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