| ||
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 |
---|---|---|---|---|---|---|
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 | ||
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 | ||
SGC-GAK-1 | Kinase | GAK | SGC-GAK-1N | 02/18 | ||
JP3000 | RXRA, RXRB, RXRG | JP3001 | 10/23 | |||
MSC1186 | Kinase | SRPK | MSC5360 | 01/23 | ||
TP-064 | Methyltransferase | CARM1 | TP-064N | 06/16 | ||
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 | ||
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-CK2-1 | Kinase | CSNK2A1, CSNK2A2 | SGC-CK2-1N | No | 06/20 | |
IOX1 (tool compound) |
2OG | Pan-KDM | No | 01/12 | ||
FS-694 | Kinase | MAPK14 | FM-743 | No | 01/20 | |
UNC1215 | Methyl Lysine Binder | L3MBTL3 | UNC1079 | No | 08/12 | |
GSK789 | Bromodomains | BRD2, BRD3, BRD4, BRDT | GSK791 | No | 02/21 | |
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 | |
SR-318 | Kinase | MAPK14 | SR-321 | No | 01/20 | |
SGC707 | Methyltransferase | PRMT3 | XY1 | No | 06/14 | |
BI 99179 | Synthase | FASN | BI 99990 | No | 05/18 | |
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 | |
I-BRD9 | Bromodomains | BRD9 | No | 05/15 | ||
BI-1942 | Protease | CMA1 | No | 06/21 | ||
BAY-885 | Kinase | MAPK7 | BAY-693 | No | 11/18 | |
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 | |
BI-3812 | Transcription factor | BCL6 | BI-5273 | No | 11/23 | |
PFI-4 | Bromodomains | BRPF1 | No | 12/14 | ||
SGC-PI5P4Kγ/MYLK4-1 | Kinase | PI5P4K gamma, MYLK4 | SGC-PI5P4Kγ/MYLK4-1N | No | 05/23 | |
SR-302 | Kinase | DDR1, DDR2, MAPK11, MAPK14 | SR-301 | No | 06/20 | |
NVS-CECR2-1 | Bromodomains | CECR2 | NVS-CECR2-C | No | 06/15 | |
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 | |
PFI-6 | YEATS | MLLT1, MLLT3 | PFI-6N | No | 06/20 | |
TP-008 | Kinase | ACVR1B, TGFBR1 | Al11 | No | 06/19 | |
A-366 | Methyltransferase | EHMT1/GLP, EHMT2/G9a | No | 06/13 | ||
BAY-3827 | Kinase | PRKAA1, RPS6KA1 | BAY-974 | No | 01/20 | |
BTZO-1 | Cytokine | MIF | BTZO-4 | No | 05/18 | |
NVS-BPTF-1 | Bromodomains | BPTF | NVS-BPTF-C | No | 02/19 | |
BAY-293 | Nucleotide exchange factor | SOS1 | BAY-294 | No | 04/19 | |
VZ185 | Bromodomain-containing protein family | BRD7, BRD9 | cisVZ185 | No | 01/24 | |
SGC-UBD253 | UBD (ubiquitin binding domain) | HDAC6 | SGC-UBD253N | No | 01/22 | |
IPP/CNRS-A017 | Dehydrogenase | DHODH | IPP/CNRS-A019 | No | 10/19 | |
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 | |
UNC0638 | Methyltransferase | EHMT2/G9a, EHMT1/GLP | UNC0737 | No | 06/10 | |
NVS-PAK1-1 | Kinase | PAK1 | NVS-PAK1-C | No | 06/16 | |
PFI-7 | E3 ligase | GID4 | PFI-7N | No | 09/21 | |
A-1596586 | Ion channel | CFTR | A-1596584 | No | 06/19 | |
(R)-ZINC-3573 | GPCR | MRGPRX2 | (S)-ZINC-3573 | No | 06/20 | |
NI-57 | Bromodomains | BRPF1, BRD1, BRPF3 | No | 12/14 | ||
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 | |
GSK591 | Methyltransferase | PRMT5 | SGC2096 | No | 07/15 | |
BAY-091 | Kinase | PIP4K2A | BAY-0361 | No | 10/21 | |
Homer | WD40 repeat | WDR5 | nc_WDR5 and nc_VHL | No | 07/21 | |
IOX2 (requires >>> 1 microM for cell assays) |
2OG | PHD2 | No | 02/12 | ||
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 | |
BI-3802 | Transcription factor | BCL6 | BI-5273 | No | 11/23 | |
NR162 | Kinase | CASK | NR187 | No | 09/20 | |
OF-1 | Bromodomains | BRPF1, BRD1, BRPF3 | No | 07/14 | ||
MU1210 | Kinase | CLK1, CLK2, CLK4, DYRK1A, DYRK1B, DYRK2 | MU140 | No | 05/19 | |
T3-CLK | Kinase | CLK1, CLK2, CLK3, CLK4 | T3-CLK-N | No | 04/19 | |
SGK3-PROTAC1 | Kinase | SGK3 | cisSGK3-PROTAC1 | No | 01/24 | |
OICR-9429 | WD40 repeat | WDR5 | OICR-0547 | No | 05/14 | |
BI-1950 | Integrin | ITGAL | BI-9446 | Yes | 11/18 | |
FHT-2344 | SWI/SNF | SMARCA2, SMARCA4 | FHT-5908 | Yes | 09/23 | |
MLi-2 | Kinase | LRRK2 | MLi-2-NC | Yes | 05/19 | |
CS640 | Kinase | CAMK1 | CS640s | Yes | 01/23 | |
ERKi | Kinase | MAPK3, MAPK1 | ERKi-NC | Yes | 05/18 | |
BAY-386 | GPCR | F2R | BAY-448 | Yes | 05/18 | |
BAY1125976 | Kinase | AKT1/2 | BAY-940 | Yes | 11/21 | |
T-26c | Protease | MMP13 | T-26f | Yes | 05/18 | |
CCT369260 | Transcription factor | BCL6 | CCT393732 | Yes | 09/22 | |
A-192621 | GPCR | EDNRB | A-1806262 | Yes | 03/19 | |
BAY-277 | Aminopeptidase | METAP2 | BAY-8805 | Yes | 01/24 | |
MSD-M1PAM | GPCR | CHRM1 | MSD-M1PAM-NC | Yes | 08/19 | |
JQ1 | Bromodomains | BRD2, BRD3, BRD4, BRDT | (-)-JQ1 | Yes | 06/10 | |
TP-030-1 | Kinase | RIPK1 | TP-030n | Yes | 09/20 | |
MRK-560 | Protease | Gamma secretase complex | GSI-NC | Yes | 05/18 | |
8RK64 | Regulator protein | UCHL1 | JYQ88 | Yes | 09/21 | |
L-Moses | Bromodomains | KAT2A, KAT2B | D-Moses | Yes | 10/17 | |
BI 639667 | GPCR | CCR1 | BI-9307 | Yes | 11/18 | |
TP-060 | Glucosyltransferase | UGCG | TP-060n | Yes | 09/23 | |
BAY-3153 | GPCR | CCR1 | BAY-173 | Yes | 02/21 | |
GSK864 | Dehydrogenase | IDH1 | GSK990 | Yes | 11/15 | |
A-485 | Transferase | EP300, CREBBP | A-486 | Yes | 05/18 | |
Borussertib | Kinase | AKT1, AKT2 | RL2578 | Yes | 10/21 | |
DDR-TRK-1 | Kinase | DDR, TRK | DDR-TRK-1N | Yes | 08/18 | |
TP-024 | GPCR | GPR52 | TP-024n | Yes | 11/18 | |
BAY 1753011 | GPCR | AVPR1A, AVPR2 | BAY-2297 | Yes | 12/23 | |
MRIA9 | Kinase | SIK1, SIK2, SIK3 | MR7 | Yes | 08/21 | |
MSD-CYP11B2 | Cytochrome P450 | CYP11B2 | MSD-CYP11B2 Negative control | Yes | 06/19 | |
Ogerin | GPCR | GPR68 | ZINC32547799 | Yes | 06/20 | |
MRL-650 | GPCR | CNR1 | MRL-CB1-NC | Yes | 05/18 | |
GSK6853 | Bromodomains | BRPF1 | GSK9311 | Yes | 01/17 | |
PF-04457845 | Hydrolase | FAAH | PF-04875474 | Yes | 05/18 | |
JNJ-6204 | Kinase | CSNK1D/CSNK1E | JNJ-0293 | Yes | 09/22 | |
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 | |
BI 207127 | RNA polymerase | HCV NS5B | BI-7656 | Yes | 11/20 | |
TP-004 | Protease | METAP2 | TPn-004 | Yes | 05/18 | |
MSC-4381 | Monocarboxylate transporter | SLC16A3 | MSC-0516 | Yes | 09/21 | |
TP-020 | Transferase | MGAT2 | TP-020n | Yes | 11/18 | |
PPTN | GPCR | P2RY14 | PPTN-NC | Yes | 06/19 | |
BAY-826 | Kinase | TIE1, TEK, DDR1, DDR2 | BAY-309 | Yes | 05/18 | |
GSK973 | Bromodomains | BRD2, BRD3, BRD4, BRDT | GSK943 | Yes | 02/21 | |
(R)-9s | GPCR | ADRA1D | (S)-9s | Yes | 05/18 | |
TP-051 | GPCR | FFAR1 | TP-051n | Yes | 09/22 | |
A-079 | Ion channel | TRPA1 | A-226 | Yes | 11/18 | |
BAY 1816032 | Kinase | BUB1 | BAY-283 | Yes | 10/22 | |
UCSF924 | GPCR | DRD4 | UCSF924NC | Yes | 04/19 | |
BIBO3304 | GPCR | NPY1R | BIBO3457 | Yes | 01/24 | |
MU1700 | Kinase | ALK1, ALK2 | MU1700NC | Yes | 02/22 | |
A-1155463 | Regulator protein | BCL2L1 | A-1107969 | Yes | 11/19 | |
BAY-390 | Ion channel | TRPA1 | BAY-9897 | Yes | 09/20 | |
PF-04418948 | GPCR | PTGER2 | PF-04475866 | Yes | 05/18 | |
JNJ-54119936 | Nuclear hormone receptor | RORC | JNJ-53721590 | Yes | 09/21 | |
BAY-1797 | Ion channel | P2X4 | BAY-207 | Yes | 11/18 | |
UNC1999 | Methyltransferase | EZH2 | UNC2400 | Yes | 05/13 | |
ABT-724 | GPCR | DRD4 | A-769 | Yes | 05/18 | |
GSK046 | Bromodomains | BRD2, BRD3, BRD4, BRDT | Yes | 02/21 | ||
GNE-2256 | Kinase | IRAK4 | GNE-6689 | Yes | 11/21 | |
BAY-876 | Solute carriers | SLC2A1 | BAY-588 | Yes | 05/18 | |
SAFit2 | Isomerase | FKBP5 | ddSAFit2 | Yes | 09/22 | |
TP-030-2 | Kinase | RIPK1 | TP-030n | Yes | 09/20 | |
GSM1 | Protease | Gamma secretase complex | GSM-NC | Yes | 05/18 | |
TP-040 | Hydrolase | OGA | TP-040n | Yes | 09/21 | |
BI 653048 | Nuclear hormone receptor | NR3C1 | BI-3047 | Yes | 11/18 | |
BI-3231 | 17β-hydroxysteroid dehydrogenases | HSD17B13 | BI-0955 | Yes | 09/23 | |
UNC0642 | Methyltransferase | EHMT2/G9a, EHMT1/GLP | Yes | 08/12 | ||
MU1742 | Kinase | CK1δ, CK1ε | MU2027 | Yes | 10/22 | |
Skepinone-L | Kinase | MAPK14 | FM-743 | Yes | 01/20 | |
BAY-7598 | Protease | MMP12 | BAY-694 | Yes | 05/18 | |
GSK778 | Bromodomains | BRD2, BRD3, BRD4, BRDT | Yes | 02/21 | ||
BAY-707 | Hydrolase | NUDT1 | BAY-604 | Yes | 05/18 | |
JNJ-65355394 | Hydrolase | OGA | JNJ-73924149 | Yes | 11/21 | |
JNJ-39758979 | GPCR | HRH4 | JNJ-39668551 | Yes | 09/22 | |
BI-1230 | Protease | HCV NS3 | BI-1675 | Yes | 03/19 | |
BAY-6096 | GPCR | ADRA2B | BAY-726 | Yes | 12/23 | |
GSK2801 | Bromodomains | BAZ2A, BAZ2B | GSK8573 | Yes | 12/14 | |
MRL-SYKi | Kinase | SYK | MRL-SYKi-NC | Yes | 05/18 | |
A-446 | Hydrolase | GLS | A-426 | Yes | 07/21 | |
ABT-546 | GPCR | EDNRA | A-545 | Yes | 05/18 | |
BI-2545 | Phosphodiesterase | ENPP2 | BI-3017 | Yes | 11/18 | |
JNJ-42226314 | Serine hydrolase | MGLL | JNJ-8034 | Yes | 09/23 | |
BAY-179 | Complex I | BAY-070 | Yes | 01/20 | ||
BAY-474 | Kinase | MET | BAY-827 | Yes | 05/18 | |
BAY-6672 | GPCR | PTGFR | BAY-403 | Yes | 11/20 | |
BI-9627 | Solute carriers | SLC9A1 | BI-0054 | Yes | 05/18 | |
TP-021 | Transcription factor | BCL6 | TP-021n | Yes | 11/18 | |
BI-8668 | Sodium channels | Epithelial sodium channel (ENaC) | BI-0337 | Yes | 11/23 | |
THPP-1 | Phosphodiesterase | PDE10A | THPP-1-NC | Yes | 06/19 | |
WM-1119 | Transferase | KAT6A, KAT6B | WM-2474 | Yes | 06/20 | |
BI-9564 | Bromodomains | BRD9, BRD7 | Yes | 04/15 | ||
CRTH2 antagonist | GPCR | PTGDR2 | CRTH2 negative control | Yes | 05/18 | |
BI 605906 | Kinase | IKBKB | BI-5026 | Yes | 06/21 | |
KISS1-305 | GPCR | KISS1R | KISS1-543 | Yes | 05/18 | |
BI-2081 | GPCR | FFAR1 | BI-0340 | Yes | 09/22 | |
BI-4394 | Protease | MMP13 | BI-4395 | Yes | 11/18 | |
BAY-7081 | Phoshodiesterase | PDE9A | BAY-7424 | Yes | 09/23 | |
WEB2086 | GPCR | PTAFR | WEB2387 | Yes | 01/24 | |
BAY-985 | Kinase | TBK1, IKBKE | BAY-440 | Yes | 01/20 | |
BI-2540 | Reverse transcriptase | HIV NNRT | BI-2439 | Yes | 11/20 | |
GSK484 | Arginine deiminases | PAD4 | GSK106 | Yes | 03/15 | |
PF-05105679 | Ion channel | TRPM8 | PF-05257137 | Yes | 05/18 | |
PFI-653 | Hydrolase | VNN1 | PFI-653-N | Yes | 09/21 | |
BAY-784 | GPCR | GNRHR | BAY-786 | Yes | 11/18 | |
BAY-549 | Kinase | ROCK1, ROCK2 | BAY-4900 | Yes | 06/19 | |
BAZ2-ICR | Bromodomains | BAZ2A, BAZ2B | Yes | 05/14 | ||
NVS-MALT1 | Protease | MALT1 | NVS-MALT1-C | Yes | 02/20 | |
BI 665915 | Lipoxygenase | ALOX5AP | BI-0153 | Yes | 05/18 | |
GSK620 | Bromodomains | BRD2, BRD3, BRD4, BRDT | Yes | 02/21 | ||
TP-472 | Bromodomains | BRD9, BRD7 | TP-472N | Yes | 06/16 | |
ABT-100 | Transferase | FNTB | A-108 | Yes | 05/18 | |
TP-050 | Ion channel | GRIN2A | TP-050n | Yes | 09/22 | |
BAY-678 | Protease | ELANE | BAY-677 | Yes | 05/18 | |
JNJ-9350 | Oxidase | SMOX | JNJ-4545 | Yes | 09/22 | |
M4K2234 | Kinase | ALK1, ALK2 | M4K2234NC | Yes | 02/22 | |
A-1211212 | Regulator protein | BCL2 | A-1210227 | Yes | 11/19 | |
BAY-069 | Amino acid transaminase | BCAT1, BCAT2 | BAY-771 | Yes | 09/20 | |
BAY-598 | Methyltransferase | SMYD2 | BAY-369 | Yes | 04/15 | |
BI-1935 | Hydrolase | EPHX2 | BI-2049 | Yes | 05/18 | |
JNJ-42396302 | Phosphodiesterase | PDE10A | JNJ-40573663 | Yes | 09/21 |
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