PROTACs, molecular glues, ubiquitin systems, chaperones and proteostasis.
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Other Research Tools (75) · Additional reagents, building blocks and specialized research tools.
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CAS 1949837-12-0
ARV-771 is a VHL-recruiting BET protein degrader for prostate cancer and targeted protein degradation research. The primary study reports pan-BET degradation, downstream c-MYC suppression and activity in prostate cancer models.
CAS 882697-00-9
Anle138b is an aggregation-modulating research compound studied in α-synucleinopathies. Published mouse data connect reduced oligomer burden with neuronal and motor outcomes.
CAS 1190948-58-3
Diptoindonesin G is an HSP90 modulator for chaperone biology and endocrine-resistant breast-cancer research.
CAS 7497-07-6
NSC-405020 is a novel small molecule inhibitor of MT1-MMP that specifically targets PEX domain rather than the catalytic domain of MT1-MMP with IC50 >100 μM and does not inhibit the catalytic activity of MT1-MMP or MMP-2. NSC-405020 directly interacts with…
CAS 2645-32-1
PR-619 is a broad-range DUB inhibitor with EC50 of 3.93, 4.9, 6.86, 7.2, and 8.61 μM for USP4, USP8, USP7, USP2, and USP5, respectively.
CAS 1346574-57-9
GSK126 is a potent, highly selective inhibitor of EZH2 methyltransferase with an IC50 of 9.9 nM.
CAS 432001-69-9
Skp2 Inhibitor C1(SKPin C1) is a specific small molecule inhibitor of Skp2-mediated p27 degradation, selectively inhibited Skp2-mediated p27 degradation by reducing p27 binding through key compound-receptor contacts.IC50 value: Target: Skp2 inhibitor; p27…
CAS 935888-69-0
Oprozomib (ONX 0912; PR047) is an orally bioavailable inhibitor for CT-L activity of 20S proteasome β5/LMP7 with IC50 of 36 nM/82 nM.The anti-MM activity of Oprozomib is associated with activation of caspase-8, caspase-9, caspase-3, and PARP, as well as…
CAS 1572414-83-5
ML-323 is a reversible, potent USP1-UAF1 inhibitor with IC50 of 76 nM in a Ub-Rho assay. The measured inhibition constants of ML-323 for the free enzyme (Ki) is 68 nM.
CAS 603139-19-1
Odanacatib (MK-0822) is a potent and selective inhibitor of cathepsin K, with an IC50 of 0.2 nM for human cathepsin K.
D927 is a molecular glue and promotes glucose uptake in the absence of insulin. D927 also increases the affinity of RAS binding to PI3Kα by ~500-fold. In vivo, D927 mimicks the effects of insulin and rapidly lowers blood glucose concentrations.
CAS 1418013-75-8
NMS-873 is a potent, selective allosteric VCP/p97 inhibitor with IC50 value of 30 nM.
CAS 418805-02-4
PYR-41 is a specific and cell permeable inhibitor of ubiquitin-activating enzyme E1 with an IC50 of < 10 μM, with no or little activity at E2.
CAS 908115-27-5
SNX-5422 (PF-04929113), a prodrug of SNX-2112, is an orally active Hsp90 inhibitor, with a Kd of 41 nM, and also induces Her-2 degradation, with an IC50 of 37 nM.
CAS 202590-98-5
Birabresib (OTX-015) is a potent bromodomain (BRD2/3/4) inhibitor with IC50s ranging from 92 to 112 nM.
CAS 847499-27-8
Delanzomib(CEP-18770) is a novel orally-active inhibitor of the chymotrypsin-like activity of the proteasome that down-modulates the nuclear factor-kappaB (NF-kappaB) activity.
CAS 1164470-53-4
Sal003 is a potent cell-permeable analog of the eIF2α phosphatase inhibitor Salubrinal with enhanced aqueous solubility.IC50 value:Target: eIF2α phosphatase inhibitorSal003 has been shown to prevent dephosphorylation of eIF-2α which has been shown to regulate…
CAS 912999-49-6
AT13387 is a selective potent Hsp90 inhibitor with IC50 of 18 nM in A375 cells, displays a long duration of anti-tumor activity. in vitro: AT13387 is a synthetic, orally bioavailable, small-molecule inhibitor of heat shock protein 90 (Hsp90) with potential…
CAS 1609402-14-3
HA15 is a molecule that targets specifically BiP/GRP78/HSPA5target: BiP, GRP78, HSPA5 [1]In vitro: HA15 induces ER stress leading to cancer cell death. kills cancer cells by targeting BiP to increase ER stress, leading to melanoma cell death by concomitant…
CAS 1260907-17-2
GSK 525762A is a BET bromodomain inhibitor with IC50 of 32.5-42.5 nM.
CAS 1268524-70-4
(+)-JQ-1 is a BET bromodomain inhibitor, with IC50s of 77 and 33 nM for the first and second bromodomain (BRD4(1/2)).
CAS 1268524-71-5
(-)-JQ-1 is the stereoisomer of (+)-JQ1. (+)-JQ1 potently decreases expression of both BRD4 target genes, whereas (−)-JQ1 has no effect.
CAS 354813-19-7
Balicatib(AAE-581) is a potent and selective inhibitor of cathepsin K; 10-100 fold more potent in cell-based enzyme occupancy assays than against cathepsin B, L, and S.
CAS 179324-69-7
Bortezomib (PS-341) is a potent 20S proteasome inhibitor with a Ki of 0.6 nM.
CAS 142880-36-2
Ilomastat (Galardin; GM6001) is a broad spectrum matrix metalloprotease (MMP) inhibitor, with Ki of 0.4 nM, 0.5 nM, 27 nM, 3.7 nM, 0.1 nM, 0.2 nM, 3.6 nM, 13.4 nM, 0.36 nM for MMP-1/2/3/7/8/9/12/14/26, respectively.
CAS 191732-72-6
Lenalidomide is a potent inhibitor of TNF-α used as a immunomodulatory drug. It has also been shown to have anti-angiogenic properties.
CAS 668467-91-2
LDN-57444 is a reversible, competitive and site-directed inhibitor of ubiquitin C-terminal hydrolase L1 (UCH-L1), with an IC50 of 0.88 μM and a Ki of 0.40 μM; LDN-57444 also suppresses UCH-L3 activity, with an IC50 of 25 μM.
CAS 1337531-36-8
GSK2606414 is a cell-permeable and orally available PERK inhibitor with an IC50 of 0.4 nM.
CAS 1216665-49-4
APY29 is an allosteric modulator of IRE1α which inhibits IRE1α autophosphorylation with IC50 of 280 nM and activates IRE1α RNase activity.
CAS 1239908-20-3
Ixazomib citrate (MLN9708) is a reversible inhibitor of the chymotrypsin-like proteolytic β5 site of the 20S proteasome with an IC50 of 3.4 nM and a Ki of 0.93 nM.
CAS 1134156-31-2
VER-155008 is an inhibitor of Hsp70, with IC50s of 0.5 μM, 2.6 μM, and 2.6 μM for Hsp70, Hsc70 and Grp7, respectively, and with a Kd of 0.3 μM for Hsp70.
CAS 1337532-29-2
GSK2656157 is a selective and ATP-competitive inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK) with an IC50 of 0.9 nM.
CAS 405060-95-9
Salubrinal is a cell-permeable and selective inhibitor of eIF2α dephosphorylation.
CAS 934343-74-5
NVP-HSP990 is a potent and selective Hsp90 inhibitor, with IC50 values of 0.6, 0.8, and 8.5 nM for Hsp90α, Hsp90β, and Grp94, respectively.
CAS 1624602-30-7
VR23 is a small molecule that potently inhibited the activities of trypsin-like proteasomes (IC50 = 1 nM), chymotrypsin-like proteasomes (IC50 = 50-100 nM), and caspase-like proteasomes (IC50 = 3 μM).
CAS 1589527-65-0
KIRA6 allosterically inhibits IRE1α RNase kinase activity with an IC50 of 0.6 µM.
CAS 34157-83-0
Tripterin (Celastrol) is a proteasome inhibitor which potently and preferentially inhibits the chymotrypsin-like activity of a purified 20S proteasome with IC50 of 2.5 μM.
CAS 292605-14-2
SB-3CT is a potent and competitive inhibitor of matrix metalloproteinase (MMP-2) and MMP-9.
CAS 1300031-49-5
I-BET151 is a BET bromodomain inhibitor which inhibits BRD4, BRD2, and BRD3 with pIC50 of 6.1, 6.3, and 6.6, respectively.
CAS 519055-62-0
Tasisulam is a small molecule antitumor agent that inhibits mitotic progression and induces vascular normalization. Tasisulam induces apoptosis via the intrinsic pathway[1].
CAS 1799711-21-9
dBET1 is a potent BRD4 protein degrader based on PROTAC technology with an EC50 of 430 nM.
CAS 201677-61-4
Sivelestat(ONO5046; LY544349; EI546) is a competitive inhibitor of human neutrophil elastase(IC50 = 44 nM; Ki=200 nM); also inhibited leukocyte elastase obtained from rabbit, rat, hamster and mouse.ONO-5046 did not inhibit trypsin, thrombin, plasmin, plasma…
CAS 1401223-22-0
PI-1840 is a potent and selective inhibitor for chymotrypsin-like (CT-L) (IC50 value = 27 ± 0.14 nM) over trypsin-like and peptidylglutamyl peptide hydrolyzing (IC50 values >100 μM) activities of the proteasome.
CAS 187034-31-7
TAPI-2 is a broad-spectrum inhibitor of matrix metalloprotease (MMP), tumour necrosis factorα-converting enzyme (TACE) and a disintegrin and metalloproteinase (ADAM), with an IC50 of 20±10 μM for MMP.
CAS 747412-49-3
Luminespib (NVP-AUY922) is a potent HSP90 inhibitor with IC50s of 7.8 and 21 nM for HSP90α and HSP90β, respectively.
