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Tankyrase-IN-2

" in MedChemExpress (MCE) Product Catalog:

By Targets:	PARP (7) Wnt (5) β-catenin (2)
By Research Areas:	Cancer (7) Neurological Disease (1)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-145584

Nesuparib JPI-547/OCN-201	PARP Wnt β-catenin	Neurological Disease Cancer
Nesuparib (JPI-547) is the orally active inhibitor for PARP 1/2 and *Tankyrase 1/2* that inhibits tankyrases 1, tankyrases 2, and PARP 1 with IC₅₀s of 5, 1 and 2 nM, respectively. Nesuparib exhibits antitumor activity and can be used in research of advanced solid tumor ^[2] .

HY-137849

RK-582	PARP	Cancer
RK-582 is a tankyrase inhibitor, antitumor agent, and orally bioavailable growth inhibitor, with an IC₅₀ of 36.1 nM against human *tankyrase-1* and an IC₅₀ of 39.2 nM against human *tankyrase-2. In APC-mutated colorectal cancer cells, the sensitivity to RK-582 correlates with the level of active β-catenin*, while drug resistance associates with PIK3CA mutation. RK-582 can be used for the research of colorectal cancer ^[2].

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-123892

RK-287107 1 Publications Verification	PARP	Cancer
RK-287107 is a potent and specific *tankyrase* inhibitor with IC₅₀s of 14.3 and 10.6 nM for *tankyrase-1* and *tankyrase-2*, respectively. RK-287107 blocks colorectal cancer cell growth .

HY-117705

G244-LM	Wnt PARP	Cancer
G244-LM is a potent and specific inhibitor of *tankyrase 1/2* that inhibits Wnt signaling .

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 IC₅₀**s of 0.709 μM and 0.215 μM, respectively ^[2].

HY-145584A

Nesuparib hydrochloride JPI-547/OCN-201 hydrochloride	PARP Wnt β-catenin	Cancer
Nesuparib (JPI-547) hydrochloride is the orally active inhibitor for PARP 1/2 and *Tankyrase 1/2* that inhibits tankyrases 1, tankyrases 2, and PARP 1 with IC₅₀s of 5, 1 and 2 nM, respectively. Nesuparib hydrochloride exhibits antitumor activity and can be used in research of advanced solid tumor ^[2] .

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MCE Japan Authorized Agent ナミキ商事株式会社コスモ・バイオ株式会社重松貿易株式会社
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BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.

BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

MedchemExpress Validation 03

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred

MedchemExpress Validation 04

MedchemExpress Validation

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Tankyrase-IN-2

Inhibitors & Agonists