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Chemical Probes
Chemical Probes
Potent, selective and cell-permeable inhibitors of protein function ("chemical probes") are valued reagents in both fundamental and applied biological research, and they are essential for the early stages of drug discovery by allowing preclinical target validation in both academic and industrial laboratories.
SGC chemical probes are open-access reagents that are meant to be used by the biomedical research community with no restrictions on use. To acquire a sample, follow the links on the webpage of your desired chemical probe. You can sort the table by clicking the column headers.
The SGC probes set is complemented by the donated probe set
Name | Structures | Protein family | Specific Targets | Control | In Vivo Activity* | Added |
---|---|---|---|---|---|---|
SKI-73 | Methyltransferase | CARM1 | SKI-73N | 07/17 | ||
MRK-740 | Methyltransferase | PRDM9 | MRK-740-NC | 06/18 | ||
SGC-SMARCA-BRDVIII | Bromodomains | PB1(5), SMARCA2/4 | SGC-BRDVIII-NC | 12/20 | ||
A-395 | WD40 repeat | EED | A-395N | 07/16 | ||
UNC6934 | Methyl Lysine Binder | NSD2-PWWP1 | UNC7145 | 06/19 | ||
BAY-6035 | Methyltransferase | SMYD3 | BAY-444 | 06/17 | ||
MSC1186 | Kinase | SRPK | MSC5360 | 01/23 | ||
TP-064 | Methyltransferase | CARM1 | TP-064N | 06/16 | ||
SGC-GAK-1 | Kinase | GAK | SGC-GAK-1N | 02/18 | ||
FM-381 | Kinase | JAK3 | FM-479 | 02/17 | ||
BI01383298 | Solute carriers | SLC13A5 | BI01372674 | 01/18 | ||
VinSpinIn | Spindlin domains | Spin1 | VinSpinIC | 09/18 | ||
SGC-CAF382-1 | Kinase | CDKL5 | SGC-CAF268-1N | 09/23 | ||
GSK8814 | Bromodomains | ATAD2, ATAD2B | GSK8815 | 01/17 | ||
JP3000 | RXRA, RXRB, RXRG | JP3001 | 10/23 | |||
TH-257 | Kinase | LIMK1, LIMK2 | TH-263 | 07/17 | ||
BI-9321 | Methyl Lysine Binder | NSD3 | BI-9466 | 07/18 | ||
JA397 | Kinase | CDK14-18 | JA314 | 07/23 | ||
LLY-283 | Methyltransferase | PRMT5 | LLY-284 | 07/16 | ||
SGC6870 | Methyltransferase | PRMT6 | SGC6870N | 06/19 | ||
PFI-5 | Methyltransferase | SMYD2 | PFI-5N | 07/17 | ||
SGC3027 | Methyltransferase | PRMT7 | SGC3027N | 03/18 | ||
SGC-CK2-2 | Kinase | CK2/CSNK2 | SGK-CK2-2N | 05/23 | ||
JA310 | Kinase | MST3, MST4 | JA262 | 11/23 | ||
GSK4027 | Bromodomains | KAT2A, KAT2B | GSK4028 | 06/17 | ||
SGC-AAK1-1 | Kinase | AAK1, BMP2K, BIKE | SGC-AAK1-1N | 02/18 | ||
TP-238 | Bromodomains | CECR2, BPTF | TP-422 | 09/18 | ||
BAY-850 | Bromodomains | ATAD2 | BAY-460 | 01/17 | ||
SGC-STK17B-1 | Kinase | STK17B, DRAK2 | SGC-STK17B-1N | 02/20 | ||
TH-257 | Kinase | LIMK1, LIMK2 | TH-263 | 07/23 | ||
SGC-CAMKK2-1 | Kinase | CAMKK1, CAMKK2 | SGC-CAMKK2-1N | No | 01/20 | |
Bromosporine (BSP) (tool compound) |
Bromodomains | pan-Bromodomain | No | 01/13 | ||
MRK-990 | Methyltransferase | PRMT9, PRMT5 | MRK-990-NC | No | 10/22 | |
SGC-CBP30 | Bromodomains | CREBBP, EP300 | BDOIA513 | No | 03/13 | |
UNC8732 | Methyl Lysine Binder | NSD2 | UNC8884 | No | 01/24 | |
MS023 | Methyltransferase | PRMT1, PRMT3, CARM1, PRMT6, PRMT8 | MS094 | No | 07/15 | |
FS-694 | Kinase | MAPK14 | FM-743 | No | 01/20 | |
GSK789 | Bromodomains | BRD2, BRD3, BRD4, BRDT | GSK791 | No | 02/21 | |
PFI-4 | Bromodomains | BRPF1 | No | 12/14 | ||
SGC-PI5P4Kγ/MYLK4-1 | Kinase | PI5P4K gamma, MYLK4 | SGC-PI5P4Kγ/MYLK4-1N | No | 05/23 | |
NVS-CECR2-1 | Bromodomains | CECR2 | NVS-CECR2-C | No | 06/15 | |
T3-CLK | Kinase | CLK1, CLK2, CLK3, CLK4 | T3-CLK-N | No | 04/19 | |
GSK-LSD1 | Lysine Demethylase | KDM1A/LSD1 | No | 03/14 | ||
PFI-2 | Methyltransferase | SETD7 | (S)-PFI-2 | No | 05/13 | |
PFI-8 | YEATS | YEATS | PFI-8N | No | 01/24 | |
MS049 | Methyltransferase | CARM1, PRMT6 | MS049N | No | 06/15 | |
SR-318 | Kinase | MAPK14 | SR-321 | No | 01/20 | |
BI-1942 | Protease | CMA1 | No | 06/21 | ||
PFI-6 | YEATS | MLLT1, MLLT3 | PFI-6N | No | 06/20 | |
A-366 | Methyltransferase | EHMT1/GLP, EHMT2/G9a | No | 06/13 | ||
NVS-BPTF-1 | Bromodomains | BPTF | NVS-BPTF-C | No | 02/19 | |
SGC-UBD253 | UBD (ubiquitin binding domain) | HDAC6 | SGC-UBD253N | No | 01/22 | |
LLY-507 (Multiple Off-target Effects) |
Methyltransferase | SMYD2 | SGC705 | No | 11/13 | |
SGC-GSK3-1 | Kinase | GSK3 | SGC-CDKL5/GSK3-1N | No | 09/23 | |
A-196 | Methyltransferase | SUV420H1, SUV420H2 | A-197, SGC2043 | No | 07/15 | |
NVS-MLLT-1 | YEATS | MLLT1, MLLT3 | NVS-iMLLT-C | No | 03/20 | |
BI-3812 | Transcription factor | BCL6 | BI-5273 | No | 11/23 | |
UNC0638 | Methyltransferase | EHMT2/G9a, EHMT1/GLP | UNC0737 | No | 06/10 | |
BI 99179 | Synthase | FASN | BI 99990 | No | 05/18 | |
NVS-PAK1-1 | Kinase | PAK1 | NVS-PAK1-C | No | 06/16 | |
SR-302 | Kinase | DDR1, DDR2, MAPK11, MAPK14 | SR-301 | No | 06/20 | |
PFI-7 | E3 ligase | GID4 | PFI-7N | No | 09/21 | |
NI-57 | Bromodomains | BRPF1, BRD1, BRPF3 | No | 12/14 | ||
BAY-885 | Kinase | MAPK7 | BAY-693 | No | 11/18 | |
SGC-CLK-1 | Kinase | CLK1, CLK2, CLK4 | SGC-CLK-1N | No | 02/20 | |
GSK343 | Methyltransferase | EZH2 | No | 08/12 | ||
MRK-952 | Hydrolase | NUDT5 | MRK-952-NC | No | 10/22 | |
SGC0946 | Methyltransferase | DOT1L | SGC0649 | No | 08/12 | |
TP-008 | Kinase | ACVR1B, TGFBR1 | Al11 | No | 06/19 | |
SGC-UBD1031 | UBD (ubiquitin binding domain) | SGC-UBD1031N | No | 05/24 | ||
GSK591 | Methyltransferase | PRMT5 | SGC2096 | No | 07/15 | |
BAY-3827 | Kinase | PRKAA1, RPS6KA1 | BAY-974 | No | 01/20 | |
Homer | WD40 repeat | WDR5 | nc_WDR5 and nc_VHL | No | 07/21 | |
IOX2 (requires >>> 1 microM for cell assays) |
2OG | PHD2 | No | 02/12 | ||
VZ185 | Bromodomain-containing protein family | BRD7, BRD9 | cisVZ185 | No | 01/24 | |
IPP/CNRS-A017 | Dehydrogenase | DHODH | IPP/CNRS-A019 | No | 10/19 | |
PFI-1 | Bromodomains | BRD2, BRD3, BRD4, BRDT | No | 11/11 | ||
SGC-PIKFYVE-1 | Kinase | PIKfyve | SGC-PIKFYVE-1N | No | 10/22 | |
PFI-3 | Bromodomains | SMARCA2, PBRM1, SMARCA4 | PFI-3oMet | No | 11/13 | |
OICR11029 | Transcription factor | BCL6 | OICR11600 | No | 01/24 | |
NR162 | Kinase | CASK | NR187 | No | 09/20 | |
OF-1 | Bromodomains | BRPF1, BRD1, BRPF3 | No | 07/14 | ||
A-1596586 | Ion channel | CFTR | A-1596584 | No | 06/19 | |
(R)-ZINC-3573 | GPCR | MRGPRX2 | (S)-ZINC-3573 | No | 06/20 | |
BTZO-1 | Cytokine | MIF | BTZO-4 | No | 05/18 | |
MU1210 | Kinase | CLK1, CLK2, CLK4, DYRK1A, DYRK1B, DYRK2 | MU140 | No | 05/19 | |
BAY-091 | Kinase | PIP4K2A | BAY-0361 | No | 10/21 | |
BAY-293 | Nucleotide exchange factor | SOS1 | BAY-294 | No | 04/19 | |
OICR-9429 | WD40 repeat | WDR5 | OICR-0547 | No | 05/14 | |
SGC-CK2-1 | Kinase | CSNK2A1, CSNK2A2 | SGC-CK2-1N | No | 06/20 | |
IOX1 (tool compound) |
2OG | Pan-KDM | No | 01/12 | ||
UNC1215 | Methyl Lysine Binder | L3MBTL3 | UNC1079 | No | 08/12 | |
BAY-299 | Bromodomains | TAF1, BRD1 | BAY-364 | No | 06/16 | |
CK156 | Kinase | STK17A, DRAK1 | CKJB71 | No | 10/21 | |
SGC-CDKL5_GSK3 | Kinase | CDKL5, GSK3 | SGC-CDKL5/GSK3-1N | No | 09/23 | |
LP99 | Bromodomains | BRD9, BRD7 | 2S,3R-enantiomer | No | 12/14 | |
I-CBP112 | Bromodomains | CREBBP, EP300 | No | 03/13 | ||
BAY-805 | USP (ubiquitin specific protease) | USP21 | BAY-728 | No | 10/22 | |
BI-3802 | Transcription factor | BCL6 | BI-5273 | No | 11/23 | |
SGC707 | Methyltransferase | PRMT3 | XY1 | No | 06/14 | |
GSK-J1 use pro-drug GSK-J4 for cell assays |
Lysine Demethylase | KDM6B/JMJD3, KDM6A/UTX, KDM5B/JARID1B | GSK-J2 (GSK-J5) | No | 07/12 | |
SGK3-PROTAC1 | Kinase | SGK3 | cisSGK3-PROTAC1 | No | 01/24 | |
I-BRD9 | Bromodomains | BRD9 | No | 05/15 | ||
BI-4394 | Protease | MMP13 | BI-4395 | Yes | 11/18 | |
BAY1125976 | Kinase | AKT1/2 | BAY-940 | Yes | 11/21 | |
FHT-2344 | SWI/SNF | SMARCA2, SMARCA4 | FHT-5908 | Yes | 09/23 | |
MLi-2 | Kinase | LRRK2 | MLi-2-NC | Yes | 05/19 | |
PF-05105679 | Ion channel | TRPM8 | PF-05257137 | Yes | 05/18 | |
8RK64 | Regulator protein | UCHL1 | JYQ88 | Yes | 09/21 | |
BAY-784 | GPCR | GNRHR | BAY-786 | Yes | 11/18 | |
CCT369260 | Transcription factor | BCL6 | CCT393732 | Yes | 09/22 | |
BAY-277 | Aminopeptidase | METAP2 | BAY-8805 | Yes | 01/24 | |
MSD-M1PAM | GPCR | CHRM1 | MSD-M1PAM-NC | Yes | 08/19 | |
BI 665915 | Lipoxygenase | ALOX5AP | BI-0153 | Yes | 05/18 | |
TP-030-1 | Kinase | RIPK1 | TP-030n | Yes | 09/20 | |
ABT-100 | Transferase | FNTB | A-108 | Yes | 05/18 | |
Borussertib | Kinase | AKT1, AKT2 | RL2578 | Yes | 10/21 | |
MU1700 | Kinase | ALK1, ALK2 | MU1700NC | Yes | 02/22 | |
TP-060 | Glucosyltransferase | UGCG | TP-060n | Yes | 09/23 | |
BI-1935 | Hydrolase | EPHX2 | BI-2049 | Yes | 05/18 | |
BAY-3153 | GPCR | CCR1 | BAY-173 | Yes | 02/21 | |
BAY-678 | Protease | ELANE | BAY-677 | Yes | 05/18 | |
BI-1950 | Integrin | ITGAL | BI-9446 | Yes | 11/18 | |
JNJ-6204 | Kinase | CSNK1D/CSNK1E | JNJ-0293 | Yes | 09/22 | |
BAY 1753011 | GPCR | AVPR1A, AVPR2 | BAY-2297 | Yes | 12/23 | |
UNC1999 | Methyltransferase | EZH2 | UNC2400 | Yes | 05/13 | |
MSD-CYP11B2 | Cytochrome P450 | CYP11B2 | MSD-CYP11B2 Negative control | Yes | 06/19 | |
ERKi | Kinase | MAPK3, MAPK1 | ERKi-NC | Yes | 05/18 | |
Ogerin | GPCR | GPR68 | ZINC32547799 | Yes | 06/20 | |
BAY-386 | GPCR | F2R | BAY-448 | Yes | 05/18 | |
MSC-4381 | Monocarboxylate transporter | SLC16A3 | MSC-0516 | Yes | 09/21 | |
A-192621 | GPCR | EDNRB | A-1806262 | Yes | 03/19 | |
JNJ-4355 | BCL2 protein family | MCL1 | JNJ-78732576 | Yes | 09/23 | |
BI-5524 | Chymotrypsin | ELANE | BI-5525 | Yes | 01/24 | |
BAY-899 | GPCR | LHCGR | BAY-897 | Yes | 01/20 | |
MRK-560 | Protease | Gamma secretase complex | GSI-NC | Yes | 05/18 | |
BI 207127 | RNA polymerase | HCV NS5B | BI-7656 | Yes | 11/20 | |
T-26c | Protease | MMP13 | T-26f | Yes | 05/18 | |
GSK973 | Bromodomains | BRD2, BRD3, BRD4, BRDT | GSK943 | Yes | 02/21 | |
BI 639667 | GPCR | CCR1 | BI-9307 | Yes | 11/18 | |
TP-051 | GPCR | FFAR1 | TP-051n | Yes | 09/22 | |
UNC0642 | Methyltransferase | EHMT2/G9a, EHMT1/GLP | Yes | 08/12 | ||
MU1742 | Kinase | CK1δ, CK1ε | MU2027 | Yes | 10/22 | |
PPTN | GPCR | P2RY14 | PPTN-NC | Yes | 06/19 | |
A-485 | Transferase | EP300, CREBBP | A-486 | Yes | 05/18 | |
JNJ-54119936 | Nuclear hormone receptor | RORC | JNJ-53721590 | Yes | 09/21 | |
TP-024 | GPCR | GPR52 | TP-024n | Yes | 11/18 | |
BAY 1816032 | Kinase | BUB1 | BAY-283 | Yes | 10/22 | |
GSK2801 | Bromodomains | BAZ2A, BAZ2B | GSK8573 | Yes | 12/14 | |
BIBO3304 | GPCR | NPY1R | BIBO3457 | Yes | 01/24 | |
A-1155463 | Regulator protein | BCL2L1 | A-1107969 | Yes | 11/19 | |
MRL-650 | GPCR | CNR1 | MRL-CB1-NC | Yes | 05/18 | |
BAY-390 | Ion channel | TRPA1 | BAY-9897 | Yes | 09/20 | |
PF-04457845 | Hydrolase | FAAH | PF-04875474 | Yes | 05/18 | |
GSK046 | Bromodomains | BRD2, BRD3, BRD4, BRDT | Yes | 02/21 | ||
GNE-2256 | Kinase | IRAK4 | GNE-6689 | Yes | 11/21 | |
TP-004 | Protease | METAP2 | TPn-004 | Yes | 05/18 | |
TP-040 | Hydrolase | OGA | TP-040n | Yes | 09/21 | |
TP-020 | Transferase | MGAT2 | TP-020n | Yes | 11/18 | |
SAFit2 | Isomerase | FKBP5 | ddSAFit2 | Yes | 09/22 | |
BI-9564 | Bromodomains | BRD9, BRD7 | Yes | 04/15 | ||
BAY-826 | Kinase | TIE1, TEK, DDR1, DDR2 | BAY-309 | Yes | 05/18 | |
TP-030-2 | Kinase | RIPK1 | TP-030n | Yes | 09/20 | |
(R)-9s | GPCR | ADRA1D | (S)-9s | Yes | 05/18 | |
JNJ-65355394 | Hydrolase | OGA | JNJ-73924149 | Yes | 11/21 | |
BI-3231 | 17β-hydroxysteroid dehydrogenases | HSD17B13 | BI-0955 | Yes | 09/23 | |
UCSF924 | GPCR | DRD4 | UCSF924NC | Yes | 04/19 | |
GSK484 | Arginine deiminases | PAD4 | GSK106 | Yes | 03/15 | |
Skepinone-L | Kinase | MAPK14 | FM-743 | Yes | 01/20 | |
PF-04418948 | GPCR | PTGER2 | PF-04475866 | Yes | 05/18 | |
GSK778 | Bromodomains | BRD2, BRD3, BRD4, BRDT | Yes | 02/21 | ||
A-079 | Ion channel | TRPA1 | A-226 | Yes | 11/18 | |
A-446 | Hydrolase | GLS | A-426 | Yes | 07/21 | |
BAY-1797 | Ion channel | P2X4 | BAY-207 | Yes | 11/18 | |
JNJ-39758979 | GPCR | HRH4 | JNJ-39668551 | Yes | 09/22 | |
BAZ2-ICR | Bromodomains | BAZ2A, BAZ2B | Yes | 05/14 | ||
BAY-6096 | GPCR | ADRA2B | BAY-726 | Yes | 12/23 | |
ABT-724 | GPCR | DRD4 | A-769 | Yes | 05/18 | |
TP-472 | Bromodomains | BRD9, BRD7 | TP-472N | Yes | 06/16 | |
M4K2234 | Kinase | ALK1, ALK2 | M4K2234NC | Yes | 02/22 | |
JNJ-42226314 | Serine hydrolase | MGLL | JNJ-8034 | Yes | 09/23 | |
BAY-598 | Methyltransferase | SMYD2 | BAY-369 | Yes | 04/15 | |
BAY-179 | Complex I | BAY-070 | Yes | 01/20 | ||
GSM1 | Protease | Gamma secretase complex | GSM-NC | Yes | 05/18 | |
BAY-6672 | GPCR | PTGFR | BAY-403 | Yes | 11/20 | |
BAY-876 | Solute carriers | SLC2A1 | BAY-588 | Yes | 05/18 | |
BI 605906 | Kinase | IKBKB | BI-5026 | Yes | 06/21 | |
BI 653048 | Nuclear hormone receptor | NR3C1 | BI-3047 | Yes | 11/18 | |
BI-2081 | GPCR | FFAR1 | BI-0340 | Yes | 09/22 | |
CS640 | Kinase | CAMK1 | CS640s | Yes | 01/23 | |
BI-8668 | Sodium channels | Epithelial sodium channel (ENaC) | BI-0337 | Yes | 11/23 | |
THPP-1 | Phosphodiesterase | PDE10A | THPP-1-NC | Yes | 06/19 | |
BAY-7598 | Protease | MMP12 | BAY-694 | Yes | 05/18 | |
WM-1119 | Transferase | KAT6A, KAT6B | WM-2474 | Yes | 06/20 | |
BAY-707 | Hydrolase | NUDT1 | BAY-604 | Yes | 05/18 | |
PFI-653 | Hydrolase | VNN1 | PFI-653-N | Yes | 09/21 | |
BI-1230 | Protease | HCV NS3 | BI-1675 | Yes | 03/19 | |
BAY-7081 | Phoshodiesterase | PDE9A | BAY-7424 | Yes | 09/23 | |
JQ1 | Bromodomains | BRD2, BRD3, BRD4, BRDT | (-)-JQ1 | Yes | 06/10 | |
WEB2086 | GPCR | PTAFR | WEB2387 | Yes | 01/24 | |
BAY-985 | Kinase | TBK1, IKBKE | BAY-440 | Yes | 01/20 | |
MRL-SYKi | Kinase | SYK | MRL-SYKi-NC | Yes | 05/18 | |
BI-2540 | Reverse transcriptase | HIV NNRT | BI-2439 | Yes | 11/20 | |
ABT-546 | GPCR | EDNRA | A-545 | Yes | 05/18 | |
GSK620 | Bromodomains | BRD2, BRD3, BRD4, BRDT | Yes | 02/21 | ||
BI-2545 | Phosphodiesterase | ENPP2 | BI-3017 | Yes | 11/18 | |
TP-050 | Ion channel | GRIN2A | TP-050n | Yes | 09/22 | |
BAY-549 | Kinase | ROCK1, ROCK2 | BAY-4900 | Yes | 06/19 | |
BAY-474 | Kinase | MET | BAY-827 | Yes | 05/18 | |
GSK864 | Dehydrogenase | IDH1 | GSK990 | Yes | 11/15 | |
NVS-MALT1 | Protease | MALT1 | NVS-MALT1-C | Yes | 02/20 | |
BI-9627 | Solute carriers | SLC9A1 | BI-0054 | Yes | 05/18 | |
L-Moses | Bromodomains | KAT2A, KAT2B | D-Moses | Yes | 10/17 | |
DDR-TRK-1 | Kinase | DDR, TRK | DDR-TRK-1N | Yes | 08/18 | |
JNJ-42396302 | Phosphodiesterase | PDE10A | JNJ-40573663 | Yes | 09/21 | |
TP-021 | Transcription factor | BCL6 | TP-021n | Yes | 11/18 | |
MRIA9 | Kinase | SIK1, SIK2, SIK3 | MR7 | Yes | 08/21 | |
JNJ-9350 | Oxidase | SMOX | JNJ-4545 | Yes | 09/22 | |
A-1211212 | Regulator protein | BCL2 | A-1210227 | Yes | 11/19 | |
CRTH2 antagonist | GPCR | PTGDR2 | CRTH2 negative control | Yes | 05/18 | |
GSK6853 | Bromodomains | BRPF1 | GSK9311 | Yes | 01/17 | |
BAY-069 | Amino acid transaminase | BCAT1, BCAT2 | BAY-771 | Yes | 09/20 | |
KISS1-305 | GPCR | KISS1R | KISS1-543 | Yes | 05/18 |
Chemical Handles
This versatile modality can be used to develop tools for proximity-inducing chemistry, tracers for target engagement assays, PROTACs, chemical inducers of degradation, and pull-down reagents. Handles bind their target with Kd < 1 micromolar. Their selectivity and cell activity has not been determined.
Chemical Handle | Chemical Probe | Structures | Protein family | Specific Targets | Control | In Vivo Activity* | Added |
---|---|---|---|---|---|---|---|
PFI-E3H1 | PFI-7 | E3 ligase | GID4 | PFI-7N | No | 09/21 |
Please select a protein family