ACKR3, which activates the beta-arrestin pathway and acts as a scavenger receptor for SDF-1. Binds to the allosteric site (site 2) of integrins and activates integrins ITGAV:ITGB3, ITGA4:ITGB1 and ITGA5:ITGB1 in a CXCR4-independent manner. Acts as a positive regulator of monocyte migration and a negative regulator of monocyte adhesion via the LYN kinase. Stimulates migration of monocytes and T-lymphocytes through its receptors, CXCR4 and ACKR3, and decreases monocyte adherence to surfaces coated with ICAM-1, a ligand for beta-2 integrins. SDF1A/CXCR4 signaling axis inhibits beta-2 integrin LFA-1 mediated adhesion of monocytes to ICAM-1 through LYN kinase. Inhibits CXCR4-mediated infection by T-cell line-adapted HIV-1. Plays a protective role after myocardial infarction. Induces down-regulation and internalization of ACKR3 expressed in various cells. Has several critical functions during embryonic development; required for B-cell lymphopoiesis, myelopoiesis in bone marrow and heart ventricular septum formation. Stimulates the proliferation of bone marrow-derived B-cell progenitors in the presence of IL7 as well as growth of stromal cell-dependent pre-B-cells.
TTD ID
T04773
Uniprot ID
P48061
DrugMap ID
TT4UGTF
Ensemble ID
ENST00000343575.11
HGNC ID
HGNC:10672
ChEMBL ID
CHEMBL3286074

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 2 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info 
C71(1.13)  LDD1508  [1]
NAIA_5
 Probe Info 
N.A.  LDD2223  [2]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0215  AC10 HEK-293T C71(1.13)  LDD1508  [1]
 LDCM0277  AC18 HEK-293T C71(0.99)  LDD1516  [1]
 LDCM0279  AC2 HEK-293T C71(1.11)  LDD1518  [1]
 LDCM0281  AC21 HEK-293T C71(1.02)  LDD1520  [1]
 LDCM0286  AC26 HEK-293T C71(1.03)  LDD1525  [1]
 LDCM0289  AC29 HEK-293T C71(0.97)  LDD1528  [1]
 LDCM0295  AC34 HEK-293T C71(1.17)  LDD1534  [1]
 LDCM0298  AC37 HEK-293T C71(1.22)  LDD1537  [1]
 LDCM0304  AC42 HEK-293T C71(1.12)  LDD1543  [1]
 LDCM0307  AC45 HEK-293T C71(1.15)  LDD1546  [1]
 LDCM0312  AC5 HEK-293T C71(1.11)  LDD1551  [1]
 LDCM0313  AC50 HEK-293T C71(1.14)  LDD1552  [1]
 LDCM0316  AC53 HEK-293T C71(1.10)  LDD1555  [1]
 LDCM0321  AC58 HEK-293T C71(1.09)  LDD1560  [1]
 LDCM0325  AC61 HEK-293T C71(1.24)  LDD1564  [1]
 LDCM0248  AKOS034007472 HEK-293T C71(1.04)  LDD1511  [1]
 LDCM0372  CL103 HEK-293T C71(1.12)  LDD1576  [1]
 LDCM0376  CL107 HEK-293T C71(0.97)  LDD1580  [1]
 LDCM0381  CL111 HEK-293T C71(0.99)  LDD1585  [1]
 LDCM0385  CL115 HEK-293T C71(1.07)  LDD1589  [1]
 LDCM0389  CL119 HEK-293T C71(1.08)  LDD1593  [1]
 LDCM0394  CL123 HEK-293T C71(1.14)  LDD1598  [1]
 LDCM0398  CL127 HEK-293T C71(1.09)  LDD1602  [1]
 LDCM0402  CL15 HEK-293T C71(1.24)  LDD1606  [1]
 LDCM0405  CL18 HEK-293T C71(1.06)  LDD1609  [1]
 LDCM0409  CL21 HEK-293T C71(1.00)  LDD1613  [1]
 LDCM0415  CL27 HEK-293T C71(1.03)  LDD1619  [1]
 LDCM0418  CL3 HEK-293T C71(0.96)  LDD1622  [1]
 LDCM0419  CL30 HEK-293T C71(1.08)  LDD1623  [1]
 LDCM0422  CL33 HEK-293T C71(1.24)  LDD1626  [1]
 LDCM0428  CL39 HEK-293T C71(0.98)  LDD1632  [1]
 LDCM0432  CL42 HEK-293T C71(1.03)  LDD1636  [1]
 LDCM0435  CL45 HEK-293T C71(1.12)  LDD1639  [1]
 LDCM0445  CL54 HEK-293T C71(1.25)  LDD1648  [1]
 LDCM0448  CL57 HEK-293T C71(1.20)  LDD1651  [1]
 LDCM0451  CL6 HEK-293T C71(1.05)  LDD1654  [1]
 LDCM0455  CL63 HEK-293T C71(1.05)  LDD1658  [1]
 LDCM0458  CL66 HEK-293T C71(1.14)  LDD1661  [1]
 LDCM0461  CL69 HEK-293T C71(1.08)  LDD1664  [1]
 LDCM0471  CL78 HEK-293T C71(1.03)  LDD1674  [1]
 LDCM0475  CL81 HEK-293T C71(1.11)  LDD1678  [1]
 LDCM0481  CL87 HEK-293T C71(1.03)  LDD1684  [1]
 LDCM0484  CL9 HEK-293T C71(1.12)  LDD1687  [1]
 LDCM0485  CL90 HEK-293T C71(1.34)  LDD1688  [1]
 LDCM0488  CL93 HEK-293T C71(1.24)  LDD1691  [1]
 LDCM0494  CL99 HEK-293T C71(1.06)  LDD1697  [1]
 LDCM0495  E2913 HEK-293T C71(1.03)  LDD1698  [1]
 LDCM0468  Fragment33 HEK-293T C71(1.00)  LDD1671  [1]
 LDCM0022  KB02 MGG123 C55(1.20)  LDD2469  [3]
 LDCM0023  KB03 MGG123 C55(1.51)  LDD2886  [3]
 LDCM0024  KB05 MGG123 C55(1.56)  LDD3303  [3]

References

1 Accelerating multiplexed profiling of protein-ligand interactions: High-throughput plate-based reactive cysteine profiling with minimal input. Cell Chem Biol. 2024 Mar 21;31(3):565-576.e4. doi: 10.1016/j.chembiol.2023.11.015. Epub 2023 Dec 19.
Mass spectrometry data entry: PXD044402
2 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
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