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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 |
---|---|---|---|---|---|---|
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 | |
BI 653048 | Nuclear hormone receptor | NR3C1 | BI-3047 | Yes | 11/18 | |
BI-3231 | 17β-hydroxysteroid dehydrogenases | HSD17B13 | BI-0955 | Yes | 09/23 | |
UCSF924 | GPCR | DRD4 | UCSF924NC | Yes | 04/19 | |
CS640 | Kinase | CAMK1 | CS640s | Yes | 01/23 | |
Skepinone-L | Kinase | MAPK14 | FM-743 | Yes | 01/20 | |
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 | |
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 | |
JQ1 | Bromodomains | BRD2, BRD3, BRD4, BRDT | (-)-JQ1 | Yes | 06/10 | |
BAY-474 | Kinase | MET | BAY-827 | Yes | 05/18 | |
BAY-6672 | GPCR | PTGFR | BAY-403 | Yes | 11/20 | |
GSK864 | Dehydrogenase | IDH1 | GSK990 | Yes | 11/15 | |
BI-9627 | Solute carriers | SLC9A1 | BI-0054 | Yes | 05/18 | |
L-Moses | Bromodomains | KAT2A, KAT2B | D-Moses | Yes | 10/17 | |
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 | ||
CRTH2 antagonist | GPCR | PTGDR2 | CRTH2 negative control | Yes | 05/18 | |
BI 605906 | Kinase | IKBKB | BI-5026 | Yes | 06/21 | |
GSK6853 | Bromodomains | BRPF1 | GSK9311 | Yes | 01/17 | |
KISS1-305 | GPCR | KISS1R | KISS1-543 | Yes | 05/18 | |
BI-2081 | GPCR | FFAR1 | BI-0340 | Yes | 09/22 | |
DDR-TRK-1 | Kinase | DDR, TRK | DDR-TRK-1N | Yes | 08/18 | |
TP-021 | Transcription factor | BCL6 | TP-021n | Yes | 11/18 | |
BI-8668 | Sodium channels | Epithelial sodium channel (ENaC) | BI-0337 | Yes | 11/23 | |
MRIA9 | Kinase | SIK1, SIK2, SIK3 | MR7 | Yes | 08/21 | |
THPP-1 | Phosphodiesterase | PDE10A | THPP-1-NC | Yes | 06/19 | |
WM-1119 | Transferase | KAT6A, KAT6B | WM-2474 | Yes | 06/20 | |
PF-05105679 | Ion channel | TRPM8 | PF-05257137 | Yes | 05/18 | |
PFI-653 | Hydrolase | VNN1 | PFI-653-N | Yes | 09/21 | |
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 | |
BI 665915 | Lipoxygenase | ALOX5AP | BI-0153 | Yes | 05/18 | |
GSK620 | Bromodomains | BRD2, BRD3, BRD4, BRDT | Yes | 02/21 | ||
ABT-100 | Transferase | FNTB | A-108 | Yes | 05/18 | |
TP-050 | Ion channel | GRIN2A | TP-050n | Yes | 09/22 | |
BAY-784 | GPCR | GNRHR | BAY-786 | Yes | 11/18 | |
BAY-549 | Kinase | ROCK1, ROCK2 | BAY-4900 | Yes | 06/19 | |
NVS-MALT1 | Protease | MALT1 | NVS-MALT1-C | Yes | 02/20 | |
BI-1935 | Hydrolase | EPHX2 | BI-2049 | Yes | 05/18 | |
JNJ-42396302 | Phosphodiesterase | PDE10A | JNJ-40573663 | Yes | 09/21 | |
BAY-678 | Protease | ELANE | BAY-677 | Yes | 05/18 | |
JNJ-9350 | Oxidase | SMOX | JNJ-4545 | Yes | 09/22 | |
MU1700 | Kinase | ALK1, ALK2 | MU1700NC | 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 | |
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 | |
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 | |
UNC1999 | Methyltransferase | EZH2 | UNC2400 | Yes | 05/13 | |
MRK-560 | Protease | Gamma secretase complex | GSI-NC | Yes | 05/18 | |
8RK64 | Regulator protein | UCHL1 | JYQ88 | Yes | 09/21 | |
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 | |
TP-030-1 | Kinase | RIPK1 | TP-030n | Yes | 09/20 | |
BAY-3153 | GPCR | CCR1 | BAY-173 | Yes | 02/21 | |
A-485 | Transferase | EP300, CREBBP | A-486 | Yes | 05/18 | |
Borussertib | Kinase | AKT1, AKT2 | RL2578 | Yes | 10/21 | |
BI 639667 | GPCR | CCR1 | BI-9307 | Yes | 11/18 | |
TP-060 | Glucosyltransferase | UGCG | TP-060n | Yes | 09/23 | |
UNC0642 | Methyltransferase | EHMT2/G9a, EHMT1/GLP | Yes | 08/12 | ||
MU1742 | Kinase | CK1δ, CK1ε | MU2027 | Yes | 10/22 | |
MRL-650 | GPCR | CNR1 | MRL-CB1-NC | Yes | 05/18 | |
PF-04457845 | Hydrolase | FAAH | PF-04875474 | Yes | 05/18 | |
JNJ-6204 | Kinase | CSNK1D/CSNK1E | JNJ-0293 | Yes | 09/22 | |
TP-024 | GPCR | GPR52 | TP-024n | Yes | 11/18 | |
BAY 1753011 | GPCR | AVPR1A, AVPR2 | BAY-2297 | Yes | 12/23 | |
MSD-CYP11B2 | Cytochrome P450 | CYP11B2 | MSD-CYP11B2 Negative control | Yes | 06/19 | |
GSK2801 | Bromodomains | BAZ2A, BAZ2B | GSK8573 | Yes | 12/14 | |
Ogerin | GPCR | GPR68 | ZINC32547799 | Yes | 06/20 | |
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 | |
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-9564 | Bromodomains | BRD9, BRD7 | Yes | 04/15 | ||
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 | |
TP-020 | Transferase | MGAT2 | TP-020n | Yes | 11/18 | |
PPTN | GPCR | P2RY14 | PPTN-NC | Yes | 06/19 | |
GSK484 | Arginine deiminases | PAD4 | GSK106 | Yes | 03/15 | |
PF-04418948 | GPCR | PTGER2 | PF-04475866 | Yes | 05/18 | |
JNJ-54119936 | Nuclear hormone receptor | RORC | JNJ-53721590 | Yes | 09/21 | |
A-079 | Ion channel | TRPA1 | A-226 | Yes | 11/18 | |
BAY 1816032 | Kinase | BUB1 | BAY-283 | Yes | 10/22 | |
BIBO3304 | GPCR | NPY1R | BIBO3457 | Yes | 01/24 | |
A-1155463 | Regulator protein | BCL2L1 | A-1107969 | Yes | 11/19 | |
BAY-390 | Ion channel | TRPA1 | BAY-9897 | Yes | 09/20 | |
ABT-724 | GPCR | DRD4 | A-769 | Yes | 05/18 | |
GSK046 | Bromodomains | BRD2, BRD3, BRD4, BRDT | Yes | 02/21 | ||
TP-472 | Bromodomains | BRD9, BRD7 | TP-472N | Yes | 06/16 | |
GNE-2256 | Kinase | IRAK4 | GNE-6689 | Yes | 11/21 | |
BAY-1797 | Ion channel | P2X4 | BAY-207 | Yes | 11/18 | |
BAZ2-ICR | Bromodomains | BAZ2A, BAZ2B | Yes | 05/14 | ||
BAY-598 | Methyltransferase | SMYD2 | BAY-369 | Yes | 04/15 | |
GSM1 | Protease | Gamma secretase complex | GSM-NC | Yes | 05/18 | |
TP-040 | Hydrolase | OGA | TP-040n | Yes | 09/21 | |
BAY-876 | Solute carriers | SLC2A1 | BAY-588 | Yes | 05/18 | |
SAFit2 | Isomerase | FKBP5 | ddSAFit2 | Yes | 09/22 | |
M4K2234 | Kinase | ALK1, ALK2 | M4K2234NC | Yes | 02/22 | |
TP-030-2 | Kinase | RIPK1 | TP-030n | Yes | 09/20 | |
BAY-299 | Bromodomains | TAF1, BRD1 | BAY-364 | No | 06/16 | |
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 | |
LP99 | Bromodomains | BRD9, BRD7 | 2S,3R-enantiomer | No | 12/14 | |
CK156 | Kinase | STK17A, DRAK1 | CKJB71 | No | 10/21 | |
A-1596586 | Ion channel | CFTR | A-1596584 | No | 06/19 | |
SGC-CDKL5_GSK3 | Kinase | CDKL5, GSK3 | SGC-CDKL5/GSK3-1N | No | 09/23 | |
(R)-ZINC-3573 | GPCR | MRGPRX2 | (S)-ZINC-3573 | No | 06/20 | |
BAY-091 | Kinase | PIP4K2A | BAY-0361 | No | 10/21 | |
I-CBP112 | Bromodomains | CREBBP, EP300 | No | 03/13 | ||
BAY-805 | USP (ubiquitin specific protease) | USP21 | BAY-728 | No | 10/22 | |
SGC707 | Methyltransferase | PRMT3 | XY1 | No | 06/14 | |
I-BRD9 | Bromodomains | BRD9 | No | 05/15 | ||
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 | |
MS023 | Methyltransferase | PRMT1, PRMT3, CARM1, PRMT6, PRMT8 | MS094 | No | 07/15 | |
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 | |
BI-3802 | 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 | |
NVS-CECR2-1 | Bromodomains | CECR2 | NVS-CECR2-C | No | 06/15 | |
MS049 | Methyltransferase | CARM1, PRMT6 | MS049N | No | 06/15 | |
T3-CLK | Kinase | CLK1, CLK2, CLK3, CLK4 | T3-CLK-N | No | 04/19 | |
SGK3-PROTAC1 | Kinase | SGK3 | cisSGK3-PROTAC1 | No | 01/24 | |
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 | |
GSK789 | Bromodomains | BRD2, BRD3, BRD4, BRDT | GSK791 | No | 02/21 | |
PFI-6 | YEATS | MLLT1, MLLT3 | PFI-6N | No | 06/20 | |
A-366 | Methyltransferase | EHMT1/GLP, EHMT2/G9a | No | 06/13 | ||
FS-694 | Kinase | MAPK14 | FM-743 | No | 01/20 | |
A-196 | Methyltransferase | SUV420H1, SUV420H2 | A-197, SGC2043 | No | 07/15 | |
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 | |
BI 99179 | Synthase | FASN | BI 99990 | No | 05/18 | |
NVS-PAK1-1 | Kinase | PAK1 | NVS-PAK1-C | No | 06/16 | |
NVS-MLLT-1 | YEATS | MLLT1, MLLT3 | NVS-iMLLT-C | No | 03/20 | |
SR-318 | Kinase | MAPK14 | SR-321 | No | 01/20 | |
UNC0638 | Methyltransferase | EHMT2/G9a, EHMT1/GLP | UNC0737 | No | 06/10 | |
NI-57 | Bromodomains | BRPF1, BRD1, BRPF3 | No | 12/14 | ||
BI-1942 | Protease | CMA1 | No | 06/21 | ||
PFI-7 | E3 ligase | GID4 | PFI-7N | No | 09/21 | |
GSK591 | Methyltransferase | PRMT5 | SGC2096 | No | 07/15 | |
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 | |
SGC-UBD1031 | UBD (ubiquitin binding domain) | SGC-UBD1031N | No | 05/24 | ||
BI-3812 | Transcription factor | BCL6 | BI-5273 | No | 11/23 | |
Homer | WD40 repeat | WDR5 | nc_WDR5 and nc_VHL | No | 07/21 | |
IOX2 (requires >>> 1 microM for cell assays) |
2OG | PHD2 | No | 02/12 | ||
SR-302 | Kinase | DDR1, DDR2, MAPK11, MAPK14 | SR-301 | No | 06/20 | |
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 | |
BTZO-1 | Cytokine | MIF | BTZO-4 | No | 05/18 | |
NR162 | Kinase | CASK | NR187 | No | 09/20 | |
TP-008 | Kinase | ACVR1B, TGFBR1 | Al11 | No | 06/19 | |
BAY-3827 | Kinase | PRKAA1, RPS6KA1 | BAY-974 | No | 01/20 | |
OF-1 | Bromodomains | BRPF1, BRD1, BRPF3 | No | 07/14 | ||
MU1210 | Kinase | CLK1, CLK2, CLK4, DYRK1A, DYRK1B, DYRK2 | MU140 | No | 05/19 | |
BAY-293 | Nucleotide exchange factor | SOS1 | BAY-294 | No | 04/19 | |
VZ185 | Bromodomain-containing protein family | BRD7, BRD9 | cisVZ185 | No | 01/24 | |
IPP/CNRS-A017 | Dehydrogenase | DHODH | IPP/CNRS-A019 | No | 10/19 | |
OICR-9429 | WD40 repeat | WDR5 | OICR-0547 | No | 05/14 | |
SGC-AAK1-1 | Kinase | AAK1, BMP2K, BIKE | SGC-AAK1-1N | 02/18 | ||
BAY-850 | Bromodomains | ATAD2 | BAY-460 | 01/17 | ||
TP-238 | Bromodomains | CECR2, BPTF | TP-422 | 09/18 | ||
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 | ||
A-395 | WD40 repeat | EED | A-395N | 07/16 | ||
MRK-740 | Methyltransferase | PRDM9 | MRK-740-NC | 06/18 | ||
SGC-SMARCA-BRDVIII | Bromodomains | PB1(5), SMARCA2/4 | SGC-BRDVIII-NC | 12/20 | ||
BAY-6035 | Methyltransferase | SMYD3 | BAY-444 | 06/17 | ||
UNC6934 | Methyl Lysine Binder | NSD2-PWWP1 | UNC7145 | 06/19 | ||
TP-064 | Methyltransferase | CARM1 | TP-064N | 06/16 | ||
SGC-GAK-1 | Kinase | GAK | SGC-GAK-1N | 02/18 | ||
MSC1186 | Kinase | SRPK | MSC5360 | 01/23 | ||
FM-381 | Kinase | JAK3 | FM-479 | 02/17 | ||
BI01383298 | Solute carriers | SLC13A5 | BI01372674 | 01/18 | ||
GSK8814 | Bromodomains | ATAD2, ATAD2B | GSK8815 | 01/17 | ||
VinSpinIn | Spindlin domains | Spin1 | VinSpinIC | 09/18 | ||
SGC-CAF382-1 | Kinase | CDKL5 | SGC-CAF268-1N | 09/23 | ||
TH-257 | Kinase | LIMK1, LIMK2 | TH-263 | 07/17 | ||
LLY-283 | Methyltransferase | PRMT5 | LLY-284 | 07/16 | ||
BI-9321 | Methyl Lysine Binder | NSD3 | BI-9466 | 07/18 | ||
JA397 | Kinase | CDK14-18 | JA314 | 07/23 | ||
PFI-5 | Methyltransferase | SMYD2 | PFI-5N | 07/17 | ||
SGC6870 | Methyltransferase | PRMT6 | SGC6870N | 06/19 | ||
SGC3027 | Methyltransferase | PRMT7 | SGC3027N | 03/18 | ||
JP3000 | RXRA, RXRB, RXRG | JP3001 | 10/23 | |||
SGC-CK2-2 | Kinase | CK2/CSNK2 | SGK-CK2-2N | 05/23 | ||
GSK4027 | Bromodomains | KAT2A, KAT2B | GSK4028 | 06/17 | ||
JA310 | Kinase | MST3, MST4 | JA262 | 11/23 |
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