>98%,Standard References

A novel potent, selective, orally available PI3Kδ inhibitor with IC50 of 31 nM.

A potent, specific, orally available, ATP‑competitive inhibitor of Chk1 and Chk2 with Ki of 2.2 nM and 0.07 nM, respectively.

ABC294640 is an orally available, aryladamantane compound and selective inhibitor of sphingosine kinase-2 (SK2) with potential antineoplastic activity.

ABT-263 (Navitoclax) is a potent inhibitor of Bcl-xL, Bcl-2 and Bcl-w with Ki of ≤ 0.5 nM, ≤1 nM and ≤ 1 nM, respectively.

Acalabrutinib (ACP-196) is a second-generation, selective, irreversible inhibitor of BTK.

Acalisib (GS-9820) is a potent and selective inhibitor of PI3Kδ with IC50 value of 12.7 nM.

AG-120 is a first-in-class, orally available, selective, potent inhibitor of the mutated IDH1 protein.

AG-221 is an orally available, selective, potent inhibitor of the mutated IDH2 protein.

AG-490 (Tyrphostin B42) is an inhibitor of EGFR, ErbB2 and JAK2 with IC50 of 0.1 μM, 13.5 μM, and ~10 μM, respectively.

AG-881 is a potent and selective orally available inhibitor of mutated forms of both isocitrate dehydrogenase type 1 (IDH1) in the cytoplasm and type 2 (IDH2).

AMG 900 is a potent and highly selective pan-Aurora kinases inhibitor for Aurora A/B/C with IC50 of 5 nM/4 nM /1 nM; >10-fold selective for Aurora kinases than p38α, Tyk2, JNK2, Met and Tie2.

An inhibitor of LPS-induced TNFαrelease.Pomalidomide is thalidomide derivative that displays inhibition of LPS-induced TNFα release. Shows immunomodulator and anticancer effects.

AP24534 is a novel, potent multi-target inhibitor of Abl, PDGFRα, VEGFR2, FGFR1 and Src with IC50 of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM and 5.4 nM, respectively.

Apilimod(STA 5326) is a potent IL-12/IL-23 inhibitor, IL-12 production in cultures of IFN-r/LPS–stimulated human PBMCs is strongly inhibited by STA-5326 with an IC50 of 10 nM.

APTO-253 is a novel small molecule with potent anti-tumor activity in cancer cells via induction of the gene that expresses the Krüppel-like factor 4 (KLF4) master transcription factor, leading to cell cycle inhibition and programmed cell death.

ARQ 092 is an oral activie, potent and selective AKT inhibitor with IC50 values: 5.0 nM (AKT1); 4.5 nM (AKT2); 16 nM (AKT3).

ARQ-531 is a potent, reversible, orally available inhibitor of both wild type and C481S-mutant BTK kinase with IC50 of 0.85 and 0.39 nM,

ASP3026 is a novel and selective inhibitor for ALK with IC50 of 3.5 nM.

AT-101 is a BH3 mimetic known to be a potent inhibitor of antiapoptotic Bcl-2 family members.

AT7519 is a multi-CDK inhibitor for CDK1, 2, 4, 6 and 9 with IC50 of 10-210 nM; less potent to CDK3 and little active to CDK7.

AT7519 is a novel multi-CDK inhibitor for CDK1/cyclin B, CDK2/Cyclin A, CDK3/Cyclin E, CDK4/Cyclin D1, CDK5/p35 and CDK6/Cyclin D3 with IC50 of 210 nM, 47 nM, 360 nM, 100 nM, 13 nM and 170 nM, respectively.

AT7519 trifluoroacetate is a multi-CDK inhibitor for CDK1, 2, 4, 6 and 9 with IC50 of 10-210 nM; less potent to CDK3 and little active to CDK7.

AT9283 is a small molecule a multi-targeted inhibitor with of 4, 1.2, 1.1 and approximate 3 nM for Bcr-Abl(T3151), Jak2 and Jak3, aurora A and B, respectively.

AZ 960 is a novel ATP competitive JAK2 inhibitor with IC50 and Ki of <3 nM and 0.45 nM, 3-fold selectivity of AZ960 for JAK2 over JAK3.

AZD1152 (barasertib), pro-drug of barasertib-hQPA, is a selective Aurora B kinase inhibitor, AZD1152 inhibited the proliferation various types of human leukemia cells with an IC50 ranging from 3 nM to 40 nM.

AZD5153 is a potent bivalent triazolopyridazine based Bromodomain and Extraterminal (BET) Inhibitor.

Bafetinib (INNO-406) is a potent and selective dual Bcr-Abl/Lyn inhibitor with IC50 of 5.8 nM and 19 nM, respectively.

BAY 1143572 is a highly selective, potent and orally available inhibitor of PTEFb/CDK9; inhibits the proliferation of AML cell lines with a median IC50 of 385 nM.

BAY-1436032 (BAY1436032) is a potent, selective, orally available inhibitor of pan-mutant IDH1 with IC50 of 15 nM for both IDH1 R132H and R132C, respectively.

BAY-1895344 is a potent and selective ATM inhibitor. BAY 1895344 shows potent anti-tumor efficacy in monotherapy and strong combination potential with the targeted alpha therapy Radium-223 dichloride.

Belizatinib(TSR-011) is an orally available inhibitor of both the receptor tyrosine kinase anaplastic lymphoma kinase (ALK) and the tropomyosin-related kinases (TRK) TRKA, TRKB, and TRKC, with potential antineoplastic activity.

BGB-3111 is a potent, selective and orally available Bruton's tyrosine kinase (Btk) inhibitor.

BGJ398 (NVP-BGJ398) is a potent and selective FGFR inhibitor for FGFR1/2/3 with IC50 of 0.9 nM/1.4 nM/1 nM, >40-fold selective for FGFR versus FGFR4 and VEGFR2, and little activity to Abl, Fyn, Kit, Lck, Lyn and Yes. Phase 2.

BI2536 is a potent Plk1 inhibitor with IC50 of 0.83 nM, BI2536 shows 4- and 11-fold greater selectivity against Plk2 and Plk3; BI2536 also is a BRD4 inhibitor(IC50= 25 nM).

BKM120 is a selective PI3K inhibitor of p110α/β/δ/γ with IC50 of 52 nM/166 nM/116 nM/262 nM, respectively. Reduced potency against VPS34, mTOR, DNAPK, with little activity to PI4Kβ.

BMS-906024 is a highly potent, selective inhibitor of γ-secretase mediated signaling of Notch1/2/3/4 receptors with IC50 of 1.6/0.7/3.4/2.9 nM, respectively.

Bortezomib is a potent 20S proteasome inhibitor with Ki of 0.6 nM.

CA4948-Analog is an analog of Emavusertib. It has similar property to CA-4948, which is a potent, and orally active interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor. It was reported in patent WO 2015104688. Emavusertib, also known as CA-4948 i

CAL-101 is a selective p110δ inhibitor with IC50 of 2.5 nM; shown to have 40- to 300-fold greater selectivity for p110δ thanp110α/β/γ, and 400- to 4000-fold more selectivity to p110δ than C2β, hVPS34, DNA-PK and mTOR.

Carfilzomib is an irreversible proteasome inhibitor with an IC50 of 5 nM in ANBL-6 and RPMI 8226 cells,showed potent activity against COVID-19(SARS-COV-2).

CB-5083 is a novel first in class, potent orally bio-available p97 inhibitor that disrupts cellular protein homeostasis and demonstrates anti-tumor activity in solid and hematological models .

CC-115 is a dual inhibitor of DNA-dependent protein kinase (DNA-PK) and mammalian target of rapamycin (mTOR), with potential antineoplastic activity.

CC-122 is a novel agent for DLBCL with antitumor and immunomodulatory activity.CC-122 binds CRBN and degrades Aiolos and Ikaros resulting in a mimicry of IFN signaling and apoptosis in DLBCL.

CC-223 is a potent mTOR kinase inhibitor (IC50=16 nM), with >150-fold sensitivity over the related lipid kinase PI3Kα (IC50=4 μM).

CC-401 is a second generation ATP-competitive anthrapyrazolone c-Jun N terminal kinase (JNK) inhibitor with potential antineoplastic activity.

Chidamide is a class I HDAC inhibitor with IC50s of 95/160/67/733 nM for HDAC1/2/3/8; also inhibits HDAC10/11(IC50=78/432 nM); no inhibition on HDAC4/5/7/9/6(IC50>30 uM).

CHR-2797 is an aminopeptidase inhibitor, with IC50 values of 100 nM for LAP3 (LAP), 150 nM for PSAP (PuSA) and 220 nM for CD13 (Aminopeptidase N).

CHZ868 is a type II JAK2 inhibitor with an IC50 of 0.17 μM in EPOR JAK2 WT Ba/F3 cell.

CNDAC is the active component of sapacitabine.

Crenolanib (CP-868596) is a potent and selective inhibitor of PDGFRα/β with Kd of 2.1 nM/3.2 nM, also potently inhibits FLT3, sensitive to D842V mutation not V561D mutation, >100-fold more selective for PDGFR than c-Kit, VEGFR-2, TIE-2, FGFR-2, EGFR, erbB

CX-4945 (Silmitasertib) is a potent and selective ATP-competitive small molecule protein kinase CK2 inhibitor with a Ki and an IC50 of 0.38 and 1 nM for recombinant human CK2α, respectively.

CX-6258 is a potent, orally efficacious Pim 1/2/3 kinase(IC50=5 nM/25 nM/16 nM) inhibitor with excellent biochemical potency and kinase selectivity.

CYT997 is a potent microtubule polymerization inhibitor with IC50 of 10-100 nM in cancer cell lines. Phase 1/2.

Danusertib (PHA-739358) is an Aurora inhibitor for Aurora A/B/C, Bcr-Abl, c-RET and FGFR with IC50 of 13 nM/79 nM/61 nM, 25 nM, 31 nM and 47 nM, respectively.

Dasatinib (BMS-354825, Sprycel) is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of ＜1 nM, 0.5 nM and 79 nM, respectively.

DCC-2036 is a conformational control Bcr-Abl inhibitor for Abl1(WT) and Abl1(T315I) with IC50 of 0.8 nM and 4 nM, also inhibits SRC, LYN, FGR, HCK, KDR, FLT3, and Tie-2, and low activity to seen towards c-Kit. Phase 1/2.

DDP-38003 dihydrochloride is an novel, orally available inhibitor of histone lysine-specific demethylase 1A (KDM1A/LSD1) with an IC50 of 84 nM.

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.

Dinaciclib (SCH727965) is a novel and potent CDK inhibitor for CDK2, CDK5, CDK1 and CDK9 with IC50 of 1 nM, 1 nM, 3 nM and 4 nM, respectively.

Dovitinib (TKI258, CHIR258) is a novel multi-target inhibitor for Flt3, c-Kit, FGFR1/3, VEGFR1/2/3, PDGFRα/β with IC50 of 1 nM, 2 nM, 8 nM/9 nM and 10 nM/13 nM/8 nM, 210 nM/27 nM respectively.

Dovitinib(CHIR-258; TKI258) lactate is a potent inhibitor of fibroblast growth factor receptor 3 (FGFR3) with an IC50 of 5 nM.

Milademetan (DS-3032) is a specific and orally active MDM2 inhibitor for the research of acute myeloid leukemia (AML) or solid tumors. Milademetan (DS-3032) induces G1 cell cycle arrest, senescence and apoptosis.

Tomivosertib (eFT-508) is a potent and selective MNK1/2 inhibitor with IC50s of 2.4 nM and 1 nM, respectively. It potentially results in decreased tumor cell proliferation and tumor growth. Tomivosertib (eFT-508) inhibits eIF4E phosphorylation and dramatically downregulates PD-L1 protein abundance.

Enzastaurin (LY317615) is a potent PKCβ selective inhibitor with IC50 of 6 nM, 6- to 20-fold selectivity against PKCα, PKCγ and PKCε. Phase 3.

EPZ011989 is a potent, orally-available EZH2 Inhibitor.

Erdafitinib (JNJ-42756493) is a potent and orally available FGFR family inhibitor; inhibits FGFR1-4 with IC50 values of 1.2, 2.5, 3.0 and 5.7nM, respectively.

EW-7197 is a potent ALK5 inhibitor. EW-7197 showed potent in vivo anti-metastatic activity, indicating its potential for use as an anti-cancer therapy.

Flavopiridol competes with ATP to inhibit CDKs including CDK1, CDK2, CDK4 and CDK6 with IC50 of ~ 40 nM, and CDK7 with IC50 of 300 nM.

Flavopiridol hydrochloride competes with ATP to inhibit CDKs including CDK1, CDK2, CDK4 and CDK6 with IC50 of ~ 40 nM. It is 7.5-fold more selective for CDK1/2/4/6 than CDK7. Flavopiridol is initially found to inhibit EGFR and PKA.

FLT3/AXL inhibitor

Pexmetinib is a potent Tie-2 and p38 MAPK dual inhibitor, with IC50s of 1 nM, 35 nM and 26 nM for Tie-2, p38α and p38β, respectively, and can be used in the research of acute myeloid leukemia.

GDC0575（ARRY-575，RG7441）is a small molecule inhibitor of cell cycle checkpoint kinase 1 (Chk1), with potential chemosensitization activity.

GSK 525762A is a potent small molecule inhibitors that disrupt the function of the BET family of bromodomains (Brd2, Brd3, and Brd4).

GSK3326595(EPZ015938) is the first-in-class protein arginine methyltransferase-5 (PRMT5) inhibitor.

GSK690693 is a pan-Akt inhibitor targeting Akt1, Akt2 and Akt3 with IC50 of 2 nM, 13 nM, and 9 nM, respectively.

IACS-010759 (IACS010759) is a small molecule inhibitor of mitochondrial oxidative phosphorylation (OXPHOS), targets complex I of the mitochondrial electron transport chain.

Iberdomide (CC-220) is a cereblon modulator in clinical development for systemic lupus erythematosis. Iberdomide exhibits an IC50 of 60 nM in TR-FRET cereblon binding assay.

ICG-001 is a small-molecule antagonist of b-catenin/TCF-mediated transcription (IC50 = 3 uM) and specifically downregulates the expression of a subset of b-catenin/TCF-responsive genes. ICG-001 binds specifically to cyclic AMP response element-binding pro

Imatinib Mesylate is orally bioavailability mesylate salt of Imatinib, which is a multi-target inhibitor of v-Abl, c-Kit and PDGFR with IC50 of 0.6 μM, 0.1 μM and 0.1 μM, respectively.

IPI-145 is an orally bioavailable, highly selective and potent small molecule inhibitor of the delta and gamma isoforms of phosphoinositide-3 kinase (PI3K) with potential immunomodulating and antineoplastic activities.

Itacitinib is a potent and selective inhibitor of JAK1, with >20-fold selectivity for JAK1 over JAK2 and >100-fold over JAK3 and TYK2; Itacitinib is used in the research of myelofibrosis.

KPT-330, analog of KPT-185, is an orally bioavailable selective CRM1 inhibitor.

KW 2449 is a multikinase inhibitor of FLT3, ABL, ABL-T315I, and Aurora kinase.

KW-2478 is a nonansamycin HSP90 inhibitor with IC50 of 3.8 nM. Phase 1/2

LOXO-101 is a small molecule that was designed to block the ATP binding site of the TRK family of receptors, with 2 to 20 nM cellular potency against the TRKA, TRKB, and TRKC kinases.

ORY-1001 dihydrochloride (RG-6016, Ladademstat) is a highly potent, selective inhibitor of lysine-specific demethylase KDM1A (LSD1) with IC50 of 18 nM, displays high selectivity for KDM1A over other FAD-containing monoamine oxidases.

LY2157299 is a potent TGFβ receptor I (TβRI) inhibitor with IC50 of 56 nM. Phase 2.

LY2784544 is a potent JAK2 inhibitor with IC50 of 3 nM, effective in JAK2V617F, 8- and 20-fold selective versus JAK1 and JAK3. Phase 2.

LY2874455 is a novel and potent FGF/FGFR inhibitor.

LY3039478 a orally bioavailable, novel small molecule Notch inhibitor with an IC50 of ~1nM in most of the tumor cell lines tested.

LY3214996 is a selective and novel ERK1/2 inhibitor with IC50 of 5 nM for both enzymes in biochemical assays. It potently inhibits cellular phospho-RSK1 in BRAF and RAS mutant cancer cell lines.

LY335979 (Zosuquidar) is a potent modulator of P-glycoprotein-mediated multidrug resistance with Ki of 60 nM.

MAK683 is a novel PRC2/EED inhibitor.

Methoxsalen (Oxsoralen)

MGCD0103 (Mocetinostat) is a potent HDAC inhibitor with IC50 of 0.15, 0.29 and 1.66 μM for HDAC 1, HDAC 2 and HDAC 3, respectively.

MI-503 is a highly potent and orally bioavailable small molecule inhibitor of the menin-MLL interaction.

MI-77301 (SAR405838) is an orally available MDM2 antagonist with Ki of 0.88 nM. Phase 1.

MLN2238 inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with IC50 and Ki of 3.4 nM and 0.93 nM, respectively, also inhibits the caspase-like (β1) and trypsin-like (β2) proteolytic sites, with IC50 of 31 and 3500 nM.

MLN4924 is a small molecule inhibitor of Nedd8 activating enzyme (NAE) with IC50 of 4 nM.

MLN-9708 is a proteasome inhibitor, which inhibits the activity of the proteasome, blocking the targeted proteolysis normally performed by the proteasome.

Nilotinib (AMN-107, Tasigna) is a Bcr-Abl inhibitor with IC50 less than 30 nM.

NVP-AEW541 is a potent inhibitor of IGF-1R with IC50 of 86 nM.

NVP-TAE684(TAE684) is a highly potent and selective small-molecule ALK inhibitor, which blocked the growth of ALCL-derived and ALK-dependent cell lines with IC50 values between 2 and 10 nM.

Olutasidenib is a highly potent, selective inhibitor of mutant Isocitrate dehydrogenase (IDH)1 that could be used in the treatment of acute myeloid leukemia.

ONO-4059 is a highly selective, orally bioavailable BTK inhibitor with a potency (IC50) of 2.2 nM.

ONO-4059 is a novel Small Molecule Dual Inhibitor Of Bruton’s Tyrosine Kinase (Btk) and Tec Kinase.

Oprozomib (ONX 0912) selectively inhibits CT-L activity of 20S proteasome β5/LMP7 with IC50 of 36 nM/82 nM.

OSI-027 is a selective and potent dual inhibitor of mTORC1 and mTORC2 with IC50 of 22 nM and 65 nM, respectively.

OSU-03012(AR-12) is a potent inhibitor of recombinant PDK-1 with IC50 of 5 μM and 2-fold increase in potency over OSU-02067.

OTSSP167 is a highly potent MELK inhibitor (IC50 = 0.41 nM) and inhibited the phosphorylation of PSMA1 (proteasome subunit alpha type 1) and DBNL (drebrin-like).

OTSSP167 is a highly potent MELK inhibitor (IC50 = 0.41 nM) and inhibited the phosphorylation of PSMA1 (proteasome subunit alpha type 1) and DBNL (drebrin-like).

PAK4-IN-1 is an inhibitor of p21-activated kinases (PAKs), with IC50 of ≤100 nM in MTT assay.

Panobinostat(LBH-589) is a broad-spectrum HDAC inhibitor; low nanomolar concentrations (IC50=5-20 nM) of LBH589 induced cell-cycle arrest, apoptosis, and histone (H3K9 and H4K8) hyperacetylation in MOLT-4 and Reh cell.

PCI-32765 (Ibrutinib) is a potent and highly selective Btk inhibitor with IC50 of 0.5 nM.

PF-04449913 is a potent and orally bioavailable inhibitor of smoothened with IC50 of 5 nM(Gli-luciferase reporter reporter in C3H10T1/2); the hedgehog pathway inhibitor

PIM447 is novel pan-PIM kinase inhibitor, including Moloney Murine Leukemia (PIM) 1, 2, and 3 Kinase.

PKC-412 is a broad spectrum protein kinase inhibitor. Inhibits conventional PKC isoforms (α, β, γ), PDFRβ, VEGFR2, Syk, PKCη, Flk-1, Flt3, Cdk1/B, PKA, c-Kit, c-Fgr, c-Src, VEGFR1 and EGFR. Displays potent antitumor activity.

PKI-587 is a highly potent dual PI3K/mTOR kinase inhibitor with IC50 of 0.4 nM and <0.1 μM for PI3K-α and mTOR, respectively.

Plerixafor is a chemokine receptor antagonist for CXCR4 and CXCL12-mediated chemotaxis with IC50 of 44 nM and 5.7 nM, respectively.

PLX51107 is a novel BET inhibitor with a unique binding mode in the acetylated lysine binding pocket of BRD4 that differentiates it from other compounds under investigation.

Pracinostat(SB939) is a potent pan-HDAC inhibitor with IC50 of 40-140 nM with exception for HDAC6; has no activity against the class III isoenzyme SIRT I.

PRIMA-1 is a mutant p53 reactivator, restores the sensitivity of TP53 mutant-type thyroid cancer cells to the histone methylation inhibitor 3-Deazaneplanocin A.

PX-478 is an inhibitor of HIF-1a with an IC50 of 20-30μM enhances radiosensitivity of prostate carcinoma cells.

Quarfloxin (CX-3543) is a fluoroquinolone derivative with antineoplastic activity.

Quizartinib (AC220) is a second-generation FLT3 inhibitor for Flt3(ITD/WT) with IC50 of 1.1 nM/4.2 nM, 10-fold more selective for Flt3 than KIT, PDGFRα, PDGFRβ, RET, and CSF-1R. Phase 1/2.

Rigosertib (ON-01910) is a non-ATP-competitive inhibitor of PLK1 with IC50 of 9 nM; shows 30-fold greater selectivity against PLK2 and no activity to PLK3.

S55746 hydrochloride is a potent, orally active and selective BCL-2 inhibitor, with Kis and Kds of 1.3 nM, 520 nM and 3.9 nM, 186 nM for BCL-2 and BCL-XL, respectively. S55746 hydrochloride has antitumor activity.

S55746 (BLC201) is a potent, orally active and selective BCL-2 inhibitor, with a Ki of 1.3 nM and a Kd of 3.9 nM. S55746 (BLC201) has antitumor activity with low toxicity[1].

S63845 is a potent and selective myeloid cell leukemia 1 (MCL1) inhibitor; binds human MCL1 with a Kd of 0.19 nM.

SB743921 is a kinesin spindle protein (KSP) inhibitor with Ki of 0.1 nM, almost no affinity to MKLP1, Kin2, Kif1A, Kif15, KHC, Kif4 and CENP-E.

SCH 900776 is a selective Chk1 inhibitor with IC50 of 3 nM. It shows 50-fold selectivity against Chk2. Phase 2.

SGI-110 (S-110) is a stable and potent inhibitor for DNA methylation, inhibits DNMT1 when SGI-110 is activated by phosphorylation and incorporated into DNA.

SNS-032(BMS-387032) is a potent inhibitor of cyclin-dependent kinases (cdks) 9, 2 and 7 (IC50 values are 4, 38 and 62 nM respectively).

Sotrastaurin(AEB-071) is a potent and selective pan-PKC inhibitor, mostly for PKCθ with Ki of 0.22 nM; inactive to PKCζ.

TAK-659 hydrochloride is a potent, selective and orally available spleen tyrosine kinase (Syk) inhibitor with an IC50 of 3.2 nM.

TAK-901 is a non-selective Aurora kinase inhibitor (IC50s = 3.1, 10, and 4.2 nM for Aurora A, B, and C, respectively).

Tasisulam sodium is The sodium salt of an acyl-sulfonamide with potential antineoplastic activity.

Tenalisib (RP6530) is a novel, potent, and selective PI3Kδ and PI3Kγ inhibitor with IC50 values of 25 and 33 nM, respectively.

TGR-1202 hydrochloride is an orally available, next generation PI3Kdelta inhibitor, inhibits PI3Kδ activity in enzyme and cell based assays with IC50 and EC50 values of 22.2 and 24.3 nM respectively.

TGR-1202 is an orally available, next generation PI3Kdelta inhibitor, inhibits PI3Kδ activity in enzyme and cell based assays with IC50 and EC50 values of 22.2 and 24.3 nM respectively.

The water-soluble prodrug of GMX-1778 (CHS-828), which is a potent and specific inhibitor of the NAD(+) biosynthesis enzyme NAMPT with IC50 of <20 nM.

Tinostamustine is the first representative of the A-DAC principle, a new approach in chemotherapy that uses fusion technology to combine an alkylating agent with a pan-histone deacetylase inhibitor (HDAC) to simultaneously damage DNA and block damage repa

Tipifarnib (IND 58359; R115777) is a potent and specific farnesyltransferase inhibitor with an IC50 of 0.6 nM.

Valspodar(PSC833) is a P-glycoprotein (P-gp) inhibitor widely used in preclinical and clinical studies for overcoming multidrug resistance (MDR).

VLX1570 is a competitive inhibitor of proteasome DUB activity, with an IC50 of ~10 μM in vitro.

Volasertib(BI6727) is a highly potent PLK1 inhibitor with an IC50 of 0.87 nM; shows 6- and 65-fold greater selectivity against Plk2 and Plk3.

Vorinostat (SAHA) is an HDAC1/3 inhibitor with IC50 of ~10 nM.

Voruciclib is a protein kinase inhibitor specific for the cyclin-dependent kinase 4 (CDK4) with potential antineoplastic activity.

VX-680 (MK-0457, Tozasertib) is a pan-Aurora inhibitor of Aurora A, Aurora B and Aurora C with Kiapp of 0.6 nM, 18 nM and 4.6 nM, respectively.

YM155 is a potent IAP (inhibitor of apoptosis proteins) inhibitor for survivin with IC50 of 0.54 nM.

ZM-447439 is a selective and ATP-competitive inhibitor for Aurora A and Aurora B with IC50 of 110 nM and 130 nM, respectively.

Motixafortide (BKT140 4-fluorobenzoyl) is a novel CXCR4 antagonist with an IC50 vakue of ～1 nM.

GSK461364 is a potent small molecule Polo-like kinase 1 (PLK1) inhibitor with a Ki of 2.2 nM.