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TNKS inhibitor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	TNK1 (6) AAK1 (1) Apoptosis (4) Aurora Kinase (1) CaMK (2) CDK (1) Epigenetic Reader Domain (1) ERK (1) Ferroptosis (1) LIM Kinase (LIMK) (1) LRRK2 (2) PARP (36) PPAR (1) PROTACs (1) Salt-inducible Kinase (SIK) (1) STAT (2) Tyrosinase (3) ULK (1) Wnt (6) β-catenin (4)
By Research Areas:	Cancer (42) Cardiovascular Disease (1) Inflammation/Immunology (2) Metabolic Disease (1) Neurological Disease (2)

Inhibitors & Agonists

Fluorescent Dye

Biochemical Assay Reagents

Targets Recommended: TNK1

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-23338

TNKS-2-IN-1	PARP	Others
TNKS-2-IN-1 (Compound 13g) is a *TNKS-2* inhibitor. TNKS-2-IN-1 inhibits TNKS-1 and TNKS-2 with IC₅₀s of 259 nM and 1100 nM .

HY-156332

TNKS-2-IN-2	PARP	Cancer
TNKS-2-IN-2 is a potent and selective inhibitor of *TNKS2* with an IC₅₀ of 22 nM .

HY-U00422

K-756 2 Publications Verification	PARP	Cancer
K-756 is a direct and selective tankyrase (TNKS) inhibitor, which inhibits the ADP-ribosylation activity of *TNKS1* and *TNKS2* with IC₅₀s of 31 and 36 nM, respectively.

HY-145111

TNK2-IN-1	Tyrosinase	Cancer
TNK2-IN-1 is a *TNK2* inhibitor. TNK2-IN-1 has an IC₅₀ of 224 nM for TNK2. TNK2-IN-1 can be used for the research of cancer .

HY-153259

TNKS1/2-IN-2	TNK1 PARP	Cancer
TNKS1/2-IN-2 (Compound 21) is a potent and selective tankyrases inhibitor. TNKS1/2-IN-2 exhibits IC₅₀ values of 4 nM and 63 nM against TNK1 and TNK2 in the enzymatic assay, respectively. TNKS1/2-IN-2 inhibits proliferation of A549 and H292 cell lines with IC₅₀ values of 39.5 nM and 12.8 nM, respectively. TNKS1/2-IN-2 can be used for the research of cancer .

HY-12601

TNKS 22 TNKS-IN-22	PARP	Cancer
TNKS 22 (compound 22) is an orally active and selective tankyrase inhibitor. TNKS 22 inhibits *TNKS1* and *TNKS2* with IC₅₀s of 0.1 and 4.1 nM, respectively .

HY-12577

TNKS1/2-IN-1	PARP	Cancer
TNKS1/2-IN-1 is a potent tankyrase TNKS1/2 inhibitor with pIC₅₀s ranging from 7.1-8.2. TNKS1/2-IN-1 can be used for research of cancer, fibrosis, and other hyperproliferative diseases .

HY-172747

TNKS-2-IN-3	PARP	Cancer
TNKS-2-IN-3 (Compound 5) is a selective competitive tankyrase 2 (TNKS2) inhibitor with an IC₅₀ value of 0.3 nM, showing over 20-fold selectivity over TNKS1 and more than 100-fold selectivity over PARP1/2. TNKS-2-IN-3 stabilizes axin and suppresses the Wnt/β-catenin pathway by inhibiting TNKS2-mediated ADP-ribosylation, exhibiting antiproliferative activity in colorectal cancer cells. TNKS-2-IN-3 is proming for rasearch of solid tumors with aberrant Wnt pathway activation, such as colorectal cancer .

HY-173480

TNKS-IN-3	PARP	Cancer
TNKS-IN-3 (Compound 6) is a *TNKS2* inhibitor (K_i: 8.5 nM). TNKS-IN-3 has good activity (IC₅₀: 71 nM) and can effectively inhibit the WNT/β-catenin signaling pathway. TNKS-IN-3 can be used in the research of diseases such as cancer and fibrosis .

HY-173349

TDI-012804	PARP	Cancer
TDI-012804 is a *TNKS2* inhibitor that selectively inhibits intracellular endogenous *TNKS2* protein. TDI-012804 increases the expression of AXIN1 protein in cells that are heterozygous (Tnks1HET) and completely knocks out (Tnks1KO) for TNKS1. TDI-012804 inhibits the proliferation of ApcQ1405X/Tnks1KO organoids (EC₅₀ of 59.1 nM) and is selectively toxic to Tnks1KO AKP-G12D and AKP-G13D organoids .

HY-12418

Stenoparib 2 Publications Verification E7449; 2X-121	PARP	Cancer
Stenoparib (E7449) is a potent PARP1 and PARP2 inhibitor and also inhibits *TNKS1* and *TNKS2, with IC₅₀s of 2.0, 1.0, ～50 and ～50 nM for PARP1, PARP2, TNKS1 and TNKS*2, respectively, using ³²P-NAD ⁺ as substrate.

HY-146336

PARP1/2/TNKS1/2-IN-1	PARP Apoptosis	Cancer
PARP1/2/TNKS1/2-IN-1 (Compound I-9) is a dual PARP-1, PARP-2, *TNKS1* and *TNKS2* inhibitor with IC₅₀ values of 0.25 nM, 1.2 nM, 13.5 nM and 4.15 nM against PARP-1, PARP-2, TNKS1 and TNKS2, respectively. PARP1/2/TNKS1/2-IN-1 exhibits favorable synergistic antitumor efficacy and induces apoptosis .

HY-147245

Basroparib STP1002	PARP	Cancer
Basroparib (STP1002) is a selective, orally active inhibitor of tankyrase (TNKS1/TNKS2) with IC₅₀ of 29.94 nM and 3.68 nM for TNKS1 and TNKS2, respectively. Basroparib has an IC₅₀ of >10 μM for PARP1. Basroparib binds to TNKS, stabilizes AXIN1/2 proteins, blocks Wnt/β-catenin signaling pathway, inhibits tumor cell proliferation and induces apoptosis, while reducing cancer stem cell properties. Basroparib can be used in colorectal cancer (CRC) studies with KRAS mutations (such as G12V/G12D) to overcome acquired resistance to MEK inhibitors. STP1002 has synergistic antitumor activity with MEK inhibitors .

HY-121719

TIQ-A	PARP	Cardiovascular Disease Cancer
TIQ-A is a potent *TNKS* (poly-ART, PARP) inhibitor, with an IC₅₀ of 24 nM for *TNKS2*. TIQ-A is a potential anti-ischemic agent .

HY-13968

JW 55 3 Publications Verification	PARP	Cancer
JW 55 is a potent and selective β-catenin signaling pathway inhibitor, which functions via inhibition of the PARP domain of tankyrase 1 and tankyrase 2 (TNKS1/2). JW 55 decreases auto-PARsylation of TNKS1/2 in vitro with IC₅₀s of 1.9 μM and 830 nM respectively.

HY-12438

G007-LK 5+ Cited Publications	PARP	Cancer
G007-LK is a potent and selective inhibitor of *TNKS1* and *TNKS2, with IC₅₀*s of 46 nM and 25 nM, respectively.

HY-13990G

NVP-TNKS656 TNKS656	PPAR Apoptosis	Cancer
NVP-TNKS656 (GMP) is NVP-TNKS656 (HY-13990) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. NVP-TNKS656 is a highly potent, selective, and orally active *TNKS2* inhibitor with IC₅₀ of 6 nM, and is > 300 fold selectivity against PARP1 and PARP2.

HY-117700

TNKS-IN-2	Wnt PARP	Cancer
TNKS-IN-2 (compound 40) is a potent and selective tankyrase (TNKS) inhibitor with pIC₅₀ values of 8.1, 7.0 for TANKS and Wnt, respectively .

HY-13990

NVP-TNKS656 TNKS656	PARP Apoptosis	Cancer
NVP-TNKS656 is a highly potent, selective, and orally active *TNKS2* inhibitor with IC₅₀ of 6 nM, and is > 300 fold selectivity against PARP1 and PARP2.

HY-19351

MN-64 3 Publications Verification	PARP	Cancer
MN-64 is a potent tankyrase 1 inhibitor, with IC₅₀s of 6 nM, 72 nM, 19.1 μM, and 39.4 μM for *TNKS1, TNKS*2, ARTD1 and ARTD2, respectively.

HY-153332

Tankyrase-IN-5	PARP	Cancer
Tankyrase-IN-5 (Compound 30f), an analogue of MSC2504877 (HY-123851), is a tankyrase *TNKS1* and *TNKS2* inhibitor with IC₅₀s of 2.3 nM and 7.9 nM, respectively .

HY-123851

MSC2504877 M2912	PARP	Cancer
MSC2504877 (M2912) is a potent and orally active tankyrase inhibitor with IC₅₀s of 0.0007, 0.0008, 0.54 µM for TNKS, TNKS2, PARP1, respectively. MSC2504877 increases the expression of AXIN2 and TNKS protein levels and decreases β-catenin levels. MSC2504877 shows anti-tumor activity .

HY-147886

PARP1-IN-11 1 Publications Verification	PARP	Cancer
PARP1-IN-11 (compound 49) is a potent PARP1 inhibitor with IC₅₀ value of 0.082 µM. PARP1-IN-11 shows complete inhibition of PARP2 and substantially inhibits PARP3, TNKS1 and TNKS2 .

HY-108516

TC-E 5001	Wnt PARP	Cancer
TC-E 5001 is an inhibitor of Wnt pathway that inhibits tankyrase 1/2 (TNKS1/2) via novel adenosine pocket binding, with K_ds of 79 nM and 28 nM, respectively. TC-E 5001 also inhibits Axin2 and STF, with IC₅₀s of 0.709 μM and 0.215 μM, respectively .

HY-16910

WIKI4 3 Publications Verification	PARP β-catenin Wnt	Cancer
WIKI4 is a potent tankyrase inhibitor with an IC₅₀ of 26 nM for *TNKS2. WIKI4 potently inhibits* Wnt/β-catenin signaling and that its half-maximal response dose is 75 nM. WIKI4 mediates its effects on Wnt/β-catenin signaling by inhibiting the enzymatic activity of *TNKS2* . WIKI4 is cytotoxic to SCLC cells with an IC₅₀ value of 0.02 μM .

HY-126248

Tankyrase-IN-2	PARP Wnt	Cancer
Tankyrase-IN-2 (compound 5k) is a potent, selective, and orally active tankyrase inhibitor (IC₅₀s of 10, 7, and 710 nM for TNKS1, TNKS2 as well as PARP1, respectively). Tankyrase-IN-2 has favorable physicochemical profile and pharmacokinetic properties modulating Wnt pathway activity in a colorectal xenograft model .

HY-12975

AZ6102 1 Publications Verification	PARP	Cancer
AZ6102 is a potent dual *TNKS1* and *TNKS2* inhibitor, with IC₅₀s of 3 nM and 1 nM, respectively, and alao has 100-fold selectivity against other PARP family enzymes, with IC₅₀s of 2.0 μM, 0.5 μM, and >3 μM, for PARP1, PARP2, and PARP6, respectively.

HY-152197

Tankyrase-IN-3	PARP	Cancer
Tankyrase-IN-3 is a tankyrase 1 (TNKS1) inhibitor with an IC₅₀ value of 22 nM. Tankyrase-IN-3 can be used for the research of cancer .

HY-145267

OM-153	PARP Wnt	Cancer
OM-153 is a potent and orally active tankyrase inhibitor with IC₅₀s of 13 nM and 2 nM for tankyrase 1 and tankyrase 2 (TNKS1/2), respectively. OM-153 inhibits luciferase-based Wnt/β-catenin signaling reporter activity with an IC₅₀ value of 0.63 nM. OM-153 shows inhibition of Wnt/β-catenin signaling and proliferation in COLO 320DM .

HY-152198

Tankyrase-IN-4	PARP	Cancer
Tankyrase-IN-4 is a tankyrase 1 (TNKS1) inhibitor with an IC₅₀ value of 0.8 nM. Tankyrase-IN-4 can be used for the research of cancer .

HY-15811

XMD8-87 ACK1-B19	Tyrosinase	Cancer
XMD8-87 is a potent *TNK2* inhibitor with IC₅₀ values of 38 and 113 nM for the D163E and R806Q mutations, respectively.

HY-101243

XMD16-5	Tyrosinase	Cancer
XMD16-5 is a potent *TNK2* inhibitor with IC₅₀ values of 16 and 77 nM for the D163E and R806Q mutations, respectively.

HY-137849

RK-582	PARP	Cancer
RK-582 is an orally active, spiroindoline-based selective inhibitor of tankyrase. The IC₅₀s of RK-582 against TNKS1/PARP5A and PARP1 are 36.1 nM and 18.168 nM, respectively. RK-582 inhibits rectal cancer COLO-320DM cells (GI50=0.23 μM) and significantly inhibits tumor growth in a COLO-320DM mouse xenograft model .

HY-168925

EXQ-2d	Wnt PARP β-catenin	Cancer
EXQ-2d is the inhibitor for tankyrase and inhibits *TNKS1* and *TNKS2* with an IC₅₀ of 48.8 nM and 13.8 nM (pIC₅₀=7.31 and 7.86). EXQ-2d inhibits WNT/β-catenin signaling pathway with IC₅₀ of 515 nM. EXQ-2d exhibits anti-proliferative activity in cancer cells COLO 320DM and RKO with GI₅₀ of 4.9 μM and 77 μM .

HY-15147

XAV-939 Maximum Cited Publications 149 Publications Verification	β-catenin PARP	Cancer
XAV-939 is a Tankyrase inhibitor. XAV-939 has inhibitory activity for TNKS1 and TNKS2 with IC₅₀ values of 5 nM and 2 nM, respectively. XAV-939 also is an enhancer of osteoblastic differentiation of hMSCs. XAV-939 can be used for the research of conditions associated with activated Wnt signaling, such as cancer, fibrotic diseases and conditions associated with low bone formation .

HY-147316

TP-5801	STAT TNK1	Cancer
TP-5801 is an orally active *TNK1* (non-receptor tyrosine kinase) inhibitor (IC₅₀=1.40 nM), and shows anti-tumor activity .

HY-147316A

TP-5801 TFA	STAT TNK1	Cancer
TP-5801 TFA is an orally active *TNK1* (non-receptor tyrosine kinase) inhibitor (IC₅₀=1.40 nM), and shows anti-tumor activity .

HY-W294889

OUL245	PARP	Cancer
OUL245 is a 7-Hydroxy derivative, and a selectively PARP2 inhibitor (IC₅₀=44 nM). OUL245 also inhibits other PARP and TNKS enzymes with IC₅₀s of 2.9-8.8 μM .

HY-100847

AZ0108	PARP	Cancer
AZ0108 is an inhibitor for poly ADP-ribose polymerase (PARP), which inhibits PARP1, PARP2, PARP3, PARP6, TNKS1, TNKS2, with IC₅₀s of <0.03, <0.03, 2.8, 0.083, 3.2, >3 μM, respectively. AZ0108 prevents centrosome clustering with an EC₅₀ of 0.053 μM, and exhibits cytotoxicity in cell OCI-LY-19 with GI₅₀ of 0.017 μM. AZ0108 exhibits good in vivo pharmacokinetic characters in rat/mouse models .

HY-15147R

XAV-939 (Standard)	β-catenin PARP	Cancer
XAV-939 (Standard) is the analytical standard of XAV-939. This product is intended for research and analytical applications. XAV-939 is a Tankyrase inhibitor. XAV-939 has inhibitory activity for TNKS1 and TNKS2 with IC50 values of 5 nM and 2 nM, respectively. XAV-939 also is an enhancer of osteoblastic differentiation of hMSCs. XAV-939 can be used for the research of conditions associated with activated Wnt signaling, such as cancer, fibrotic diseases and conditions associated with low bone formation .

HY-143338

ART-IN-1	PARP	Cancer
ART-IN-1 (compound 7) is a selective PARP inhibitor with IC₅₀s of 19, 22, 2.4, >100, 1.1 µM for PARP2, TNKS2, PARP10, PARP14, PARP15, respectively .

HY-14443

XMD8-92 10+ Cited Publications	Epigenetic Reader Domain ERK TNK1 CaMK	Cancer
XMD8-92 is a potent ERK5 (BMK1)/BRD4 inhibitor with K_ds of 80 and 190 nM, respectively. XMD8-92 inhibits DCAMKL2, PLK4 and TNK1 with K_ds of 190, 600 and 890 nM, respectively. Anti-cancer activity .

HY-155246

PARP1-IN-15	Apoptosis PARP	Cancer
PARP1-IN-15 (Compound 6) is a PARP1 inhibitor. PARP1-IN-15 inhibits tankyrase (TNKS) and facilitates DNA double-strand breaks damage. PARP1-IN-15 induces tumor cell apoptosis. PARP1-IN-15 has anti-cancer activity in triple-negative breast cancer (TNBC) cells and TNBC patient-derived organoids. PARP1-IN-15 can be used for research of TNBC with or without BRCA1 mutations .

HY-15800

CZC-25146 hydrochloride	TNK1 LRRK2	Neurological Disease Inflammation/Immunology
CZC-25146 hydrochloride is a potent LRRK2 inhibitor with IC₅₀ values of 4.76 nM and 6.87 nM for wild-type LRRK2 and G2019S LRRK2, respectively. CZC-25146 hydrochloride inhibits PLK4, GAK, TNK1, CAMKK2 and PIP4K2C as well. CZC-25146 hydrochloride prevents mutant LRRK2-induced injury of neurons in vitro. CZC-25146 hydrochloride exhibits relatively favorable pharmacokinetic properties in mice. CZC-25146 hydrochloride can increase normal α-1-antitrypsin (AAT) secretion and reduce inflammatory cytokines. CZC-25146 hydrochloride can be used to research Parkinson's disease and liver diseases .

HY-15800A

CZC-25146	TNK1 LRRK2	Neurological Disease Inflammation/Immunology
CZC-25146 is a potent and orally active LRRK2 inhibitor with IC₅₀ values of 4.76 nM and 6.87 nM for wild-type LRRK2 and G2019S LRRK2, respectively. CZC-25146 inhibits PLK4, GAK, TNK1, CAMKK2 and PIP4K2C as well. CZC-25146 prevents mutant LRRK2-induced injury of neurons in vitro. CZC-25146 exhibits relatively favorable pharmacokinetic properties in mice. CZC-25146 can increase normal α-1-antitrypsin (AAT) secretion and reduce inflammatory cytokines. CZC-25146 can be used to research Parkinson's disease and liver diseases .

HY-148063

DB0614	PROTACs AAK1 Aurora Kinase CaMK CDK Ferroptosis Salt-inducible Kinase (SIK) LIM Kinase (LIMK) ULK	Metabolic Disease
DB0614 is a PROTAC based on Cereblon ligand, which is a selective and potent targeted protein degrader of NEK9 inhibitor. DB0614 can degrade ABL1, ABL2, BLK, CDK11B, CDK4, CSK, EPHA3, FER, GAK, LIMK1, MAP3K20, MAP4K1, MAP4K2, MAP4K3, MAP4K5, MAPK14, MAPK7, MAPK8, MAPK9, MAPKAPK2, MAPKAPK3, NLK, PDIK1L, PTK2B, RIPK1, RPS6KA1, RPS6KA3, SIK2, SIK3, STK35, TNK2 and ULK1. DB0614 can be used for research of disease or disorder mediated by aberrant kinase activity .(Blue: Thalidomide-4-OH (HY-103596), Black: linker, Pink: FLT3-IN-17 (HY-148070))

Cat. No.	Product Name	Type

HY-13990G

NVP-TNKS656 (GMP) TNKS656 (GMP)	Fluorescent Dye
NVP-TNKS656 (GMP) is NVP-TNKS656 (HY-13990) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. NVP-TNKS656 is a highly potent, selective, and orally active *TNKS2* inhibitor with IC₅₀ of 6 nM, and is > 300 fold selectivity against PARP1 and PARP2.

Cat. No.	Product Name	Type

HY-13990G

NVP-TNKS656 (GMP) TNKS656 (GMP)	Biochemical Assay Reagents
NVP-TNKS656 (GMP) is NVP-TNKS656 (HY-13990) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. NVP-TNKS656 is a highly potent, selective, and orally active *TNKS2* inhibitor with IC₅₀ of 6 nM, and is > 300 fold selectivity against PARP1 and PARP2.

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