-
mitotic progression inhibitor
3-Hydroxycapric acid is an inhibitor for mitotic progression. -
Bcl-2 inhibitor
ABT-263 also called Navitoclax is a potent and orally bioavailable Bcl-2 family inhibitor (Ki's of <1 nmol/L for Bcl-2, Bcl-xL, and Bcl-w). it maintains a high affinity for Bcl-xL, Bcl-2, and Bcl-w, (Ki ≤1 nmol/L), but binds more weakly to Mcl-1 and A1.- Yibo Wen, .et al. , Ren Fail, 2023, Dec;45(1):2194440 PMID: 37154092
- Rindert Missiaen, .et al. , Cell Metab, 2022, Aug 2;34(8):1151-1167 PMID: 35839757
- Ashlyn Parkhurst, .et al. , Cell Death Dis, 2022, Apr 28;13(4):410 PMID: 35484114
- Suzuki, Keiji, .et al. , Mutat Res Genet Toxicol Environ Mutagen, 2022, 876-877. 503448
- Rotem Ben-Hamo, .et al. , Nat Commun, 2020, 11: 3296
- Hua Xu, .et al. , Cancers (Basel), 2020, Apr; 12(4): 831 PMID: 32235588
- Hiroki Akiyama, .et al. , Cancers, 2020, 12 (2) PMID: 32050632
- Stephanie Ketterer, .et al. , Nat Commun, 2020, Oct 12;11(1):5133 PMID: 33046706
- Makoto Koyama, .et al. , Int J Oncol, 2020, Sep 2 PMID: 32901840
- Min Li, .et al. , Nat Commun, 2020, 11: 4051 PMID: 32792548
- Hamzehlou S, .et al. , Eur J Pharmacol, 2019, Nov 15;863:172705 PMID: 31574259
- Momeny M, .et al. , Cell Oncol (Dordr), 2019, Apr 25 PMID: 31025257
- Anderson R, .et al. , EMBO J, 2019, Feb 8. pii: e100492 PMID: 30737259
- Shinya Ishida, .et al. , Oncotarget, 2018, Jun 1; 9(42): 26834-26851 PMID: 29928488
- Rhys Anderson, .et al. , bioRxiv, 2018, 2018
- Ryuta Mikawa, .et al. , Aging Cell, 2018, Oct; 17(5): e12827 PMID: 30058137
- Joo Sang Lee, .et al. , Nat Commun, 2018, 9: 2546 PMID: 29959327
- Toshiyuki Sumi, .et al. , Int J Oncol, 2018, Jul; 53(1): 33-46 PMID: 29658609
- Wei TW, .et al. , Cancer Res, 2017, Jan 15;77(2):494-508 PMID: 28069801
- Yusuke Takagi, .et al. , Cancer Sci, 2016, Sep; 107(9): 1270-1280 PMID: 27348272
- Matsumoto M, .et al. , Biochem Biophys Res Commun, 2016, Apr 29;473(2):490-6 PMID: 26996126
-
VEGFR inhibitor
Regorafenib (BAY 73-4506) is a multikinase inhibitor with IC50 of 17, 40 and 69 nM c-KIT, VEGFR2, B-Raf. Regorafenib (BAY 73-4506) is an orally bioavailable multikinase inhibitor targeting both the tumor and its vasculature.- Hasan U, .et al. , Research Square, 2023, 13 Apr
- Paula Sagmeister, .et al. , J Hepatocell Carcinoma, 2022, Jul 9;9:595-607 PMID: 35845819
- Majid Momeny, .et al. , Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
- Jindal A, .et al. , J Transl Sci, 2020, 7: 1-10
- Makoto Koyama, .et al. , Int J Oncol, 2020, Sep 2 PMID: 32901840
- Mariko Fujisawa, .et al. , Anticancer Res, 2020, 40: 4445-4455 PMID: 32727774
- Majid Momeny, .et al. , Eur J Pharmacol, 2020, 882:173298
- Sunil Kumar Yadava, .et al. , Colloids Surf B Biointerfaces, 2020, Mar 2;190:110927 PMID: 32169777
- Takeshi Uenaka, .et al. , Hum Mol Genet, 2018, Nov 15; 27(22): 3974-3985 PMID: 30137437
- Yi Xu, .et al. , Free Radic Biol Med, 2016, Jul; 96: 67-77 PMID: 27101738
-
Bcl-2 Inhibitor
ABT-737 is a pan-Bcl-2 inhibitor. IC50 values ranged from 192 nM (the pre-B cell line Hal-01) to <10 μM (Nalm-6, K562 and HL-60).- Jung Mo Lee, .et al. , Yonsei Med J, 2022, Jan;63(1):16-25 PMID: 34913280
- AidaVarela-Moreira, .et al. , Int J Pharm, 2022, Apr 25;618:121638 PMID: 35257802
- Daniel F R Boehmer, .et al. , Sci Immunol, 2021, Jul 16;6(61) PMID: 34272227
- Shivani Arora, .et al. , Med, 2021, 2,1-13
- Ying Ji, .et al. , Nat Commun, 2020, Aug 25;11(1):4249 PMID: 32843618
- Birgit Ritschka, .et al. , Genes Dev, 2020, Apr 1;34(7-8):489-494 PMID: 32139422
- Hiroki Akiyama, .et al. , Cancers, 2020, 12 (2) PMID: 32050632
- Hsu CC, .et al. , Arch Oral Biol, 2020, Mar;111:104653 PMID: 31935534
- Gupta VK, .et al. , Apoptosis, 2020, Feb;25(1-2):135-150 PMID: 31867678
- Meikle V, .et al. , Antimicrob Agents Chemother, 2018, Nov 12. pii: AAC.01846-18 PMID: 30420480
- Chauhan D, .et al. , Cell Rep, 2018, Nov 27;25(9):2354-2368.e5 PMID: 30485805
- Jose Mario Gonzalez-Meljem, .et al. , Nat Commun, 2017, 8: 1819 PMID: 29180744
- Zhang C, .et al. , J Biol Chem, 2017, Sep 8;292(36):15105-15120 PMID: 28673964
- Eun Young Kim, .et al. , Neoplasia, 2017, Apr; 19(4): 354-363 PMID: 28319809
- Masayoshi Toge, .et al. , Int J Oncol., 2015, Apr;46(4):1844-8 PMID: 25647738
-
Bcl-2 Inhibitor
Bcl-2 homology domain-3 (BH3) mimetic,antagonize all antiapoptotic Bcl-2 family proteins (average IC50, 3 umol/L), including Mcl-1 (IC50, 2.9 umol/L) and Bfl-1 (IC50, 5 umol/L).- Ashlyn Parkhurst, .et al. , Cell Death Dis, 2022, Apr 28;13(4):410 PMID: 35484114
- Silva S, .et al. , Sci Rep, 2019, Nov 27;9(1):17703 PMID: 31776405
- Chi-Hung R. Or, .et al. , Int J Mol Sci, 2016, Jan; 18(1): 44 PMID: 28035994
- P Geserick, .et al. , Cell Death Dis., 2014, 5(9): e1412 PMID: 25210795
-
Aurora inhibitor
Danusertib (PHA-739358) is an Aurora kinase inhibitor for Aurora A/B/C with IC50 of 13 nM/79 nM/61 nM in cell-free assays, modestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc. Phase 2- Vijaya Bharti, .et al. , Cell Rep, 2022, Dec 20;41(12):111826 PMID: 36543138
-
TNF-alpha inhibitor
Pomalidomide is a derivative of thalidomide and acts as an immunomodulator. -
E3 ubiquitin ligase inhibitor
Thalidomide can directly inhibit angiogenesis induced by bFGF or VEGF in vivo. -
Caspase-1/4 inhibitor
VX-765 is a novel Caspase-1 inhibitor,which is an enzyme that controls the generation of two cytokines, IL-1b and IL-18.- Joseph Flores, .et al. , Cell Death Dis, 2022, Oct 11;13(10):864 PMID: 36220815
- Arjun Thapa, .et al. , Leukemia, 2021, 23 February
- Prenitha Mercy Ignatius Arokia Doss, .et al. , Cell Rep, 2021, Mar 9;34(10):108833 PMID: 33691111
- Joseph Flores, .et al. , Nat Commun, 2020, Sep 11;11(1):4571 PMID: 32917871
- Joseph Flores, .et al. , Nat Commun, 2018, 9: 3916 PMID: 30254377
- Mohamed F. Ali, .et al. , Front Immunol, 2017, 8: 1504 PMID: 29170665
- García-Fernández A, .et al. , J Control Release, 2017, Feb 28;248:60-70 PMID: 28069553
- Jiujiu Yu, .et al. , Proc Natl Acad Sci U S A, 2014, 111(43): 15514-15519 PMID: 25313054
-
Survivin Inhibitor
YM155 is a novel small molecule survivin suppressant with an IC50 of 0.54 nM for the inhibition of survivin promoter activity.- Ali Nasrollahzadeh, .et al. , Biochim Biophys Acta Mol Cell Res, 2021, Jun 26;1868(10):119087 PMID: 34182011
- Chia-Hui Huang, .et al. , Toxicol Appl Pharmacol, 2020, Apr 17;397:115013 PMID: 32305283
- Turner TH, .et al. , Sci Rep, 2020, Jan 30;10(1):1493 PMID: 32001757
- Chiou JT, .et al. , Toxicol Appl Pharmacol, 2019, Dec 16;387:114857 PMID: 31837377
- Hamzehlou S, .et al. , Eur J Pharmacol, 2019, Nov 15;863:172705 PMID: 31574259
- Momeny M, .et al. , Cell Oncol (Dordr), 2019, Apr 25 PMID: 31025257
- Yamamoto M, .et al. , Anticancer Res, 2019, Feb;39(2):609-617 PMID: 30711936
- Vázquez-Mellado MJ, .et al. , Oncol Rep, 2018, Nov 27 PMID: 30483799
- MASAHIRO YAMAMOTO, .et al. , Anticancer Res, 2018, Dec 38 (12) 6699-6706 PMID: 30504379
- Ahn MR, .et al. , Drug Discov Ther, 2017, 11(6):300-306 PMID: 29332887
- MASAYA MINODA, .et al. , Int J Oncol, 2015, Sep; 47(3): 891-899 PMID: 26166250
-
IAP inhibitor
AT-406 is an orally bioavailable inhibitor of IAP family of proteins with potential apoptotic inducing and antineoplastic activity. AT-406 selectively inhibits the biological activity of IAP proteins, including X chromosome-linked IAP (XIAP), the cellular IAPs 1 (c-IAP1) and 2 (c-IAP2) and melanoma inhibitor of apoptosis protein (ML-IAP).- Yoshikawa M, .et al. , J Med Chem, 2018, Mar 22;61(6):2384-2409 PMID: 29485864
- Tsuyoshi Ishii, .et al. , Sci Rep, 2017, 7: 13000 PMID: 29026104
-
MDMX Inhibitor
NSC207895 is a cell-permeable benzofuroxan compound that downregulates the p53 negative regulator MDMX protein level in MCF-7, LNCaP, and A549 cells (1 to 10 µM for 16 to 24 h) by suppressesing MDMX promoter transcription activity (IC50 = 2.5 µM in HT1080 cells), leading to enhanced p53 stabilization and activation.
-
multi-kinase inhibitor
Lestaurtinib (CEP-701;KT-5555) is a multi-kinase inhibitor with potent activity against the Trk family of receptor tyrosine kinases. Lestaurtinib inhibits JAK2, FLT3 and TrkA with IC50s of 0.9, 3 and less than 25 nM, respectively. -
MDM2 inhibitor
Nutlin 3a is a potent inhibitor of MDM2 (mouse double minute 2) binding to p53 that induces the expression of p53 regulated genes, and shows potent antiproliferative activity in cells expressing functional p53.- Sho Watanabe, .et al. , J Crohns Colitis, 2021, Feb 17 PMID: 33596306
- Shun Zhang, .et al. , BPB Reports, 2019, 2, 130-133
- Momoko Ishimine, .et al. , Dis Markers, 2018, 2018: 5280736 PMID: 29651325
-
VEGFR1/2/3/PDGFRβ/Kit/RET/Raf-1 inhibitor
Regorafenib Hydrochloride is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively. -
RIPK1 inhibitor
Necrostatin-1 is an ATP-competitive, allosteric inhibitor of receptor-interacting protein kinase 1 (RIPK1) (EC50 = 182 nM). -
N-SMase inhibitor
GW4869 is a cell permeable, selective inhibitor of N-SMase (neutral sphingomyelinase).
- Guohao Wang, .et al. , Nat Commun, 2021, Sep 30;12(1):5733 PMID: 34593794
-
Bcl-2 inhibitor
Gambogic acid is a natural product isolated from the Garcinia hanburyi tree. Gambogic Acid activates caspases with EC50 of 0.78-1.64 μM and competitively inhibits Bcl-XL, Bcl-2, Bcl-W, Bcl-B, Bfl-1 and Mcl-1 with IC50 of 1.47, 1.21, 2.02, 0.66, 1.06 and 0.79 μM, respectively. -
TNF inhibitor
Etanercept, a dimeric fusion protein that binds TNF, acts as a TNF inhibitor. -
miR-544 inhibitor
SID 3712249 (MiR-544 Inhibitor 1) is an inhibitor of the biogenesis of microRNA-544 (miR-544). -
Pan Caspase Inhibitor
Z-VAD-FMK is a cell-permeable, irreversible pan-caspase inhibitor. Inhibits caspase processing and apoptosis induction in tumor cells in vitro (IC50 = 0.0015 - 5.8 mM). Active in vivo.- Chantal-Kristin Wenzel, .et al. , Toxicol In Vitro, 2023, Sep;91:105625 PMID: 37268255
- Joshua H Choe, .et al. , Cancer Discov, 2023, May 4;13(5):1250-1273 PMID: 37067901
- Yu-Chih Hsu, .et al. , Int J Med Sci, 2023, 20(4): 444-454 PMID: 37057216
- Debin Qi, .et al. , Cell Cycle, 2023, Apr;22(7):818-828 PMID: 36482709
- Ming-Chun Hung, .et al. , Cell Biosci, 2022, 12: 122 PMID: 35918763
- Kaori Kanemaru, .et al. , Nat Commun, 2022, May 9;13(1):2347 PMID: 35534464
- Chie Ishikawa, .et al. , Invest New Drugs, 2022, Aug;40(4):718-727 PMID: 35477814
- Aida Falgas, .et al. , Biomed Pharmacother, 2022, Jun;150:112940 PMID: 35421785
- Sumire Suzuki, .et al. , Oncol Rep, 2022, Feb;47(2):40 PMID: 34958115
- Lina Y Abou Zeid, .et al. , Cell Stress Chaperones, 2022, Jan;27(1):11-25 PMID: 34719748
- Simon Boudreault, .et al. , Viruses, 2022, Dec 3;14(12):2710 PMID: 36560714
- Kosar Jabbari, .et al. , Cancers (Basel), 2021, Sep 8;13(18):4521 PMID: 34572749
- Xiaoyue Deng, .et al. , Invest Ophthalmol Vis Sci, 2021, May 3;62(6):1 PMID: 33938913
- Liqun Zhao, .et al. , Apoptosis, 2021, Apr 27 PMID: 33905036
- Sofia Giacosa, .et al. , Cancers (Basel), 2021, Feb 2;13(3):576 PMID: 33540838
- Hannes Schmid, .et al. , Haematologica, 2021, Jan 14 PMID: 33440919
- Hua Xu, .et al. , Cancers (Basel), 2020, Apr; 12(4): 831 PMID: 32235588
- El-Ashmawy NE, .et al. , Pathol Oncol Res, 2020, Jan 4 PMID: 31902118
- Schneider D, .et al. , Clin Epigenetics, 2019, Jul 2;11(1):98 PMID: 31266541
- Fujiki K, .et al. , Cell Death Differ, 2019, Feb 25 PMID: 30804470
- T Yamamoto, .et al. , Cell Microbiol, 2019, 2019 PMID: 30702185
- Maeda N, .et al. , J Biol Chem, 2019, Nov 13. pii: jbc.RA119.010379 PMID: 31723031
- Miyazawa S, .et al. , Breast Cancer, 2019, Oct 17 PMID: 31625014
- Yeh HT, .et al. , Eur J Pharmacol, 2019, Sep 10;863:172658 PMID: 31518562
- D. Bosc, .et al. , Sci Rep, 2018, 8: 11653 PMID: 30076329
- Tsukamoto H, .et al. , J Biol Chem, 2018, Jun 29;293(26):10186-10201 PMID: 29760187
- Hiroshi Kuribayashi, .et al. , Cell Death Dis, 2018, Sep; 9(9): 891 PMID: 30166529
- Matsuo J, .et al. , Can J Microbiol, 2018, Oct 18:1-9 PMID: 30336068
- Orly Ravid, .et al. , Front Cell Neurosci, 2018, 12: 359 PMID: 30459557
- Im E, .et al. , Life Sci, 2018, Sep 15;209:259-266 PMID: 30107166
- Szalai P, .et al. , Cell Calcium, 2018, Dec;76:48-61 PMID: 30261424
- Im E, .et al. , Life Sci, 2018, Jan 1;192:286-292 PMID: 29128513
- Iriyama N, .et al. , Leuk Lymphoma, 2018, Jun;59(6):1439-1450 PMID: 28918692
- Birte Plitzko, .et al. , J Biol Chem, 2017, Dec 22; 292(51): 21102-21116 PMID: 29074620
- Akashi E, .et al. , Oncol Rep, 2017, Jul;38(1):506-514 PMID: 28586026
-
PKD inhibitor
CID 2011756 is a protein kinase D (PKD) inhibitor (IC50 values are 0.6, 0.7 and 3.2 μM for PKD2, PKD3 and PKD1 respectively). -
PKD inhibitor
kb NB 142-70 is a selective protein kinase D (PKD) inhibitor (IC50 values are 28.3, 58.7 and 53.2 nM for PKD1, 2 and 3 respectively). -
p53 inhibitor
inhibits p53 binding to mitochondria by reducing its affinity for antiapoptotic proteins Bcl-2 and Bcl-XL. -
p53 Inhibitor
Pifithrin-beta is a small molecule inhibitor of p53.- J Priyanga, .et al. , Chem Biol Interact, 2020, Nov 1;331:109250 PMID: 32956706
-
p53 inhibitor
Pifithrin-a is a reversible inhibitor of p53-mediated apoptosis and p53-dependent gene transcription such as cyclin G, p21/waf1, and mdm2 expression. -
Bcl-2 inhibitor
ABT-199 is a so-called BH3-mimetic drug, which is designed to block the function of the protein Bcl 2.- Dilay Karademir, .et al. , Med Oncol, 2023, Jul 11;40(8):234 PMID: 37432531
- Ashlyn Parkhurst, .et al. , Cell Death Dis, 2022, Apr 28;13(4):410 PMID: 35484114
- Anna L Koessinger, .et al. , Cell Death Differ, 2022, Apr 26 PMID: 35473984
- Florian J Bock, .et al. , Nat Commun, 2021, Nov 12;12(1):6572 PMID: 34772930
- Chauhan D, .et al. , Cell Rep, 2018, Nov 27;25(9):2354-2368.e5 PMID: 30485805
- Martin Grundy, .et al. , PLoS One, 2018, 13(1): e0190682 PMID: 29298347
- Joanne Dai, .et al. , J Immunol, 2018, 200 (5) 1727-1736 PMID: 29358277
-
myeloperoxidase inhibitor
PF-06282999 is a potent and selective myeloperoxidase inhibitor which is potential useful for the treatment of cardiovascular diseases. -
Caspase-6 inhibitor
Z-VEID-FMK is the specific recognition sequence for caspase-6/Mch2. Z-VEID-FMK is a synthetic peptide that irreversibly inhibits activity of VEID-dependent caspases (e.g., caspase-6). The inhibitor is designed as a methyl ester to facilitate cell permeability. -
RIP1 inhibitor
GSK481 is a novel benzoxazepinone (BOAz) series of RIP1 inhibitors. Receptor Interacting Protein Kinase 1 (RIP1) has been implicated as a key contributor to inflammation through the regulation of programmed necrosis. Inhibition of this kinase has been shown to hinder cell necrotic death, thereby establishing RIP1 as a viable target for the potential treatment of multiple inflammatory diseases. -
Caspase-2 inhibitor
Z-VDVAD-FMK is a cell-permeable, irreversible inhibitor of caspase-2. Caspase inhibitors play an important role in investigating biological processes. -
eIF2α dephosphorylation inhibitor
Salubrinal is a cell-permeable, selective inhibitor of cellular phosphatase complexes that dephosphorylate eukaryotic translation initiation factor 2 subunit α (eIF2α). Protects cells from endoplasmic reticulum stress-induced apoptosis (EC50 ~ 15 μM).- Gregory R. Kardos, .et al. , Front Oncol, 2020, 10: 834 PMID: 32637352
-
Caspase-3 inhibitor
Z-DQMD-FMK is a synthetic peptide that irreversibly inhibits the activity of Caspase-3.- Jason Segura, .et al. , PLoS One, 2023, Feb 13;18(2):e0281087 PMID: 36780482
-
NF-κB inhibitor
QNZ inhibits the activation of the transcription factor NF-κB and has been used to investigate NF-κB signaling. -
PERK inhibitor
GSK2606414 is an orally available, potent, and selective PERK inhibitor with IC50 of 0.4 nM.- Linhao Xu, .et al. , Neural Plasticity, 2021, 23 Aug
- Takashi Shimizu, .et al. , Sci Signal, 2021, Jan 26;14(667):eabb3616 PMID: 33500333
-
caspase 8 inhibitor
Z-IETD-FMK is a specific inhibitor of caspase 8.- Jason Segura, .et al. , PLoS One, 2023, Feb 13;18(2):e0281087 PMID: 36780482
- Liqun Zhao, .et al. , Apoptosis, 2021, Apr 27 PMID: 33905036
-
Bcl-2 inhibitor
Sabutoclax(BI-97C1) is a pan-Bcl-2 inhibitor, including Bcl-xL, Bcl-2, Mcl-1 and Bfl-1 with IC50 of 0.31 μM, 0.32 μM, 0.20 μM and 0.62 μM, respectively.- Christopher D. Graham, .et al. , Oncotarget, 2017, Jan 31; 8(5): 8670-8678 PMID: 28055968